Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
51353551 17950 10 None 1 3 Human 11.0 pEC50 = 11 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 17950 10 None 1 3 Human 11.0 pEC50 = 11 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
51353551 17950 10 None 1 3 Human 10.9 pEC50 = 10.9 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 17950 10 None 1 3 Human 10.9 pEC50 = 10.9 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
10649606 49349 0 None 4 2 Human 10.9 pEC50 = 10.9 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None 4 2 Human 10.9 pEC50 = 10.9 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
10649606 49349 0 None 4 2 Human 10.7 pEC50 = 10.7 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None 4 2 Human 10.7 pEC50 = 10.7 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
44336539 5075 0 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10819755 164890 0 None 218776 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL423907 164890 0 None 218776 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24769543 188119 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504406 188119 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
44562302 187608 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 666 11 2 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL498958 187608 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 666 11 2 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
24769604 188104 0 None -1 2 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504114 188104 0 None -1 2 Mouse 10.5 pEC50 = 10.5 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
10649606 49349 0 None 4 2 Human 10.4 pEC50 = 10.4 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None 4 2 Human 10.4 pEC50 = 10.4 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
44562297 188038 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 631 9 2 7 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL502974 188038 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 631 9 2 7 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
4627 809 44 None -1 6 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
864 809 44 None -1 6 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
9833444 809 44 None -1 6 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
CHEMBL1121 809 44 None -1 6 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
DB09142 809 44 None -1 6 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
24861113 187607 0 None 24 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL498942 187607 0 None 24 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL506201 187607 0 None 24 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
44336539 5075 0 None 1 3 Human 10.3 pEC50 = 10.3 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None 1 3 Human 10.3 pEC50 = 10.3 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
24861114 188550 3 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 582 7 1 6 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL510690 188550 3 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 582 7 1 6 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
44562301 188464 0 None 3 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL509464 188464 0 None 3 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24861060 188141 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446789 188141 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504861 188141 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
24861060 188141 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL446789 188141 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL504861 188141 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
155530671 170996 0 None 47863 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1627 65 14 19 4.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4464703 170996 0 None 47863 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1627 65 14 19 4.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
46869398 61595 0 None 5 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774043 61595 0 None 5 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
24769605 178142 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL468372 178142 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
53233689 61527 0 None 2 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773877 61527 0 None 2 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
155524181 170286 0 None 4 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 71 18 22 2.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4453982 170286 0 None 4 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 71 18 22 2.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24769604 188104 0 None 1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504114 188104 0 None 1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
44562304 188288 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 664 9 3 7 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(=O)NC)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL507094 188288 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 664 9 3 7 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(=O)NC)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
24861394 188468 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 592 5 1 7 5.6 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL509519 188468 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 592 5 1 7 5.6 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2008.06.057
44578457 171904 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL448221 171904 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44562300 188052 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503107 188052 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24769546 172120 0 None 2 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL450105 172120 0 None 2 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24861391 188165 0 None 2 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
CHEMBL505225 188165 0 None 2 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
CHEMBL505969 188165 0 None 2 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
16755781 188199 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL443189 188199 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL505409 188199 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL505727 188199 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
16755781 188199 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL443189 188199 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505409 188199 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505727 188199 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562298 170885 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 667 10 2 8 5.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446324 170885 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 667 10 2 8 5.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562312 188060 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503331 188060 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562306 188342 0 None 8 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL508004 188342 0 None 8 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562296 188416 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 648 11 2 8 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL508772 188416 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 648 11 2 8 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562307 172137 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL450443 172137 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562303 172219 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 685 10 2 8 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL451342 172219 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 685 10 2 8 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL386682 210640 0 None 60 2 Guinea pig 10.0 pEC50 = 10 Functional
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN(C)C(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
155535107 171448 0 None 323 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1904 73 19 22 4.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471525 171448 0 None 323 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1904 73 19 22 4.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155537344 171752 0 None 46773 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4475304 171752 0 None 46773 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155532425 171182 0 None 3 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01558
CHEMBL4467338 171182 0 None 3 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01558
24769546 172120 0 None -2 2 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL450105 172120 0 None -2 2 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562301 188464 0 None -3 2 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL509464 188464 0 None -3 2 Mouse 10.0 pEC50 = 10.0 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155555346 173800 0 None 3 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4551834 173800 0 None 3 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155557064 174020 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1998 75 18 24 4.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4557012 174020 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1998 75 18 24 4.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44336539 5075 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
44578729 189039 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 531 4 0 7 5.1 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL514953 189039 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 531 4 0 7 5.1 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
53233689 61527 0 None -2 3 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773877 61527 0 None -2 3 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
46235271 73301 2 None 3 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 3 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
155516677 169522 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 72 18 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4443415 169522 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 72 18 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155544674 174364 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4565336 174364 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578728 178878 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 535 6 0 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL474067 178878 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 535 6 0 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
44562299 188282 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 646 9 3 7 5.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL507051 188282 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 646 9 3 7 5.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24769543 188119 0 None -2 2 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504406 188119 0 None -2 2 Mouse 9.9 pEC50 = 9.9 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
155536333 171606 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1865 71 17 24 1.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4473468 171606 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1865 71 17 24 1.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24861392 172349 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 574 5 1 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL451644 172349 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 574 5 1 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
44562314 188176 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505432 188176 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155564421 174696 0 None 12302 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1770 69 16 21 3.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4572516 174696 0 None 12302 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1770 69 16 21 3.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155524770 170371 0 None 12882 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1641 66 14 19 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4455361 170371 0 None 12882 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1641 66 14 19 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562309 171016 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 603 8 2 7 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446502 171016 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 603 8 2 7 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155526914 170636 0 None 2 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1837 72 19 24 0.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4459331 170636 0 None 2 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1837 72 19 24 0.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155559320 174292 0 None 1 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1872 72 18 23 3.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4563364 174292 0 None 1 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1872 72 18 23 3.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155533399 171279 0 None -2 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1838 72 19 24 1.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4468861 171279 0 None -2 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1838 72 19 24 1.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155535249 171437 0 None 2754 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1808 68 16 23 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471373 171437 0 None 2754 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1808 68 16 23 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155535579 171484 0 None 158 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471871 171484 0 None 158 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562310 172084 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL449681 172084 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155552556 173496 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1792 67 16 22 1.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4544208 173496 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1792 67 16 22 1.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
51353551 17950 10 None 1 3 Human 9.7 pEC50 = 9.7 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 17950 10 None 1 3 Human 9.7 pEC50 = 9.7 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
155542488 172563 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 69 16 22 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4520976 172563 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 69 16 22 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
54583298 61594 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774042 61594 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
44562308 172087 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL449725 172087 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155514270 169303 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL4440419 169303 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
155514432 169298 0 None 1096 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 2121 86 19 27 2.3 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4440303 169298 0 None 1096 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 2121 86 19 27 2.3 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155551968 173445 0 None 9772 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1793 69 16 20 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4542927 173445 0 None 9772 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1793 69 16 20 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
54583296 61585 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 533 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774033 61585 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 533 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
155540739 171940 0 None 3388 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1907 74 17 24 2.5 CCCC[C@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4483457 171940 0 None 3388 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1907 74 17 24 2.5 CCCC[C@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578686 178793 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473865 178793 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
44562305 188035 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL502924 188035 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155514270 169303 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4440419 169303 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578764 180230 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 535 4 0 7 5.0 O=C(c1cn(-c2ccc3c(c2)OCCO3)c(-c2ccc(F)cc2)n1)N1CCN(c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2008.06.057
CHEMBL475679 180230 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 535 4 0 7 5.0 O=C(c1cn(-c2ccc3c(c2)OCCO3)c(-c2ccc(F)cc2)n1)N1CCN(c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2008.06.057
46235271 73301 2 None 3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
155539345 172264 0 None 3235 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1850 72 16 23 3.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4514283 172264 0 None 3235 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1850 72 16 23 3.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155543163 172715 0 None 8709 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 16 25 2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4525615 172715 0 None 8709 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 16 25 2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24861060 188141 0 None -5 3 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446789 188141 0 None -5 3 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504861 188141 0 None -5 3 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
155517239 169590 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 2582 122 16 39 4.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4444353 169590 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 2582 122 16 39 4.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155547906 173104 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)C[C@H](NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4534977 173104 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)C[C@H](NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155546692 173070 0 None -3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1861 72 19 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4534236 173070 0 None -3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1861 72 19 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
46235271 73301 2 None 3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
155515427 169382 0 None 1819 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4441596 169382 0 None 1819 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155566319 175167 0 None 4677 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1850 71 16 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4583158 175167 0 None 4677 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1850 71 16 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155543995 172751 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1876 73 16 22 4.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4526455 172751 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1876 73 16 22 4.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155548381 173160 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1720 69 15 20 3.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)[C@@H](C)CC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4536393 173160 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1720 69 15 20 3.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)[C@@H](C)CC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24861174 174035 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL455742 174035 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
155562281 175268 0 None 4168 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4585323 175268 0 None 4168 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155555065 173762 0 None 4168 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4550876 173762 0 None 4168 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562313 171891 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL448118 171891 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
46235271 73301 2 None 3 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 3 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
44562306 188342 0 None -8 2 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL508004 188342 0 None -8 2 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155517761 169656 0 None 416 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4445529 169656 0 None 416 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155560670 174520 0 None 72 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4568746 174520 0 None 72 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155568312 175504 0 None 36 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 72 17 23 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4591101 175504 0 None 36 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 72 17 23 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
52949124 863 2 None 2 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None 2 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None 2 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None 2 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
44578727 189158 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515887 189158 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
46869398 61595 0 None -5 3 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774043 61595 0 None -5 3 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
54580295 61584 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774032 61584 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)cc1 10.1016/j.bmcl.2011.03.069
155532759 171189 0 None 27542 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1431 50 12 15 5.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4467402 171189 0 None 27542 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1431 50 12 15 5.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578767 172944 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL453083 172944 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL503822 172944 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44578767 172944 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL453083 172944 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503822 172944 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
54586148 61539 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 543 4 0 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773891 61539 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 543 4 0 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2011.03.069
44562311 188132 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504707 188132 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
51353551 17950 10 None 1 3 Human 9.1 pEC50 = 9.1 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responsesActivity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 17950 10 None 1 3 Human 9.1 pEC50 = 9.1 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responsesActivity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
168277247 190115 0 None -12 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5585 206 67 76 -9.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5182331 190115 0 None -12 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5585 206 67 76 -9.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
168281017 190320 0 None -10 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 4869 167 62 67 -13.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5185239 190320 0 None -10 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 4869 167 62 67 -13.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
155543846 172641 0 None -14 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1838 72 19 24 2.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4522865 172641 0 None -14 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1838 72 19 24 2.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24785705 181704 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL478398 181704 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
168280134 190147 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5585 206 67 76 -9.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5182775 190147 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5585 206 67 76 -9.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
16755782 178771 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473663 178771 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
44578424 182344 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479256 182344 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
155540394 172367 0 None 58 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 69 17 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4516794 172367 0 None 58 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 69 17 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
168273900 190104 0 None -7 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 4701 158 61 64 -14.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5182173 190104 0 None -7 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 4701 158 61 64 -14.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
168277239 190114 0 None -2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5417 197 66 73 -11.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5182323 190114 0 None -2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5417 197 66 73 -11.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL409529 211020 1 None 11 2 Guinea pig 8.9 pEC50 = 8.9 Functional
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
168276807 190042 0 None -9 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5417 197 66 73 -11.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5181266 190042 0 None -9 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5417 197 66 73 -11.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
54587150 61535 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773887 61535 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
16755781 188199 10 None -12 3 Mouse 8.9 pEC50 = 8.9 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL443189 188199 10 None -12 3 Mouse 8.9 pEC50 = 8.9 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505409 188199 10 None -12 3 Mouse 8.9 pEC50 = 8.9 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505727 188199 10 None -12 3 Mouse 8.9 pEC50 = 8.9 Functional
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
52949124 863 2 None 2 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None 2 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None 2 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None 2 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL414592 211397 0 None 8 2 Guinea pig 8.9 pEC50 = 8.9 Functional
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)N(C)C(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
52949124 863 2 None 2 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None 2 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None 2 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None 2 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10700916 173864 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4553223 173864 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155550911 173356 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1884 70 16 23 3.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4540877 173356 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1884 70 16 23 3.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
54583260 61544 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773896 61544 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.03.069
52949124 863 2 None 2 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None 2 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None 2 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None 2 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
24785703 178772 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 534 6 0 5 6.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473664 178772 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 534 6 0 5 6.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
54586175 61589 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 504 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccoc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774037 61589 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 504 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccoc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
44578611 189066 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2cccc(F)c2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515160 189066 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2cccc(F)c2)c1 10.1016/j.bmcl.2008.06.057
44578456 189005 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5cnccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL514716 189005 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5cnccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
155531277 171065 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1821 72 18 23 2.1 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4465747 171065 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1821 72 18 23 2.1 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155553502 173603 0 None -26 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 72 19 22 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OP(=O)(O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4547294 173603 0 None -26 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 72 19 22 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OP(=O)(O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155564367 174584 0 None -457 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 72 18 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4570130 174584 0 None -457 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 72 18 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
70691750 73299 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017833 73299 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
52949124 863 2 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
9055 863 2 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
CHEMBL1269258 863 2 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
DB12694 863 2 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
10507109 108740 0 None -51 4 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
CHEMBL321761 108740 0 None -51 4 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
70683295 73249 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 606 7 1 5 6.2 O=C(CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21)N1CCC(Cc2ccccc2)C1 10.1016/j.bmcl.2012.02.049
CHEMBL2017692 73249 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 606 7 1 5 6.2 O=C(CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21)N1CCC(Cc2ccccc2)C1 10.1016/j.bmcl.2012.02.049
44578531 171994 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 570 6 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OCC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL448597 171994 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 570 6 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OCC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
11571172 140054 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
Intrinsic agonistic activity at CCK receptor in SD rat at 1 uM expressed in pancreatic acinar cell lineIntrinsic agonistic activity at CCK receptor in SD rat at 1 uM expressed in pancreatic acinar cell line
ChEMBL 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm049072h
CHEMBL381347 140054 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
Intrinsic agonistic activity at CCK receptor in SD rat at 1 uM expressed in pancreatic acinar cell lineIntrinsic agonistic activity at CCK receptor in SD rat at 1 uM expressed in pancreatic acinar cell line
ChEMBL 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm049072h
52944224 17951 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 586 8 2 7 5.6 CC(C)N(C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269259 17951 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 586 8 2 7 5.6 CC(C)N(C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
70685411 73290 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 606 6 1 5 6.8 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017824 73290 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 606 6 1 5 6.8 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
54580296 61587 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774035 61587 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
24785432 180979 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 7 0 5 6.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(CC)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476725 180979 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 7 0 5 6.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(CC)cc2)c1 10.1016/j.bmcl.2008.06.057
52945789 18100 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 541 7 0 5 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1270487 18100 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 541 7 0 5 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
54586149 61542 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(C)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773894 61542 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(C)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL217236 207627 0 None 4 2 Guinea pig 8.7 pEC50 = 8.7 Functional
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
46235272 73298 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 589 8 1 7 4.9 COCCC1CCCCN1C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017832 73298 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 589 8 1 7 4.9 COCCC1CCCCN1C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
24785178 180957 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476530 180957 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
24785177 189189 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1ccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL516113 189189 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1ccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL266839 208959 0 None 7 2 Guinea pig 7.7 pEC50 = 7.7 Functional
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
54580266 61536 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 529 6 0 6 6.0 CCOc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773888 61536 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 529 6 0 6 6.0 CCOc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
70689619 73291 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 592 6 1 5 6.5 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017825 73291 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 592 6 1 5 6.5 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
155557285 173946 0 None -295 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1779 74 19 22 1.6 CCCC[C@H](NC(=O)[C@H](CNC(=O)CCCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4555341 173946 0 None -295 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1779 74 19 22 1.6 CCCC[C@H](NC(=O)[C@H](CNC(=O)CCCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155553269 173555 0 None 53 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1818 68 15 22 3.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N1CCC[C@@H]1C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4545970 173555 0 None 53 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1818 68 15 22 3.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N1CCC[C@@H]1C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578305 180588 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 5 0 5 6.1 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc(Cl)c(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476095 180588 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 5 0 5 6.1 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc(Cl)c(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
46235271 73301 2 None 3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL2017835 73301 2 None 3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL208479 207455 0 None -30 5 Human 5.6 pEC50 = 5.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
CHEMBL208479 207455 0 None -30 5 Human 5.6 pEC50 = 5.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
46234969 73294 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 626 7 1 5 7.4 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1CC1CCCCC1 10.1016/j.bmcl.2012.02.049
CHEMBL2017828 73294 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 626 7 1 5 7.4 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1CC1CCCCC1 10.1016/j.bmcl.2012.02.049
54587151 61537 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 545 6 0 7 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1OC 10.1016/j.bmcl.2011.03.069
CHEMBL1773889 61537 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 545 6 0 7 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1OC 10.1016/j.bmcl.2011.03.069
101823779 1369 29 None -354 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
16162108 1369 29 None -354 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
8408 1369 29 None -354 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
CHEMBL4451154 1369 29 None -354 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
54586174 61586 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 514 5 0 5 6.2 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774034 61586 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 514 5 0 5 6.2 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL375360 210471 4 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Activity at human CCK1 receptor expressed in HEK293 cells assessed as level of [3H]inositol produced relative to controlActivity at human CCK1 receptor expressed in HEK293 cells assessed as level of [3H]inositol produced relative to control
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm061268p
4627 809 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
864 809 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
9833444 809 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
CHEMBL1121 809 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
DB09142 809 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
4627 809 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
864 809 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
9833444 809 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
CHEMBL1121 809 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
DB09142 809 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
51353551 17950 10 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269257 17950 10 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
54580265 61532 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccccc1-c1cnc(C(=O)N2CCN(c3cnc4ccccc4c3)CC2)nc1-c1ccc(C)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773884 61532 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccccc1-c1cnc(C(=O)N2CCN(c3cnc4ccccc4c3)CC2)nc1-c1ccc(C)cc1 10.1016/j.bmcl.2011.03.069
52942901 17953 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269261 17953 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL382051 210546 0 None -331 5 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
CHEMBL217609 207634 0 None 6 2 Guinea pig 8.5 pEC50 = 8.5 Functional
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
46235271 73301 2 None 3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
155542545 172549 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1770 70 16 21 3.9 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4520699 172549 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1770 70 16 21 3.9 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL382051 210546 0 None -331 5 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
44578772 182214 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-c2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nn2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479063 182214 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-c2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nn2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
70681224 73295 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
CHEMBL2017829 73295 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
52949124 863 2 None 2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
9055 863 2 None 2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
CHEMBL1269258 863 2 None 2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
DB12694 863 2 None 2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
44578530 188101 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 556 5 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL504024 188101 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 556 5 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
54581261 61534 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 529 6 0 6 6.0 CCOc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773886 61534 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 529 6 0 6 6.0 CCOc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
54582288 61541 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2C)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773893 61541 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2C)cc1 10.1016/j.bmcl.2011.03.069
54580263 61528 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773878 61528 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.03.069
70695934 73297 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 595 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017831 73297 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 595 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
9960432 39187 6 None -3 3 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
CHEMBL147186 39187 6 None -3 3 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
10698109 106812 0 None -2 3 Guinea pig 6.4 pEC50 = 6.4 Functional
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
CHEMBL317181 106812 0 None -2 3 Guinea pig 6.4 pEC50 = 6.4 Functional
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
44578647 178748 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2c(F)cccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473457 178748 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2c(F)cccc2F)c1 10.1016/j.bmcl.2008.06.057
70695922 73248 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 558 6 1 5 5.9 CCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017691 73248 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 558 6 1 5 5.9 CCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
54581301 61590 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 503 5 1 5 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5cc[nH]c5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774038 61590 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 503 5 1 5 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5cc[nH]c5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
52949124 863 2 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
54586147 61533 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773885 61533 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
70693814 73296 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccncc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017830 73296 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccncc1 10.1016/j.bmcl.2012.02.049
52946666 17952 0 None 2 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269260 17952 0 None 2 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
44578422 180980 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5n4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476739 180980 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5n4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
52949124 863 2 None -2 3 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
9055 863 2 None -2 3 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
CHEMBL1269258 863 2 None -2 3 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
DB12694 863 2 None -2 3 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
44578562 180952 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc3c2OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL476519 180952 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc3c2OCCO3)cc1 10.1016/j.bmcl.2008.06.057
52940616 17955 0 None 1 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269263 17955 0 None 1 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
46234820 73292 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 572 6 1 5 6.1 CC(C)C1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017826 73292 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 572 6 1 5 6.1 CC(C)C1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
46235271 73301 2 None 3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human CCK1R W6.48A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R W6.48A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human CCK1R W6.48A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R W6.48A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
24785180 180958 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 536 6 0 5 6.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476531 180958 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 536 6 0 5 6.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2008.06.057
54582313 61591 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc2ccccc2cc1N1CCN(C(=O)c2ncc(-c3ccc(OC)cc3)c(-c3ccc(C)cc3)n2)CC1 10.1016/j.bmcl.2011.03.069
CHEMBL1774039 61591 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc2ccccc2cc1N1CCN(C(=O)c2ncc(-c3ccc(OC)cc3)c(-c3ccc(C)cc3)n2)CC1 10.1016/j.bmcl.2011.03.069
70689603 73247 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 588 8 1 6 5.5 COCCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017690 73247 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 588 8 1 6 5.5 COCCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
52940616 17955 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269263 17955 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
24785430 181702 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 6 0 5 6.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(C)C)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL478397 181702 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 6 0 5 6.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(C)C)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL269185 209035 0 None 5 2 Guinea pig 7.3 pEC50 = 7.3 Functional
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)NCC(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
44578398 181202 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc5ccccc45)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL477784 181202 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc5ccccc45)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
70695933 73289 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 607 7 1 6 5.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
CHEMBL2017823 73289 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 607 7 1 6 5.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
54583297 61592 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774040 61592 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
54582287 61540 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 501 5 0 6 5.3 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773892 61540 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 501 5 0 6 5.3 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.03.069
24785431 189218 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL516355 189218 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
24784941 189126 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 516 6 0 5 6.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515616 189126 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 516 6 0 5 6.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL2370248 208069 0 None -1 2 Guinea pig 7.2 pEC50 = 7.2 Functional
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
155540415 172370 0 None -1584 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1862 71 17 23 3.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4516868 172370 0 None -1584 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1862 71 17 23 3.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
54580267 61543 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 535 5 0 6 6.0 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2Cl)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773895 61543 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 535 5 0 6 6.0 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2Cl)cc1 10.1016/j.bmcl.2011.03.069
52943046 17954 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 557 8 0 6 5.8 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Oc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269262 17954 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 557 8 0 6 5.8 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Oc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
51353551 17950 10 None -18 3 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269257 17950 10 None -18 3 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
52946666 17952 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269260 17952 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
24785176 180981 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 500 5 0 4 6.5 CCc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476747 180981 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 500 5 0 4 6.5 CCc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
70683305 73300 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 635 7 1 6 6.4 Cc1cccc(CC2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL2017834 73300 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 635 7 1 6 6.4 Cc1cccc(CC2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
46235271 73301 2 None 3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
24785179 180954 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 6 0 5 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476520 180954 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 6 0 5 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2)c1 10.1016/j.bmcl.2008.06.057
54584255 61588 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774036 61588 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
44578251 181850 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL478604 181850 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44578423 189067 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515161 189067 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
155533520 171262 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 910 26 8 9 2.5 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4468598 171262 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 910 26 8 9 2.5 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24784942 180761 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 488 4 1 5 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(O)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL476297 180761 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 488 4 1 5 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(O)c2)cc1 10.1016/j.bmcl.2008.06.057
46234970 73293 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 620 7 1 5 6.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017827 73293 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 620 7 1 5 6.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
136000594 61538 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 517 4 2 7 5.0 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc(O)c(O)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773890 61538 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 517 4 2 7 5.0 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc(O)c(O)c2)cc1 10.1016/j.bmcl.2011.03.069
44578399 181372 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 492 5 1 6 4.7 COc1cccc(-n2cc(C(=O)N3CCN(c4nc5ccccc5[nH]4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL477996 181372 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 492 5 1 6 4.7 COc1cccc(-n2cc(C(=O)N3CCN(c4nc5ccccc5[nH]4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
10509945 88954 0 None 63 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL2369816 88954 0 None 63 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578455 181873 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL478630 181873 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
24784940 182205 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479046 182205 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
54581302 61593 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc(N2CCN(C(=O)c3ncc(-c4ccc(OC)cc4)c(-c4ccc(C)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2011.03.069
CHEMBL1774041 61593 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc(N2CCN(C(=O)c3ncc(-c4ccc(OC)cc4)c(-c4ccc(C)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2011.03.069
44336539 5075 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responsesActivity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responsesActivity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
52942901 17953 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269261 17953 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
155517868 169644 0 None -457 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1893 76 19 24 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4445353 169644 0 None -457 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1893 76 19 24 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578529 182192 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 7 0 5 6.8 CCCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479030 182192 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 7 0 5 6.8 CCCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
443375 205872 40 None 2 6 Human 10.1 pIC50 = 10.1 Functional
Antagonistic activity against cholecystokinin type A receptorAntagonistic activity against cholecystokinin type A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00067a001
CHEMBL9506 205872 40 None 2 6 Human 10.1 pIC50 = 10.1 Functional
Antagonistic activity against cholecystokinin type A receptorAntagonistic activity against cholecystokinin type A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00067a001
44398261 123867 0 None -91 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 6.0 pIC50 = 6.0 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 6.0 pIC50 = 6.0 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 123867 0 None -91 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
3035433 99009 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against cholecystokinin type A receptorAntagonistic activity against cholecystokinin type A receptor
ChEMBL 535 4 3 7 3.1 CC(C)C[C@@H]1N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/jm00067a001
CHEMBL283117 99009 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against cholecystokinin type A receptorAntagonistic activity against cholecystokinin type A receptor
ChEMBL 535 4 3 7 3.1 CC(C)C[C@@H]1N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/jm00067a001
44398261 123867 0 None -91 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 123867 0 None -91 2 Human 5.7 pIC50 = 5.7 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 5.7 pIC50 = 5.7 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10507071 113111 0 None -524 4 Human 4.7 pIC50 = 4.7 Functional
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL332261 113111 0 None -524 4 Human 4.7 pIC50 = 4.7 Functional
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None -7 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 5.6 pIC50 = 5.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 5.6 pIC50 = 5.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 123867 0 None -91 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL375360 210471 4 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Activity at human CCK1 receptor expressed in HEK293 cells assessed as level of [3H]inositol produced relative to controlActivity at human CCK1 receptor expressed in HEK293 cells assessed as level of [3H]inositol produced relative to control
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm061268p
44398261 123867 0 None -91 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
52949124 863 2 None 2 3 Human 8.5 pIC50 = 8.5 Functional
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None 2 3 Human 8.5 pIC50 = 8.5 Functional
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None 2 3 Human 8.5 pIC50 = 8.5 Functional
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None 2 3 Human 8.5 pIC50 = 8.5 Functional
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10008654 127094 0 None -7 2 Human 8.4 pIC50 = 8.4 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 8.4 pIC50 = 8.4 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 123867 0 None -91 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 5.3 pIC50 = 5.3 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 5.3 pIC50 = 5.3 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None -7 2 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 123867 0 None -91 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 123867 0 None -91 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None -7 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 123867 0 None -91 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67192 0 None -100 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None -100 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None -7 2 Human 6.1 pIC50 = 6.1 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 6.1 pIC50 = 6.1 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 123867 0 None -91 2 Human 6.1 pIC50 = 6.1 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None -91 2 Human 6.1 pIC50 = 6.1 Functional
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None -7 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None -7 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44306887 101591 0 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL302027 101591 0 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
44306360 157333 0 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2C)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL408395 157333 0 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2C)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
44458112 98254 0 None - 1 Guinea pig 8.2 pKd = 8.2 Functional
Compound was tested for competitive blocking of guinea pig ileal smooth muscle strip contraction to cholecystokinin-8 (CCK-8) receptorCompound was tested for competitive blocking of guinea pig ileal smooth muscle strip contraction to cholecystokinin-8 (CCK-8) receptor
ChEMBL 374 4 2 3 2.7 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL277661 98254 0 None - 1 Guinea pig 8.2 pKd = 8.2 Functional
Compound was tested for competitive blocking of guinea pig ileal smooth muscle strip contraction to cholecystokinin-8 (CCK-8) receptorCompound was tested for competitive blocking of guinea pig ileal smooth muscle strip contraction to cholecystokinin-8 (CCK-8) receptor
ChEMBL 374 4 2 3 2.7 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
44306888 101860 0 None - 2 Guinea pig 7.2 pKd = 7.2 Functional
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL303635 101860 0 None - 2 Guinea pig 7.2 pKd = 7.2 Functional
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
44306868 101613 0 None - 2 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 836 18 9 7 3.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL302150 101613 0 None - 2 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 836 18 9 7 3.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
2360 3245 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
5042 3245 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
871 3245 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
CHEMBL1697771 3245 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
DB11656 3245 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
1614 2317 60 None -1 2 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
60182 2317 60 None -1 2 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
892 2317 60 None -1 2 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
CHEMBL206025 2317 60 None -1 2 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
65937 1376 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
834 1376 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
889 1376 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
CHEMBL550781 1376 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
DB04856 1376 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
4329839 806 0 None -158 2 Rat 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
861 806 0 None -158 2 Rat 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
16168172 1742 0 None -158 2 Rat 6.1 pIC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
3559 1742 0 None -158 2 Rat 6.1 pIC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
444007 2994 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
870 2994 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB00183 2994 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
3960 2313 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 1975695
3960 2313 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 2437574
891 2313 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 1975695
891 2313 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 2437574
CHEMBL24938 2313 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 1975695
CHEMBL24938 2313 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 2437574
52949124 863 2 None 2 3 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 20851601
9055 863 2 None 2 3 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 20851601
CHEMBL1269258 863 2 None 2 3 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 20851601
DB12694 863 2 None 2 3 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 20851601
5311148 1865 5 None 41 2 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 9276016
865 1865 5 None 41 2 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 9276016
CHEMBL293226 1865 5 None 41 2 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 9276016
3888 2091 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7654246
5311196 2091 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7654246
122077 2291 45 None -8 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
890 2291 45 None -8 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
CHEMBL249973 2291 45 None -8 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
DB04867 2291 45 None -8 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
121964 205 28 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
858 205 28 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
CHEMBL323521 205 28 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
904 2977 7 None 3 3 Rat 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 8605955
9915756 2977 7 None 3 3 Rat 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 8605955
CHEMBL2111204 2977 7 None 3 3 Rat 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 8605955
CHEMBL356898 2977 7 None 3 3 Rat 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 8605955
862 807 0 None -1 2 Mouse 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12370550
127948 3662 0 None 79432 2 Rat 9.6 pIC50 = 9.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 502 7 2 4 4.5 COc1ccc2c(c1)N(c1ccccc1F)C(=O)[C@@]2(CCC(=O)O)NC(=O)C1CCc2c(C1)cccc2 8813597
884 3662 0 None 79432 2 Rat 9.6 pIC50 = 9.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 502 7 2 4 4.5 COc1ccc2c(c1)N(c1ccccc1F)C(=O)[C@@]2(CCC(=O)O)NC(=O)C1CCc2c(C1)cccc2 8813597
3476 1373 8 None 870 2 Rat 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
59751 1373 8 None 870 2 Rat 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
878 1373 8 None 870 2 Rat 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
CHEMBL39263 1373 8 None 870 2 Rat 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
4627 809 44 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
864 809 44 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
9833444 809 44 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
CHEMBL1121 809 44 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB09142 809 44 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
2281 3126 76 None -2454 2 Rat 2.2 pIC50 None 2.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
4922 3126 76 None -2454 2 Rat 2.2 pIC50 None 2.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
893 3126 76 None -2454 2 Rat 2.2 pIC50 None 2.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
CHEMBL316561 3126 76 None -2454 2 Rat 2.2 pIC50 None 2.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
DB13431 3126 76 None -2454 2 Rat 2.2 pIC50 None 2.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
2360 3245 0 None - 1 Rat 4.4 pIC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
5042 3245 0 None - 1 Rat 4.4 pIC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
871 3245 0 None - 1 Rat 4.4 pIC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
CHEMBL1697771 3245 0 None - 1 Rat 4.4 pIC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
DB11656 3245 0 None - 1 Rat 4.4 pIC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
108187 913 30 None -794 5 Rat 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 1975695
873 913 30 None -794 5 Rat 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 1975695
CHEMBL2062154 913 30 None -794 5 Rat 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 1975695
CHEMBL287735 913 30 None -794 5 Rat 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 1975695
122119 2974 0 None -1000 2 Rat 5.9 pIC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 618 12 5 6 5.1 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](CC1CNc2c1cccc2)(NC(=O)OC1C[C@H]2C([C@]1(C)CC2)(C)C)C)CCC(=O)O 1975695
882 2974 0 None -1000 2 Rat 5.9 pIC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 618 12 5 6 5.1 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](CC1CNc2c1cccc2)(NC(=O)OC1C[C@H]2C([C@]1(C)CC2)(C)C)C)CCC(=O)O 1975695
880 2208 3 None -7413 2 Rat 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 3 7 3.5 O=C(N[C@@H]1N=C(C2CCCCC2)c2c(N(C1=O)C)cccc2)Nc1cccc(c1)N(c1n[nH]nn1)C 8632408
9935175 2208 3 None -7413 2 Rat 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 3 7 3.5 O=C(N[C@@H]1N=C(C2CCCCC2)c2c(N(C1=O)C)cccc2)Nc1cccc(c1)N(c1n[nH]nn1)C 8632408
CHEMBL2093059 2208 3 None -7413 2 Rat 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 3 7 3.5 O=C(N[C@@H]1N=C(C2CCCCC2)c2c(N(C1=O)C)cccc2)Nc1cccc(c1)N(c1n[nH]nn1)C 8632408
1614 2317 60 None -1 2 Rat 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 3663268
60182 2317 60 None -1 2 Rat 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 3663268
892 2317 60 None -1 2 Rat 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 3663268
CHEMBL206025 2317 60 None -1 2 Rat 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 3663268
104929 2189 8 None -12 3 Rat 6.6 pIC50 None 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
3477 2189 8 None -12 3 Rat 6.6 pIC50 None 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
879 2189 8 None -12 3 Rat 6.6 pIC50 None 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
CHEMBL289498 2189 8 None -12 3 Rat 6.6 pIC50 None 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
10742947 3936 0 None - 1 Rat 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 8 6 4 3.7 OC(=O)CC(c1ccccc1)NC(=O)c1cccc(c1)NC(=O)c1cc2c([nH]1)ccc(c2)C(=N)N 12538004
886 3936 0 None - 1 Rat 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 8 6 4 3.7 OC(=O)CC(c1ccccc1)NC(=O)c1cccc(c1)NC(=O)c1cc2c([nH]1)ccc(c2)C(=N)N 12538004
CHEMBL137814 3936 0 None - 1 Rat 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 8 6 4 3.7 OC(=O)CC(c1ccccc1)NC(=O)c1cccc(c1)NC(=O)c1cc2c([nH]1)ccc(c2)C(=N)N 12538004
887 4047 24 None -2511 3 Rat 6.9 pIC50 None 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 9022799
9870520 4047 24 None -2511 3 Rat 6.9 pIC50 None 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 9022799
CHEMBL324547 4047 24 None -2511 3 Rat 6.9 pIC50 None 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 9022799
DB12355 4047 24 None -2511 3 Rat 6.9 pIC50 None 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 9022799
4627 809 44 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
864 809 44 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
9833444 809 44 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
CHEMBL1121 809 44 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB09142 809 44 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
10348659 1774 0 None 3 2 Human 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 604 8 2 5 5.4 O=C(NC1C(=O)N(c2ccccc2)c2c(N(C1=O)CC(=O)N(c1ccc(cc1)N(C)C)C(C)C)cccc2)Nc1ccccc1 8558528
866 1774 0 None 3 2 Human 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 604 8 2 5 5.4 O=C(NC1C(=O)N(c2ccccc2)c2c(N(C1=O)CC(=O)N(c1ccc(cc1)N(C)C)C(C)C)cccc2)Nc1ccccc1 8558528
CHEMBL1184355 1774 0 None 3 2 Human 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 604 8 2 5 5.4 O=C(NC1C(=O)N(c2ccccc2)c2c(N(C1=O)CC(=O)N(c1ccc(cc1)N(C)C)C(C)C)cccc2)Nc1ccccc1 8558528
19023535 3484 0 None - 1 Rat 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 363 4 3 3 2.0 OC(=O)C1CN(C(=O)C1NC(=O)c1c[nH]c2c1cccc2)c1ccccc1 None
883 3484 0 None - 1 Rat 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 363 4 3 3 2.0 OC(=O)C1CN(C(=O)C1NC(=O)c1c[nH]c2c1cccc2)c1ccccc1 None
11757476 2033 1 None - 1 Rat 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 15331911
876 2033 1 None - 1 Rat 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 15331911
CHEMBL2112828 2033 1 None - 1 Rat 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 15331911
868 3610 0 None - 1 Human 9.3 pIC50 None 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 609 10 2 7 7.9 COc1cc(Cl)c(cc1c1nc(sc1CCC1CCCCC1)NC(=O)c1cc2c(n1CC(=O)O)c(C)cc(c2)C)OC 10215648
9852833 3610 0 None - 1 Human 9.3 pIC50 None 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 609 10 2 7 7.9 COc1cc(Cl)c(cc1c1nc(sc1CCC1CCCCC1)NC(=O)c1cc2c(n1CC(=O)O)c(C)cc(c2)C)OC 10215648
CHEMBL3302616 3610 0 None - 1 Human 9.3 pIC50 None 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 609 10 2 7 7.9 COc1cc(Cl)c(cc1c1nc(sc1CCC1CCCCC1)NC(=O)c1cc2c(n1CC(=O)O)c(C)cc(c2)C)OC 10215648
132916 3112 11 None 602 2 Rat 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 7509389
874 3112 11 None 602 2 Rat 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 7509389
CHEMBL300072 3112 11 None 602 2 Rat 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 7509389
122077 2291 45 None 8 2 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406
890 2291 45 None 8 2 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406
CHEMBL249973 2291 45 None 8 2 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406
DB04867 2291 45 None 8 2 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
4627 809 44 None -2 5 Human 10.0 pEC50 = 10 Binding
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00017a022
864 809 44 None -2 5 Human 10.0 pEC50 = 10 Binding
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00017a022
9833444 809 44 None -2 5 Human 10.0 pEC50 = 10 Binding
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00017a022
CHEMBL1121 809 44 None -2 5 Human 10.0 pEC50 = 10 Binding
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00017a022
DB09142 809 44 None -2 5 Human 10.0 pEC50 = 10 Binding
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00017a022
10032955 167472 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
CHEMBL432256 167472 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
CHEMBL319438 209471 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00017a022
24769604 188104 0 None - 0 Human 11.0 pIC50 = 11 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504114 188104 0 None - 0 Human 11.0 pIC50 = 11 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
44562301 188464 0 None - 0 Human 10.8 pIC50 = 10.8 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL509464 188464 0 None - 0 Human 10.8 pIC50 = 10.8 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24769546 172120 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL450105 172120 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24861391 188165 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
CHEMBL505225 188165 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
CHEMBL505969 188165 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
24861394 188468 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 592 5 1 7 5.6 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL509519 188468 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 592 5 1 7 5.6 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2008.06.057
53233689 61527 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773877 61527 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
44562306 188342 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL508004 188342 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24861060 188141 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446789 188141 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504861 188141 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
155543995 172751 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1876 73 16 22 4.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4526455 172751 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1876 73 16 22 4.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562302 187608 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 666 11 2 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL498958 187608 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 666 11 2 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
155562281 175268 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4585323 175268 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
10819755 164890 0 None - 2 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL423907 164890 0 None - 2 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL411079 211115 0 None - 0 Rat 10.3 pIC50 = 10.3 Binding
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N1CSC(C)(C)[C@@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
121964 205 28 None 831 2 Rat 10.3 pIC50 = 10.3 Binding
Inhibitory activity against cholecystokinin type A receptor from rat pancreas binding assayInhibitory activity against cholecystokinin type A receptor from rat pancreas binding assay
ChEMBL None None None None 10.1021/jm00100a033
858 205 28 None 831 2 Rat 10.3 pIC50 = 10.3 Binding
Inhibitory activity against cholecystokinin type A receptor from rat pancreas binding assayInhibitory activity against cholecystokinin type A receptor from rat pancreas binding assay
ChEMBL None None None None 10.1021/jm00100a033
CHEMBL323521 205 28 None 831 2 Rat 10.3 pIC50 = 10.3 Binding
Inhibitory activity against cholecystokinin type A receptor from rat pancreas binding assayInhibitory activity against cholecystokinin type A receptor from rat pancreas binding assay
ChEMBL None None None None 10.1021/jm00100a033
155543163 172715 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 16 25 2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4525615 172715 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 16 25 2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24769605 178142 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL468372 178142 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155514270 169303 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4440419 169303 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24769543 188119 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504406 188119 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
24861060 188141 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL446789 188141 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL504861 188141 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
155539345 172264 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1850 72 16 23 3.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4514283 172264 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1850 72 16 23 3.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155514432 169298 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 2121 86 19 27 2.3 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4440303 169298 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 2121 86 19 27 2.3 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155540739 171940 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1907 74 17 24 2.5 CCCC[C@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4483457 171940 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1907 74 17 24 2.5 CCCC[C@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562303 172219 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 685 10 2 8 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL451342 172219 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 685 10 2 8 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
24861114 188550 3 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 582 7 1 6 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL510690 188550 3 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 582 7 1 6 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
155515427 169382 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4441596 169382 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155566319 175167 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1850 71 16 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4583158 175167 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1850 71 16 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155559320 174292 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1872 72 18 23 3.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4563364 174292 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1872 72 18 23 3.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
443375 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL9506 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
155547906 173104 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)C[C@H](NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4534977 173104 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)C[C@H](NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155560670 174520 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4568746 174520 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
443375 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL9506 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80683-6
443375 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Concentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissueConcentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm020424z
CHEMBL9506 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Concentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissueConcentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm020424z
443375 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
CHEMBL9506 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
443375 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm000937a
CHEMBL9506 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm000937a
443375 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL9506 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
443375 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00609-9
CHEMBL9506 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00609-9
443375 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00164a020
CHEMBL9506 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00164a020
443375 205872 40 None -2 5 Human 10.1 pIC50 = 10.1 Binding
Inhibition of cholecystokinin A receptorInhibition of cholecystokinin A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/np9800102
CHEMBL9506 205872 40 None -2 5 Human 10.1 pIC50 = 10.1 Binding
Inhibition of cholecystokinin A receptorInhibition of cholecystokinin A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/np9800102
24861113 187607 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL498942 187607 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL506201 187607 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
44562297 188038 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 631 9 2 7 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL502974 188038 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 631 9 2 7 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562299 188282 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 646 9 3 7 5.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL507051 188282 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 646 9 3 7 5.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
443375 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
CHEMBL9506 205872 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
155536333 171606 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1865 71 17 24 1.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4473468 171606 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1865 71 17 24 1.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155555346 173800 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4551834 173800 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155535579 171484 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471871 171484 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44398261 123867 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10460766 114957 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010898i
CHEMBL3350858 114957 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010898i
44562304 188288 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 664 9 3 7 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(=O)NC)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL507094 188288 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 664 9 3 7 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(=O)NC)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
155555065 173762 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4550876 173762 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL269098 209033 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Compound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasCompound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(01)81250-6
4627 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL None None None None 10.1021/jm00092a007
864 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL None None None None 10.1021/jm00092a007
9833444 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL None None None None 10.1021/jm00092a007
CHEMBL1121 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL None None None None 10.1021/jm00092a007
DB09142 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL None None None None 10.1021/jm00092a007
4627 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00105a062
864 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00105a062
9833444 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00105a062
CHEMBL1121 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00105a062
DB09142 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00105a062
443375 205872 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00105a062
CHEMBL9506 205872 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00105a062
4627 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1016/S0960-894X(00)80687-3
864 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1016/S0960-894X(00)80687-3
9833444 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1016/S0960-894X(00)80687-3
CHEMBL1121 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1016/S0960-894X(00)80687-3
DB09142 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1016/S0960-894X(00)80687-3
443375 205872 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80687-3
CHEMBL9506 205872 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80687-3
4627 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL None None None None 10.1021/jm00057a005
864 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL None None None None 10.1021/jm00057a005
9833444 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL None None None None 10.1021/jm00057a005
CHEMBL1121 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL None None None None 10.1021/jm00057a005
DB09142 809 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL None None None None 10.1021/jm00057a005
443375 205872 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00057a005
CHEMBL9506 205872 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00057a005
155532759 171189 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1431 50 12 15 5.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4467402 171189 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1431 50 12 15 5.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155517239 169590 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 2582 122 16 39 4.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4444353 169590 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 2582 122 16 39 4.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562300 188052 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503107 188052 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
4627 809 44 None -2 5 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
864 809 44 None -2 5 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
9833444 809 44 None -2 5 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
CHEMBL1121 809 44 None -2 5 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
DB09142 809 44 None -2 5 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
155517761 169656 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4445529 169656 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
72548703 161019 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor after 60 mins by scintillation counting analysisDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161019 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor after 60 mins by scintillation counting analysisDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
44562298 170885 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 667 10 2 8 5.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446324 170885 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 667 10 2 8 5.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44578764 180230 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 535 4 0 7 5.0 O=C(c1cn(-c2ccc3c(c2)OCCO3)c(-c2ccc(F)cc2)n1)N1CCN(c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2008.06.057
CHEMBL475679 180230 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 535 4 0 7 5.0 O=C(c1cn(-c2ccc3c(c2)OCCO3)c(-c2ccc(F)cc2)n1)N1CCN(c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2008.06.057
16755781 188199 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
16755781 188199 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL443189 188199 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL443189 188199 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505409 188199 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL505409 188199 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505727 188199 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL505727 188199 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
4627 809 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cellsDisplacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
864 809 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cellsDisplacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
9833444 809 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cellsDisplacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
CHEMBL1121 809 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cellsDisplacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
DB09142 809 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cellsDisplacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
4627 809 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
864 809 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
9833444 809 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
CHEMBL1121 809 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
DB09142 809 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
44578457 171904 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL448221 171904 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
24861392 172349 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 574 5 1 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL451644 172349 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 574 5 1 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
44562296 188416 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 648 11 2 8 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL508772 188416 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 648 11 2 8 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155552556 173496 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1792 67 16 22 1.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4544208 173496 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1792 67 16 22 1.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
54586148 61539 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 543 4 0 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773891 61539 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 543 4 0 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2011.03.069
155542488 172563 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1820 69 16 22 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4520976 172563 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1820 69 16 22 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL413654 211331 0 None - 2 Rat 9.7 pIC50 = 9.7 Binding
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](C)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H](N)CCC(=O)O)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00378a012
13822923 193148 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 450 3 2 5 4.5 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=NC2NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00396a028
CHEMBL53907 193148 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 450 3 2 5 4.5 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=NC2NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00396a028
44578729 189039 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 531 4 0 7 5.1 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL514953 189039 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 531 4 0 7 5.1 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
44562310 172084 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL449681 172084 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
46869398 61595 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774043 61595 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
44578728 178878 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 535 6 0 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL474067 178878 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 535 6 0 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
44562305 188035 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL502924 188035 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562314 188176 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505432 188176 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155516677 169522 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 72 18 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4443415 169522 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 72 18 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155524181 170286 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1820 71 18 22 2.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4453982 170286 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1820 71 18 22 2.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
14888734 167283 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1012 29 10 13 0.8 CSCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL430906 167283 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1012 29 10 13 0.8 CSCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44562307 172137 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL450443 172137 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
54583296 61585 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 533 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774033 61585 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 533 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
10477146 78104 1 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2111920 78104 1 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
155568312 175504 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 72 17 23 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4591101 175504 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 72 17 23 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155544674 174364 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4565336 174364 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
4627 809 44 None -1 5 Guinea pig 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(00)80680-0
864 809 44 None -1 5 Guinea pig 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(00)80680-0
9833444 809 44 None -1 5 Guinea pig 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(00)80680-0
CHEMBL1121 809 44 None -1 5 Guinea pig 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(00)80680-0
DB09142 809 44 None -1 5 Guinea pig 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(00)80680-0
14208286 67342 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 395 4 1 3 3.7 CN1C(=O)[C@@H](NC(=O)/C=C/c2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907661 67342 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 395 4 1 3 3.7 CN1C(=O)[C@@H](NC(=O)/C=C/c2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
155537344 171752 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4475304 171752 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155535107 171448 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1904 73 19 22 4.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471525 171448 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1904 73 19 22 4.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
4627 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
864 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
9833444 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
CHEMBL1121 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
DB09142 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
4627 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm00017a022
864 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm00017a022
9833444 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm00017a022
CHEMBL1121 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm00017a022
DB09142 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm00017a022
14208241 67409 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
CHEMBL1907852 67409 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
44562312 188060 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503331 188060 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
14208244 58560 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
CHEMBL168852 58560 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
4627 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00001a027
864 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00001a027
9833444 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00001a027
CHEMBL1121 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00001a027
DB09142 809 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00001a027
4627 809 44 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None None 10.1021/jm00173a006
864 809 44 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None None 10.1021/jm00173a006
9833444 809 44 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None None 10.1021/jm00173a006
CHEMBL1121 809 44 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None None 10.1021/jm00173a006
DB09142 809 44 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None None 10.1021/jm00173a006
24785705 181704 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL478398 181704 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
44562308 172087 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL449725 172087 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44578767 172944 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44578767 172944 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL453083 172944 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL453083 172944 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503822 172944 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL503822 172944 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
6957640 158814 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
CHEMBL410035 158814 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
44396718 67062 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 530 7 2 5 4.6 C[C@@H]1C(=O)N(Cc2ccccc2)C(=O)N2CCC[C@H](N[C@@H](Cc3c[nH]c4ccccc34)C(=O)OC(C)(C)C)C12 10.1021/jm0498755
CHEMBL188808 67062 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 530 7 2 5 4.6 C[C@@H]1C(=O)N(Cc2ccccc2)C(=O)N2CCC[C@H](N[C@@H](Cc3c[nH]c4ccccc34)C(=O)OC(C)(C)C)C12 10.1021/jm0498755
44562311 188132 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504707 188132 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155557064 174020 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1998 75 18 24 4.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4557012 174020 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1998 75 18 24 4.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
443375 205872 40 None -2 5 Human 9.3 pIC50 = 9.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm701575k
CHEMBL9506 205872 40 None -2 5 Human 9.3 pIC50 = 9.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm701575k
4627 809 44 None -1 5 Rat 9.3 pIC50 = 9.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL None None None None 10.1021/jm00079a003
864 809 44 None -1 5 Rat 9.3 pIC50 = 9.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL None None None None 10.1021/jm00079a003
9833444 809 44 None -1 5 Rat 9.3 pIC50 = 9.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL None None None None 10.1021/jm00079a003
CHEMBL1121 809 44 None -1 5 Rat 9.3 pIC50 = 9.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL None None None None 10.1021/jm00079a003
DB09142 809 44 None -1 5 Rat 9.3 pIC50 = 9.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL None None None None 10.1021/jm00079a003
6918156 96839 2 None - 0 Human 9.3 pIC50 = 9.3 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL269016 96839 2 None - 0 Human 9.3 pIC50 = 9.3 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
6918156 96839 2 None - 0 Guinea pig 9.3 pIC50 = 9.3 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL269016 96839 2 None - 0 Guinea pig 9.3 pIC50 = 9.3 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
155530671 170996 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1627 65 14 19 4.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4464703 170996 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1627 65 14 19 4.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155524770 170371 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1641 66 14 19 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4455361 170371 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1641 66 14 19 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562309 171016 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 603 8 2 7 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446502 171016 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 603 8 2 7 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24785703 178772 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 534 6 0 5 6.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473664 178772 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 534 6 0 5 6.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
122077 2291 45 None - 1 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.093
890 2291 45 None - 1 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.093
CHEMBL249973 2291 45 None - 1 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.093
DB04867 2291 45 None - 1 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.093
44578727 189158 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515887 189158 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
10008654 127094 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127094 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL366344 127094 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL438773 212049 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
10482714 78022 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 551 6 3 5 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(C3CCCCC3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL2111545 78022 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 551 6 3 5 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(C3CCCCC3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL2370122 208042 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL None None None CSCC[C@@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44578686 178793 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473865 178793 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL267849 208989 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
14208225 67412 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 3 3.9 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL1907855 67412 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 3 3.9 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
155535249 171437 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1808 68 16 23 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471373 171437 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1808 68 16 23 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
4627 809 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm9601664
864 809 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm9601664
9833444 809 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm9601664
CHEMBL1121 809 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm9601664
DB09142 809 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm9601664
4627 809 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm950626d
864 809 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm950626d
9833444 809 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm950626d
CHEMBL1121 809 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm950626d
DB09142 809 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm950626d
15667014 106774 0 None - 0 Guinea pig 9.2 pIC50 = 9.2 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 28 10 11 1.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL316944 106774 0 None - 0 Guinea pig 9.2 pIC50 = 9.2 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 28 10 11 1.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
132916 3112 11 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 10.1016/S0960-894X(96)00609-9
874 3112 11 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 10.1016/S0960-894X(96)00609-9
CHEMBL300072 3112 11 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 10.1016/S0960-894X(96)00609-9
443375 205872 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/0960-894X(96)00160-6
CHEMBL9506 205872 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/0960-894X(96)00160-6
443375 205872 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm991078x
CHEMBL9506 205872 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm991078x
443375 205872 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm000959x
CHEMBL9506 205872 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm000959x
44562313 171891 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL448118 171891 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
14208303 202985 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL73946 202985 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208303 202985 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL73946 202985 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
15666988 106775 0 None - 0 Guinea pig 9.1 pIC50 = 9.1 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL316949 106775 0 None - 0 Guinea pig 9.1 pIC50 = 9.1 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
15666988 106775 0 None - 0 Guinea pig 9.1 pIC50 = 9.1 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL316949 106775 0 None - 0 Guinea pig 9.1 pIC50 = 9.1 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
3476 1373 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00047a021
59751 1373 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00047a021
878 1373 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00047a021
CHEMBL39263 1373 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00047a021
14208294 202534 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 465 3 1 3 4.2 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL70984 202534 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 465 3 1 3 4.2 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
14208296 202923 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(I)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL73483 202923 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(I)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
155532425 171182 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01558
CHEMBL4467338 171182 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01558
CHEMBL1172428 206844 0 None - 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
4627 809 44 None -1 5 Rat 9.1 pIC50 = 9.1 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00548-4
864 809 44 None -1 5 Rat 9.1 pIC50 = 9.1 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00548-4
9833444 809 44 None -1 5 Rat 9.1 pIC50 = 9.1 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00548-4
CHEMBL1121 809 44 None -1 5 Rat 9.1 pIC50 = 9.1 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00548-4
DB09142 809 44 None -1 5 Rat 9.1 pIC50 = 9.1 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00548-4
3476 1373 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00120a002
59751 1373 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00120a002
878 1373 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00120a002
CHEMBL39263 1373 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00120a002
14208297 67404 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(I)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907848 67404 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(I)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208295 67407 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 3 1 3 4.2 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907850 67407 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 3 1 3 4.2 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
46235271 73301 2 None 2 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
14208268 202779 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 4 3.5 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL72428 202779 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 4 3.5 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
13822922 188492 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 436 3 2 5 4.2 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)c1cc2ccccc2[nH]1 10.1021/jm00396a028
CHEMBL50986 188492 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 436 3 2 5 4.2 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)c1cc2ccccc2[nH]1 10.1021/jm00396a028
11757476 2033 1 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 10.1021/jm991078x
876 2033 1 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 10.1021/jm991078x
CHEMBL2112828 2033 1 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 10.1021/jm991078x
CHEMBL384035 210569 1 None -8 4 Guinea pig 9.0 pIC50 = 9.0 Binding
In vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL428666 210569 1 None -8 4 Guinea pig 9.0 pIC50 = 9.0 Binding
In vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
155526914 170636 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1837 72 19 24 0.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4459331 170636 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1837 72 19 24 0.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
11017163 79135 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccccc1N1C(=O)C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
CHEMBL2114081 79135 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccccc1N1C(=O)C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
15667011 96209 0 None - 0 Human 9.0 pIC50 = 9 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL263742 96209 0 None - 0 Human 9.0 pIC50 = 9 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
15667011 96209 0 None - 0 Guinea pig 9.0 pIC50 = 9 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL263742 96209 0 None - 0 Guinea pig 9.0 pIC50 = 9 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
196641 202693 7 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 447 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL71950 202693 7 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 447 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
4627 809 44 None -1 5 Rat 9.0 pIC50 = 9 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00198-0
864 809 44 None -1 5 Rat 9.0 pIC50 = 9 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00198-0
9833444 809 44 None -1 5 Rat 9.0 pIC50 = 9 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00198-0
CHEMBL1121 809 44 None -1 5 Rat 9.0 pIC50 = 9 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00198-0
DB09142 809 44 None -1 5 Rat 9.0 pIC50 = 9 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00198-0
44469677 15004 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]CCK-8 from human recombinant CCKA receptor expressed in CHO cellsDisplacement of [125I]CCK-8 from human recombinant CCKA receptor expressed in CHO cells
ChEMBL 336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2010.06.050
CHEMBL1210154 15004 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]CCK-8 from human recombinant CCKA receptor expressed in CHO cellsDisplacement of [125I]CCK-8 from human recombinant CCKA receptor expressed in CHO cells
ChEMBL 336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2010.06.050
196641 202693 7 None - 0 Rat 9.0 pIC50 = 9 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 447 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL71950 202693 7 None - 0 Rat 9.0 pIC50 = 9 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 447 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
16755782 178771 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473663 178771 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
44329487 108027 0 None - 0 Guinea pig 9.0 pIC50 = 9 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3cccc(F)c3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL319986 108027 0 None - 0 Guinea pig 9.0 pIC50 = 9 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3cccc(F)c3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
155564421 174696 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1770 69 16 21 3.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4572516 174696 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1770 69 16 21 3.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
4627 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None None 10.1021/jm991078x
864 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None None 10.1021/jm991078x
9833444 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None None 10.1021/jm991078x
CHEMBL1121 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None None 10.1021/jm991078x
DB09142 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None None 10.1021/jm991078x
4627 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL None None None None 10.1021/jm0498755
864 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL None None None None 10.1021/jm0498755
9833444 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL None None None None 10.1021/jm0498755
CHEMBL1121 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL None None None None 10.1021/jm0498755
DB09142 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL None None None None 10.1021/jm0498755
4627 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm010898i
864 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm010898i
9833444 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm010898i
CHEMBL1121 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm010898i
DB09142 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm010898i
444998 207574 26 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm010813d
CHEMBL216166 207574 26 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm010813d
4627 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)
ChEMBL None None None None 10.1016/S0960-894X(97)00107-8
864 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)
ChEMBL None None None None 10.1016/S0960-894X(97)00107-8
9833444 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)
ChEMBL None None None None 10.1016/S0960-894X(97)00107-8
CHEMBL1121 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)
ChEMBL None None None None 10.1016/S0960-894X(97)00107-8
DB09142 809 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)
ChEMBL None None None None 10.1016/S0960-894X(97)00107-8
10033396 108102 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 824 20 8 7 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL320405 108102 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 824 20 8 7 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44329323 106859 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 574 7 3 3 6.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)Nc3ccccc3C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL317615 106859 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 574 7 3 3 6.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)Nc3ccccc3C)C2=O)c1 10.1016/S0960-894X(01)80832-5
44329331 107579 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(C)c3)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c3ccccc3)C2)cc1 10.1016/S0960-894X(01)80832-5
CHEMBL319504 107579 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(C)c3)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c3ccccc3)C2)cc1 10.1016/S0960-894X(01)80832-5
44329363 108217 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 594 7 3 3 7.2 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)Nc3ccccc3Cl)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL320821 108217 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 594 7 3 3 7.2 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)Nc3ccccc3Cl)C2=O)c1 10.1016/S0960-894X(01)80832-5
11027990 67192 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL189634 67192 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm010813d
44269000 32697 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 671 14 6 5 6.3 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/s0960-894x(00)00198-0
CHEMBL14153 32697 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 671 14 6 5 6.3 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/s0960-894x(00)00198-0
44269000 32697 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 671 14 6 5 6.3 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/s0960-894x(01)00630-8
CHEMBL14153 32697 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 671 14 6 5 6.3 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/s0960-894x(01)00630-8
155533399 171279 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1838 72 19 24 1.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4468861 171279 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1838 72 19 24 1.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
4627 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(97)00062-0
864 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(97)00062-0
9833444 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(97)00062-0
CHEMBL1121 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(97)00062-0
DB09142 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(97)00062-0
14208311 202958 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 437 3 1 3 4.3 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL73699 202958 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 437 3 1 3 4.3 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
14208227 101794 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 440 3 1 4 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL303227 101794 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 440 3 1 4 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208312 77469 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 437 3 1 3 4.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL2092865 77469 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 437 3 1 3 4.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
10373344 166081 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 844 21 8 7 3.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL428103 166081 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 844 21 8 7 3.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
10341724 78106 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL2111922 78106 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
24861174 174035 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL455742 174035 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44578424 182344 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479256 182344 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44329286 106721 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3cccc(C)c3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL316619 106721 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3cccc(C)c3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
4627 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL None None None None 10.1021/jm960249k
864 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL None None None None 10.1021/jm960249k
9833444 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL None None None None 10.1021/jm960249k
CHEMBL1121 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL None None None None 10.1021/jm960249k
DB09142 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL None None None None 10.1021/jm960249k
4627 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL None None None None 10.1021/jm960205b
864 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL None None None None 10.1021/jm960205b
9833444 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL None None None None 10.1021/jm960205b
CHEMBL1121 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL None None None None 10.1021/jm960205b
DB09142 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL None None None None 10.1021/jm960205b
4627 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL None None None None 10.1021/jm970265x
864 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL None None None None 10.1021/jm970265x
9833444 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL None None None None 10.1021/jm970265x
CHEMBL1121 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL None None None None 10.1021/jm970265x
DB09142 809 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL None None None None 10.1021/jm970265x
11082524 114954 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 591 7 3 5 5.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=S)N(Cc3ccccc3)C(=S)C[C@@H]12 10.1021/jm010898i
CHEMBL3350853 114954 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 591 7 3 5 5.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=S)N(Cc3ccccc3)C(=S)C[C@@H]12 10.1021/jm010898i
14208227 101794 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 440 3 1 4 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL303227 101794 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 440 3 1 4 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL411202 211126 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
54580295 61584 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774032 61584 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)cc1 10.1016/j.bmcl.2011.03.069
14208232 202438 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 452 5 3 4 3.2 O=C(O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL70456 202438 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 452 5 3 4 3.2 O=C(O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14208231 202544 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL71079 202544 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
10093957 202928 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 3 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL73522 202928 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 3 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10350551 107969 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 838 21 8 7 3.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL319913 107969 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 838 21 8 7 3.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
14208231 202544 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL71079 202544 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
14208231 202544 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL71079 202544 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
10093957 202928 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 3 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL73522 202928 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 3 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
46235271 73301 2 None 2 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
14208228 102633 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 470 5 3 4 3.3 O=C(O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL307661 102633 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 470 5 3 4 3.3 O=C(O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1172429 206845 0 None 26 4 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
5311188 9712 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
CHEMBL113718 9712 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
5311188 9712 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL113718 9712 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
44396619 165692 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 516 7 2 5 4.4 CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
CHEMBL426792 165692 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 516 7 2 5 4.4 CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
5311188 9712 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010898i
CHEMBL113718 9712 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010898i
5311188 9712 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL113718 9712 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL107694 206748 0 None - 0 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44329330 106703 0 None - 0 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3cccc(C)c3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL316504 106703 0 None - 0 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3cccc(C)c3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
10076650 26027 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm050689o
CHEMBL13577 26027 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm050689o
10010723 4844 0 None - 0 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 836 20 8 7 3.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(F)(F)F)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL104598 4844 0 None - 0 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 836 20 8 7 3.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(F)(F)F)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
108187 913 30 None 4 5 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00086a017
873 913 30 None 4 5 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00086a017
CHEMBL2062154 913 30 None 4 5 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00086a017
CHEMBL287735 913 30 None 4 5 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00086a017
10076650 26027 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1016/s0960-894x(01)00630-8
CHEMBL13577 26027 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1016/s0960-894x(01)00630-8
10076650 26027 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm000959x
CHEMBL13577 26027 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm000959x
44329352 110949 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(F)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
CHEMBL327496 110949 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(F)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
44578647 178748 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2c(F)cccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473457 178748 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2c(F)cccc2F)c1 10.1016/j.bmcl.2008.06.057
24785178 180957 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476530 180957 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
44578423 189067 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515161 189067 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
24785431 189218 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL516355 189218 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
52949124 863 2 None -2 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
44365788 121179 0 None - 0 Human 8.0 pIC50 = 8 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 643 7 1 7 5.5 COC(=O)n1c(C(=O)NC2C(=O)N(CC(=O)N(c3ccccc3)C(C)C)c3ccccc3N(c3ccccc3)C2=O)cc2ccccc21 10.1021/jm9601664
CHEMBL358778 121179 0 None - 0 Human 8.0 pIC50 = 8 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 643 7 1 7 5.5 COC(=O)n1c(C(=O)NC2C(=O)N(CC(=O)N(c3ccccc3)C(C)C)c3ccccc3N(c3ccccc3)C2=O)cc2ccccc21 10.1021/jm9601664
46235271 73301 2 None 2 2 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL1172252 206842 0 None -12 4 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
10046672 115582 1 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 402 3 2 3 3.8 CN1C(=O)C(NC(=O)Nc2cccc(F)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL335666 115582 1 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 402 3 2 3 3.8 CN1C(=O)C(NC(=O)Nc2cccc(F)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10364786 104392 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)NC2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL311061 104392 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)NC2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
44329383 107805 0 None - 0 Guinea pig 8.0 pIC50 = 8 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 526 6 3 3 5.5 Cc1cccc(NC(=O)N[C@H]2C[C@H](c3ccccc3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL319749 107805 0 None - 0 Guinea pig 8.0 pIC50 = 8 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 526 6 3 3 5.5 Cc1cccc(NC(=O)N[C@H]2C[C@H](c3ccccc3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
44336539 5075 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10364786 104392 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)NC2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL311061 104392 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)NC2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
10627173 204816 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 586 8 1 4 6.5 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL88602 204816 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 586 8 1 4 6.5 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
44346576 10669 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 399 4 2 3 3.8 O=C(/C=C\c1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL117158 10669 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 399 4 2 3 3.8 O=C(/C=C\c1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00047a021
14208272 67397 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 3 1 3 4.4 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL1907841 67397 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 3 1 3 4.4 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
10627173 204816 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 586 8 1 4 6.5 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
CHEMBL88602 204816 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 586 8 1 4 6.5 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
14208230 102734 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 446 3 3 3 4.5 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm00047a021
CHEMBL308414 102734 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 446 3 3 3 4.5 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm00047a021
14208274 168726 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 443 3 1 3 4.7 CN1C(=O)C(NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL441445 168726 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 443 3 1 3 4.7 CN1C(=O)C(NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
15689736 106118 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC/N=C(\S)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142702 106118 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC/N=C(\S)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
11801335 119030 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 579 7 2 4 5.5 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(F)cc1 10.1021/jm950626d
CHEMBL345786 119030 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 579 7 2 4 5.5 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(F)cc1 10.1021/jm950626d
44306868 101613 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 836 18 9 7 3.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL302150 101613 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 836 18 9 7 3.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
44306888 101860 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL303635 101860 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
13953709 161788 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 409 4 1 6 4.0 O=C(NC1N=C(c2ccccc2)c2ccccc2-n2cnnc21)OCc1ccccc1 10.1021/jm00396a028
CHEMBL416483 161788 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 409 4 1 6 4.0 O=C(NC1N=C(c2ccccc2)c2ccccc2-n2cnnc21)OCc1ccccc1 10.1021/jm00396a028
14208274 168726 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 3 1 3 4.7 CN1C(=O)C(NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL441445 168726 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 3 1 3 4.7 CN1C(=O)C(NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
9988264 109235 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 888 22 9 8 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL322955 109235 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 888 22 9 8 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
10886229 78183 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1cccc(N2C(=O)C[C@@H]3[C@@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)c1 10.1021/jm010813d
CHEMBL2112234 78183 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1cccc(N2C(=O)C[C@@H]3[C@@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)c1 10.1021/jm010813d
44382057 119829 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 420 4 2 3 3.1 Cc1cccc(NC(=O)N[C@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL352939 119829 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 420 4 2 3 3.1 Cc1cccc(NC(=O)N[C@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
44301015 197383 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 609 7 5 7 3.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)Nc3nn[nH]n3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL58658 197383 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 609 7 5 7 3.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)Nc3nn[nH]n3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
10001488 164374 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 4 3 3 3.6 O=C(Cc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL422411 164374 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 4 3 3 3.6 O=C(Cc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL2112688 207504 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Binding affinity towards Cholecystokinin type A receptor was determined in guinea pig pancreatic membranes using [125I]-BH-CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor was determined in guinea pig pancreatic membranes using [125I]-BH-CCK-8 as radioligand
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)[C@H](C)c1c[nH]c2ccccc12 10.1021/jm960078j
52949124 863 2 None -2 2 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
46235271 73301 2 None 2 2 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
46235271 73301 2 None 2 2 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
10649606 49349 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
10001488 164374 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 4 3 3 3.6 O=C(Cc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL422411 164374 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 4 3 3 3.6 O=C(Cc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
14208202 202936 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 4 2 4 4.5 O=C(Cc1cccc2sccc12)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL73563 202936 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 4 2 4 4.5 O=C(Cc1cccc2sccc12)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
44362701 120621 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL357576 120621 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
44370446 119096 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 467 15 2 4 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCC)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL346361 119096 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 467 15 2 4 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCC)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
20152922 118470 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 440 5 2 3 4.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00163a069
CHEMBL342415 118470 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 440 5 2 3 4.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00163a069
10414170 170051 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
CHEMBL445095 170051 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
15200522 119962 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 422 4 2 3 3.7 CN1C(=O)C(NC(=O)Cc2c[nH]c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL354126 119962 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 422 4 2 3 3.7 CN1C(=O)C(NC(=O)Cc2c[nH]c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL37983 210519 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity towards Cholecystokinin type A receptor by displacement of [125I]BH-CCK-8 from rat pancreatic aciniBinding affinity towards Cholecystokinin type A receptor by displacement of [125I]BH-CCK-8 from rat pancreatic acini
ChEMBL None None None CS[C@H]1CCN(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(C)=O)[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00001a019
656755 67368 28 None - 0 Guinea pig 5.0 pIC50 = 5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 397 3 1 2 4.7 CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907717 67368 28 None - 0 Guinea pig 5.0 pIC50 = 5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 397 3 1 2 4.7 CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
15167824 67377 0 None - 0 Guinea pig 5.0 pIC50 = 5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 379 3 1 2 4.6 CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
CHEMBL1907731 67377 0 None - 0 Guinea pig 5.0 pIC50 = 5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 379 3 1 2 4.6 CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
20190196 31572 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 388 4 1 4 3.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1cccnc1 10.1021/jm00163a069
CHEMBL140620 31572 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 388 4 1 4 3.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1cccnc1 10.1021/jm00163a069
15167799 118682 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 379 4 2 4 3.9 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)c1ccsc1 10.1021/jm00163a069
CHEMBL343158 118682 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 379 4 2 4 3.9 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)c1ccsc1 10.1021/jm00163a069
44381820 120112 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 689 18 7 8 2.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](C#N)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
CHEMBL354631 120112 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 689 18 7 8 2.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](C#N)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
44381821 120113 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 689 18 7 8 2.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@H](C#N)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
CHEMBL354632 120113 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 689 18 7 8 2.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@H](C#N)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
44348835 16642 0 None - 0 Rat 5.0 pIC50 = 5 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 938 25 11 11 0.2 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL124719 16642 0 None - 0 Rat 5.0 pIC50 = 5 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 938 25 11 11 0.2 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
14208262 202814 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 431 4 2 3 4.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(-c2ccccc2)cc1 10.1021/jm00047a021
CHEMBL72670 202814 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 431 4 2 3 4.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(-c2ccccc2)cc1 10.1021/jm00047a021
7216755 59228 7 None - 0 Rat 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 265 1 1 3 1.8 CN1C(=O)[C@@H](N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL171651 59228 7 None - 0 Rat 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 265 1 1 3 1.8 CN1C(=O)[C@@H](N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
44311988 102557 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 5 2 4 2.5 CN1C(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL307034 102557 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 5 2 4 2.5 CN1C(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14208206 162917 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 4 3 4 2.8 O=C1Nc2ccccc2C(c2ccccc2F)=NC1NC(=O)C(O)c1ccccc1 10.1021/jm00120a002
CHEMBL419997 162917 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 4 3 4 2.8 O=C1Nc2ccccc2C(c2ccccc2F)=NC1NC(=O)C(O)c1ccccc1 10.1021/jm00120a002
14208262 202814 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 431 4 2 3 4.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(-c2ccccc2)cc1 10.1021/jm00120a002
CHEMBL72670 202814 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 431 4 2 3 4.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(-c2ccccc2)cc1 10.1021/jm00120a002
2794055 67366 3 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 360 3 1 2 4.7 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1Cc1ccccc1 10.1021/jm00390a019
CHEMBL1907712 67366 3 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 360 3 1 2 4.7 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1Cc1ccccc1 10.1021/jm00390a019
15167780 67371 0 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 415 3 2 3 4.6 O=C1Nc2ccccc2C1C[C@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=O 10.1021/jm00390a019
CHEMBL1907723 67371 0 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 415 3 2 3 4.6 O=C1Nc2ccccc2C1C[C@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=O 10.1021/jm00390a019
15614736 166754 0 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 410 3 1 2 5.9 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=NC1Cc1cccc2ccccc12 10.1021/jm00390a019
CHEMBL429391 166754 0 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 410 3 1 2 5.9 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=NC1Cc1cccc2ccccc12 10.1021/jm00390a019
44359880 32113 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 428 7 2 5 2.4 CC(=O)NCSCC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
CHEMBL141048 32113 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 428 7 2 5 2.4 CC(=O)NCSCC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
44359841 116129 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 498 7 1 4 6.5 CCN(CC)c1ccc(NCC2CN=C(c3ccccc3F)c3ccccc3N2C)cc1C(F)(F)F 10.1021/jm00163a069
CHEMBL336881 116129 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 498 7 1 4 6.5 CCN(CC)c1ccc(NCC2CN=C(c3ccccc3F)c3ccccc3N2C)cc1C(F)(F)F 10.1021/jm00163a069
7216755 59228 7 None - 0 Rat 4.0 pIC50 = 4 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 265 1 1 3 1.8 CN1C(=O)[C@@H](N)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL171651 59228 7 None - 0 Rat 4.0 pIC50 = 4 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 265 1 1 3 1.8 CN1C(=O)[C@@H](N)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
71450869 83964 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 650 12 5 6 4.3 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCS(=O)(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL2112338 83964 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 650 12 5 6 4.3 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCS(=O)(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL2219559 83964 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 650 12 5 6 4.3 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCS(=O)(=O)O)c1ccccc1 10.1021/jm00092a007
10325770 130173 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 573 8 4 5 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)[C@@](Cc3ccccc3)(C(N)=O)C[C@H]12 10.1016/0960-894X(96)00160-6
CHEMBL368380 130173 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 573 8 4 5 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)[C@@](Cc3ccccc3)(C(N)=O)C[C@H]12 10.1016/0960-894X(96)00160-6
44349203 116553 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCCC2)C1 10.1021/jm00079a003
CHEMBL339134 116553 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCCC2)C1 10.1021/jm00079a003
45482109 196373 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)N[C@@H](Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL574062 196373 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)N[C@@H](Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
44408411 160763 0 None -2089 4 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1242 31 11 15 4.4 CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL412331 160763 0 None -2089 4 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1242 31 11 15 4.4 CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
44408484 136983 0 None -19498 4 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1033 30 13 12 1.4 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL375412 136983 0 None -19498 4 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1033 30 13 12 1.4 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm050851n
44418924 156340 0 None -19952 4 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL407198 156340 0 None -19952 4 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL333299 209645 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Compound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pigCompound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pig
ChEMBL None None None C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a068
10340882 25824 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3cccnc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL135498 25824 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3cccnc3N(C)C2=O)c1 10.1021/jm00078a018
46235271 73301 2 None 2 2 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
10256428 119183 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 529 9 4 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL347278 119183 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 529 9 4 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
108187 913 30 None - 5 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00017a022
873 913 30 None - 5 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00017a022
CHEMBL2062154 913 30 None - 5 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00017a022
CHEMBL287735 913 30 None - 5 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00017a022
CHEMBL205965 207425 0 None - 3 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
44369590 119044 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 458 7 3 6 3.5 Cc1cccc(NCNC2N=C(c3cc[nH]n3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL345880 119044 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 458 7 3 6 3.5 Cc1cccc(NCNC2N=C(c3cc[nH]n3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
51353551 17950 10 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 17950 10 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
44353183 116276 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 743-1710Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 743-1710
ChEMBL 555 8 3 4 5.2 O=C(OC1C2CC3CC(C2)CC1C3)N1CCCC1(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1 10.1016/S0960-894X(00)80156-0
CHEMBL337692 116276 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 743-1710Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 743-1710
ChEMBL 555 8 3 4 5.2 O=C(OC1C2CC3CC(C2)CC1C3)N1CCCC1(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1 10.1016/S0960-894X(00)80156-0
71456173 78075 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CC[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL2111826 78075 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CC[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
10342469 196923 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)N[C@H](Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL578650 196923 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)N[C@H](Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
44283496 99711 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 527 9 2 3 6.1 CC(=O)N(CCc1ccccc1)CC(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL288037 99711 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 527 9 2 3 6.1 CC(=O)N(CCc1ccccc1)CC(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10668688 205799 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 400 4 4 6 3.4 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N)c2)c1 10.1021/jm970373j
CHEMBL9465 205799 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 400 4 4 6 3.4 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N)c2)c1 10.1021/jm970373j
53465782 69066 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 455 9 4 3 4.6 O=C(Nc1ccccc1C(=O)NC(CCCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933101 69066 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 455 9 4 3 4.6 O=C(Nc1ccccc1C(=O)NC(CCCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10793168 167330 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 570 7 1 3 6.9 CC(C)N(C(=O)CN1C(=O)C(C)(Cc2c[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
CHEMBL431212 167330 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 570 7 1 3 6.9 CC(C)N(C(=O)CN1C(=O)C(C)(Cc2c[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
9960964 85566 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 1000 to 1100The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 1000 to 1100
ChEMBL 638 12 5 7 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCc1nnn[nH]1)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304152 85566 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 1000 to 1100The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 1000 to 1100
ChEMBL 638 12 5 7 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCc1nnn[nH]1)c1ccccc1 10.1016/S0960-894X(00)80652-6
10325426 107115 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1016/S0960-894X(01)80769-1
CHEMBL318963 107115 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1016/S0960-894X(01)80769-1
10165354 21946 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 770-2020Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 770-2020
ChEMBL 529 9 4 4 4.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(CO)Cc1ccccc1 10.1016/S0960-894X(00)80156-0
CHEMBL132233 21946 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 770-2020Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 770-2020
ChEMBL 529 9 4 4 4.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(CO)Cc1ccccc1 10.1016/S0960-894X(00)80156-0
44283132 120288 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 485 9 3 3 5.9 CC(CNCCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL35555 120288 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 485 9 3 3 5.9 CC(CNCCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10624013 33319 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 464 6 3 4 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCC1 10.1021/jm970065l
CHEMBL142063 33319 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 464 6 3 4 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCC1 10.1021/jm970065l
14208240 101875 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 418 4 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc([N+](=O)[O-])cc1 10.1021/jm00047a021
CHEMBL303724 101875 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 418 4 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc([N+](=O)[O-])cc1 10.1021/jm00047a021
14208213 202902 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 362 3 3 3 2.7 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc[nH]1 10.1021/jm00047a021
CHEMBL73272 202902 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 362 3 3 3 2.7 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc[nH]1 10.1021/jm00047a021
9896825 102504 0 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 742 14 6 10 2.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL30656 102504 0 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 742 14 6 10 2.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
14208314 102450 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 495 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccccc2I)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL306166 102450 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 495 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccccc2I)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
14208199 102598 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1c[nH]c2ccccc12 10.1021/jm00047a021
CHEMBL307370 102598 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1c[nH]c2ccccc12 10.1021/jm00047a021
CHEMBL218327 207649 0 None -2630 4 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
14208272 67397 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 3 1 3 4.4 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907841 67397 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 3 1 3 4.4 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208208 168912 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 399 4 2 3 3.8 O=C(/C=C/c1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL443009 168912 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 399 4 2 3 3.8 O=C(/C=C/c1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
10260206 166913 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 918 21 8 8 4.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL429932 166913 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 918 21 8 8 4.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL415706 211451 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44341426 109850 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 514 13 3 4 6.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccc(O)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL324022 109850 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 514 13 3 4 6.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccc(O)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
9934162 27523 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 464 5 3 4 4.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(Cc3c[nH]cn3)C2=O)c1 10.1021/jm00078a018
CHEMBL137043 27523 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 464 5 3 4 4.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(Cc3c[nH]cn3)C2=O)c1 10.1021/jm00078a018
10649606 49349 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
10432393 99882 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 422 3 3 3 4.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00121a004
CHEMBL289533 99882 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 422 3 3 3 4.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00121a004
14208242 155882 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
CHEMBL40668 155882 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
14208240 101875 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 418 4 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc([N+](=O)[O-])cc1 10.1021/jm00120a002
CHEMBL303724 101875 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 418 4 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc([N+](=O)[O-])cc1 10.1021/jm00120a002
14208242 155882 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL40668 155882 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208213 202902 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 362 3 3 3 2.7 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc[nH]1 10.1021/jm00120a002
CHEMBL73272 202902 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 362 3 3 3 2.7 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc[nH]1 10.1021/jm00120a002
5279169 25994 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 404 3 3 3 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00078a018
CHEMBL135715 25994 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 404 3 3 3 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00078a018
10070678 120242 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL355092 120242 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14208242 155882 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00078a018
CHEMBL40668 155882 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00078a018
90663976 106316 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccccc1O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144538 106316 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccccc1O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14991577 162693 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 870 20 9 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2cc(Cl)ccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL418500 162693 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 870 20 9 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2cc(Cl)ccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44381960 119773 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 474 3 3 4 4.6 CN1C(=O)[C@@H](NC(=O)Nc2cc3c4ccccc4nc-3c[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL352573 119773 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 474 3 3 4 4.6 CN1C(=O)[C@@H](NC(=O)Nc2cc3c4ccccc4nc-3c[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
44301037 100390 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 633 8 4 6 4.0 CCS(=O)(=O)NC(=O)c1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccc(C)cc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00327-P
CHEMBL293490 100390 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 633 8 4 6 4.0 CCS(=O)(=O)NC(=O)c1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccc(C)cc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00327-P
10319892 58782 2 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
CHEMBL169661 58782 2 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
14208199 102598 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1c[nH]c2ccccc12 10.1021/jm00120a002
CHEMBL307370 102598 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1c[nH]c2ccccc12 10.1021/jm00120a002
10182876 202422 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 457 7 1 3 5.1 CCCCCc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
CHEMBL70361 202422 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 457 7 1 3 5.1 CCCCCc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
14208280 67346 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 335 3 1 3 2.6 CC(C)C(=O)N[C@H]1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00120a002
CHEMBL1907665 67346 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 335 3 1 3 2.6 CC(C)C(=O)N[C@H]1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00120a002
14208315 67395 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 495 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2I)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907839 67395 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 495 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2I)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14802528 117961 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 642 14 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CNC(=O)CCCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL341281 117961 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 642 14 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CNC(=O)CCCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
15104622 9938 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 476 13 3 2 6.4 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1cccc(C)c1 10.1021/jm00116a002
CHEMBL115093 9938 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 476 13 3 2 6.4 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1cccc(C)c1 10.1021/jm00116a002
14720389 164531 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL422701 164531 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
10075297 115007 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 518 6 3 5 4.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)Nc3ccncc3)C2=O)c1 10.1021/jm00078a018
CHEMBL335239 115007 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 518 6 3 5 4.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)Nc3ccncc3)C2=O)c1 10.1021/jm00078a018
14991564 106320 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 827 21 9 9 2.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144541 106320 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 827 21 9 9 2.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44334338 108426 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 547 9 2 5 4.2 Cc1cccc(NC(=O)N[C@H](CS(=O)(=O)Cc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL321107 108426 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 547 9 2 5 4.2 Cc1cccc(NC(=O)N[C@H](CS(=O)(=O)Cc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
10319892 58782 2 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL169661 58782 2 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
14519983 119471 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ncccc2c1 10.1021/jm00124a003
CHEMBL349857 119471 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ncccc2c1 10.1021/jm00124a003
14519979 9439 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cccc2ccccc12 10.1021/jm00124a003
CHEMBL112215 9439 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cccc2ccccc12 10.1021/jm00124a003
44349070 163939 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 421 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL421438 163939 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 421 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL103485 206715 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
14208251 77474 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL2092870 77474 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
15167804 67369 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 455 6 2 3 4.6 O=C(O)CCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907719 67369 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 455 6 2 3 4.6 O=C(O)CCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
45482485 196334 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 486 8 3 6 3.8 Cn1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)cc2cc([N+](=O)[O-])ccc21 10.1016/j.bmc.2009.05.067
CHEMBL573793 196334 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 486 8 3 6 3.8 Cn1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)cc2cc([N+](=O)[O-])ccc21 10.1016/j.bmc.2009.05.067
21842317 121166 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL358646 121166 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
21842317 121166 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas at dose of 0.03 umol/kgCompound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas at dose of 0.03 umol/kg
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL358646 121166 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas at dose of 0.03 umol/kgCompound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas at dose of 0.03 umol/kg
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00556-9
10322988 10053 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL115772 10053 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
44349434 116514 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 396 11 3 3 3.6 CCC(C)(CC)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL338929 116514 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 396 11 3 3 3.6 CCC(C)(CC)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
5311201 205663 30 None - 6 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
5311201 205663 30 None - 6 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
CHEMBL9387 205663 30 None - 6 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL9387 205663 30 None - 6 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
10722103 110986 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 588 8 1 6 5.3 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ncccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL327656 110986 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 588 8 1 6 5.3 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ncccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
73349872 88771 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/0960-894X(96)00160-6
CHEMBL2367718 88771 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/0960-894X(96)00160-6
CHEMBL2367719 88771 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/0960-894X(96)00160-6
11442153 196521 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 444 7 3 4 4.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2s1 10.1016/j.bmc.2009.05.067
CHEMBL575161 196521 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 444 7 3 4 4.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2s1 10.1016/j.bmc.2009.05.067
10789434 204910 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 444 6 3 8 3.1 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccnc2)c1 10.1021/jm970373j
CHEMBL8921 204910 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 444 6 3 8 3.1 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccnc2)c1 10.1021/jm970373j
73349872 88771 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1021/jm0498755
CHEMBL2367718 88771 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1021/jm0498755
CHEMBL2367719 88771 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1021/jm0498755
10839478 110168 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 512 6 2 6 4.1 CN(C)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL325863 110168 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 512 6 2 6 4.1 CN(C)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
15104595 9997 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL115456 9997 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
138106885 166358 71 None -1 4 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
36314 166358 71 None -1 4 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
CHEMBL428647 166358 71 None -1 4 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
44592082 178564 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 411 8 4 4 3.4 CSCC[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL472079 178564 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 411 8 4 4 3.4 CSCC[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
10413579 116582 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.0 Cc1ccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)cc1 10.1021/jm00048a015
CHEMBL339260 116582 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.0 Cc1ccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)cc1 10.1021/jm00048a015
44283152 99392 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 501 10 4 4 4.8 O=C(NC(CNC(CO)Cc1ccccc1)Cc1c[nH]c2ccccc12)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL285762 99392 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 501 10 4 4 4.8 O=C(NC(CNC(CO)Cc1ccccc1)Cc1c[nH]c2ccccc12)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
14208313 67398 0 None - 0 Rat 3.9 pIC50 = 3.9 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 437 3 1 3 4.3 CN1C(=O)[C@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907842 67398 0 None - 0 Rat 3.9 pIC50 = 3.9 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 437 3 1 3 4.3 CN1C(=O)[C@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
44591978 183327 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 533 10 4 4 5.4 O=C(Nc1ccccc1C(=O)NC(Cc1ccc(OCc2ccccc2)cc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL481265 183327 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 533 10 4 4 5.4 O=C(Nc1ccccc1C(=O)NC(Cc1ccc(OCc2ccccc2)cc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
19766227 32984 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 469 6 3 4 3.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(N)Cc1c[nH]c2ccccc12 10.1021/jm00163a069
CHEMBL141786 32984 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 469 6 3 4 3.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(N)Cc1c[nH]c2ccccc12 10.1021/jm00163a069
132190 119831 16 None - 0 Rat 4.9 pIC50 = 4.9 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 O=C1NN(C(=O)Nc2ccc(Br)cc2)C(c2ccccc2)C1c1ccccc1 10.1016/S0960-894X(00)80684-8
CHEMBL352949 119831 16 None - 0 Rat 4.9 pIC50 = 4.9 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 O=C1NN(C(=O)Nc2ccc(Br)cc2)C(c2ccccc2)C1c1ccccc1 10.1016/S0960-894X(00)80684-8
10373378 49396 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 854 20 8 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)C 10.1021/jm00031a013
CHEMBL156642 49396 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 854 20 8 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)C 10.1021/jm00031a013
10530757 118058 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 553 10 3 7 3.6 COC(=O)CC(CC(=O)OC)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
CHEMBL341560 118058 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 553 10 3 7 3.6 COC(=O)CC(CC(=O)OC)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
44287092 99995 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 21 7 7 5.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL290702 99995 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 21 7 7 5.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44368382 45084 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 511 9 4 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL152682 45084 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 511 9 4 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
44286961 161518 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 22 8 7 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL416064 161518 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 22 8 7 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
10478431 9806 7 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00124a003
CHEMBL114325 9806 7 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00124a003
127050962 140215 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 283 3 1 2 2.6 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccc(F)cc1 10.1039/C6MD00052E
CHEMBL3818164 140215 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 283 3 1 2 2.6 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccc(F)cc1 10.1039/C6MD00052E
10478431 9806 7 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00116a002
CHEMBL114325 9806 7 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00116a002
10919004 78023 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 590 7 3 7 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccc([N+](=O)[O-])cc3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL2111547 78023 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 590 7 3 7 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccc([N+](=O)[O-])cc3)C(=O)C[C@@H]12 10.1021/jm010813d
10074366 120087 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3349028 120087 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3545866 120087 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
10032955 167472 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
CHEMBL432256 167472 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
52949124 863 2 None - 2 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
9055 863 2 None - 2 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
CHEMBL1269258 863 2 None - 2 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
DB12694 863 2 None - 2 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
13953715 193010 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 428 3 2 5 4.6 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2-n2cnnc21 10.1021/jm00396a028
CHEMBL53234 193010 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 428 3 2 5 4.6 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2-n2cnnc21 10.1021/jm00396a028
127050298 140309 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 265 1 1 2 2.6 CC(C)(C)N1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
CHEMBL3819315 140309 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 265 1 1 2 2.6 CC(C)(C)N1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
14208233 202812 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 490 3 3 3 4.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Br)ccc2[nH]1 10.1021/jm00120a002
CHEMBL72667 202812 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 490 3 3 3 4.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Br)ccc2[nH]1 10.1021/jm00120a002
44341429 109963 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ccccc2n1 10.1021/jm00116a002
CHEMBL324652 109963 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ccccc2n1 10.1021/jm00116a002
14888719 76883 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1041 29 11 14 -0.1 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(-c2nn[nH]n2)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079547 76883 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1041 29 11 14 -0.1 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(-c2nn[nH]n2)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44370694 47746 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL155017 47746 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
10459108 28197 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 513 8 2 5 3.9 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137516 28197 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 513 8 2 5 3.9 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
9977368 115748 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 385 3 2 4 3.0 CN1C(=O)C(NC(=O)Nc2cccnc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL335865 115748 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 385 3 2 4 3.0 CN1C(=O)C(NC(=O)Nc2cccnc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
90663992 106338 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 866 22 8 9 3.3 CN(C)c1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
CHEMBL3144561 106338 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 866 22 8 9 3.3 CN(C)c1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
14991536 106344 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 841 22 9 9 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144567 106344 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 841 22 9 9 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44279861 102709 0 None - 1 Mouse 6.9 pIC50 = 6.9 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 726 14 6 9 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL30821 102709 0 None - 1 Mouse 6.9 pIC50 = 6.9 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 726 14 6 9 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
23844129 113000 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 497 6 3 5 4.7 CNc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL332024 113000 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 497 6 3 5 4.7 CNc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
14208233 202812 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 490 3 3 3 4.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Br)ccc2[nH]1 10.1021/jm00047a021
CHEMBL72667 202812 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 490 3 3 3 4.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Br)ccc2[nH]1 10.1021/jm00047a021
10721792 167223 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 571 7 1 4 6.3 CC(C)N(C(=O)CN1C(=O)C(C)(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
CHEMBL430451 167223 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 571 7 1 4 6.3 CC(C)N(C(=O)CN1C(=O)C(C)(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
10392653 118536 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 544 5 2 5 3.4 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3ccc(Cl)cc3)N=C(c3ccccc3)c3ccccc32)CC1 10.1016/S0960-894X(00)80683-6
CHEMBL342640 118536 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 544 5 2 5 3.4 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3ccc(Cl)cc3)N=C(c3ccccc3)c3ccccc32)CC1 10.1016/S0960-894X(00)80683-6
10456021 205775 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 442 4 2 5 3.4 COC(=O)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm970373j
CHEMBL9449 205775 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 442 4 2 5 3.4 COC(=O)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm970373j
21842327 45783 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 468 6 2 4 4.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)C)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL153308 45783 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 468 6 2 4 4.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)C)C2=O)c1 10.1016/0960-894X(95)00556-9
11316391 196201 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 431 7 4 3 3.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2c([nH]1)CCCC2 10.1016/j.bmc.2009.05.067
CHEMBL572650 196201 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 431 7 4 3 3.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2c([nH]1)CCCC2 10.1016/j.bmc.2009.05.067
44382698 59160 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 742 15 5 7 5.3 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc(OS(=O)(=O)O)cc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL171375 59160 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 742 15 5 7 5.3 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc(OS(=O)(=O)O)cc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
44370446 119096 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 467 15 2 4 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCC)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL346361 119096 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 467 15 2 4 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCC)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
10392653 118536 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 544 5 2 5 3.4 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3ccc(Cl)cc3)N=C(c3ccccc3)c3ccccc32)CC1 10.1021/jm00078a018
CHEMBL342640 118536 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 544 5 2 5 3.4 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3ccc(Cl)cc3)N=C(c3ccccc3)c3ccccc32)CC1 10.1021/jm00078a018
10070677 161175 13 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL41361 161175 13 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10456021 205775 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 442 4 2 5 3.4 COC(=O)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL9449 205775 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 442 4 2 5 3.4 COC(=O)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL338056 209858 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
15673180 85570 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1100 to 1500The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1100 to 1500
ChEMBL 681 13 6 8 3.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)Nc1nn[nH]n1)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304157 85570 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1100 to 1500The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1100 to 1500
ChEMBL 681 13 6 8 3.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)Nc1nn[nH]n1)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL3142686 209383 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44272230 66740 0 None - 0 Mouse 4.9 pIC50 = 4.9 Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 442 6 3 3 2.9 C[C@H](NC(=O)C1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1)C(=O)NCCc1ccccc1 10.1016/S0960-894X(00)80644-7
CHEMBL18727 66740 0 None - 0 Mouse 4.9 pIC50 = 4.9 Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 442 6 3 3 2.9 C[C@H](NC(=O)C1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1)C(=O)NCCc1ccccc1 10.1016/S0960-894X(00)80644-7
14208310 67399 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 439 7 1 3 5.0 CCCCCc1ccc(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
CHEMBL1907843 67399 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 439 7 1 3 5.0 CCCCCc1ccc(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
10454826 98880 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.
ChEMBL 420 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2C[C@H](N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00234-K
CHEMBL282294 98880 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.
ChEMBL 420 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2C[C@H](N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00234-K
10838675 205484 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 487 8 3 8 4.1 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OCC)c2)c1 10.1021/jm970373j
CHEMBL9267 205484 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 487 8 3 8 4.1 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OCC)c2)c1 10.1021/jm970373j
10279334 124537 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 513 8 2 3 5.7 CN(CCc1ccccc1)C(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL36443 124537 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 513 8 2 3 5.7 CN(CCc1ccccc1)C(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10253714 25290 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 460 4 2 3 5.3 CN1C(=O)C(NC(=O)Nc2cccc(-c3ccccc3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135060 25290 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 460 4 2 3 5.3 CN1C(=O)C(NC(=O)Nc2cccc(-c3ccccc3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
15177358 98614 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 515 9 4 4 4.6 O=C(NC(Cc1c[nH]c2ccccc12)NC(=O)C(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL280502 98614 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 515 9 4 4 4.6 O=C(NC(Cc1c[nH]c2ccccc12)NC(=O)C(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
71457981 78119 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 1147 14 6 10 9.0 CC(C)(C)OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12.CC(C)(C)OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
CHEMBL2111993 78119 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 1147 14 6 10 9.0 CC(C)(C)OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12.CC(C)(C)OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
10720403 118925 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 6 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H]1CCCCC[C@H]1O 10.1021/jm970065l
CHEMBL344882 118925 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 6 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H]1CCCCC[C@H]1O 10.1021/jm970065l
13605417 205834 3 None - 1 Guinea pig 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
CHEMBL9485 205834 3 None - 1 Guinea pig 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
44359338 168101 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 489 6 3 3 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CC2CCC1C2 10.1021/jm970065l
CHEMBL436411 168101 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 489 6 3 3 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CC2CCC1C2 10.1021/jm970065l
9960432 39187 6 None -12 2 Human 6.9 pIC50 = 6.9 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
CHEMBL147186 39187 6 None -12 2 Human 6.9 pIC50 = 6.9 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
CHEMBL1172246 206839 0 None 1 4 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc2ccccc2)C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC1=O 10.1016/j.bmcl.2010.05.078
10762723 96582 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 386 4 3 6 3.2 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccnc2)c1 10.1021/jm970373j
CHEMBL266819 96582 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 386 4 3 6 3.2 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccnc2)c1 10.1021/jm970373j
44349324 16494 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.4 O=C(O)CCC(NC(=O)c1cccc(C(F)(F)F)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL124261 16494 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.4 O=C(O)CCC(NC(=O)c1cccc(C(F)(F)F)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44274261 98412 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 782 19 8 7 4.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL279005 98412 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 782 19 8 7 4.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44283514 170050 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 585 12 3 4 6.0 CC(Cc1c[nH]c2ccccc12)(CN(CCc1ccccc1)C(=O)CCC(=O)O)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL445094 170050 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 585 12 3 4 6.0 CC(Cc1c[nH]c2ccccc12)(CN(CCc1ccccc1)C(=O)CCC(=O)O)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
11442807 76936 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 471 9 4 4 3.2 CC(=O)N/C(=C/c1ccccc1)C(=O)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1021/jm051050n
CHEMBL208171 76936 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 471 9 4 4 3.2 CC(=O)N/C(=C/c1ccccc1)C(=O)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1021/jm051050n
45481637 196665 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 471 10 4 4 3.2 O=C(CC(=O)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)N/C=C/c1ccccc1 10.1016/j.bmc.2009.05.067
CHEMBL576347 196665 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 471 10 4 4 3.2 O=C(CC(=O)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)N/C=C/c1ccccc1 10.1016/j.bmc.2009.05.067
51353551 17950 10 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 17950 10 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
10649606 49349 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
10817241 106638 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 591 8 1 5 5.6 COc1ccc(N(C(=O)CN2C(=O)C(Cc3[nH]nc4c3CCCC4)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL316077 106638 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 591 8 1 5 5.6 COc1ccc(N(C(=O)CN2C(=O)C(Cc3[nH]nc4c3CCCC4)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
44381758 11625 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 565 9 2 5 3.4 CN1CCN(CCNC(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1181391 11625 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 565 9 2 5 3.4 CN1CCN(CCNC(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL169440 11625 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 565 9 2 5 3.4 CN1CCN(CCNC(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
44458096 84625 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 388 5 2 3 2.7 O=C(N[C@@H]1C(=O)N(Cc2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL22417 84625 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 388 5 2 3 2.7 O=C(N[C@@H]1C(=O)N(Cc2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
10009526 110014 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 655 6 3 7 4.6 O=C(Nc1cccc(-c2nn[nH]n2)c1)NC1N=C(c2ccccc2F)c2cccc(Cl)c2N(CC(=O)N2CC3CCC(CC3)C2)C1=O 10.1016/s0960-894x(98)00237-6
CHEMBL32492 110014 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 655 6 3 7 4.6 O=C(Nc1cccc(-c2nn[nH]n2)c1)NC1N=C(c2ccccc2F)c2cccc(Cl)c2N(CC(=O)N2CC3CCC(CC3)C2)C1=O 10.1016/s0960-894x(98)00237-6
54580296 61587 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774035 61587 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
10418081 109883 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 840 23 9 8 2.4 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL324219 109883 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 840 23 9 8 2.4 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44293998 187840 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 609 6 2 5 5.3 CC(=O)c1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL50215 187840 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 609 6 2 5 5.3 CC(=O)c1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
90663995 106341 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 919 23 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144564 106341 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 919 23 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
10769902 204819 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human Cholecystokinin type A receptor by the displacement of [125I]Bolton-Hunter CCK-8Binding affinity against human Cholecystokinin type A receptor by the displacement of [125I]Bolton-Hunter CCK-8
ChEMBL 601 8 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
CHEMBL88629 204819 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human Cholecystokinin type A receptor by the displacement of [125I]Bolton-Hunter CCK-8Binding affinity against human Cholecystokinin type A receptor by the displacement of [125I]Bolton-Hunter CCK-8
ChEMBL 601 8 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
10769902 204819 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 601 8 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL88629 204819 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 601 8 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10555804 111108 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 616 9 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)(OC)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL328285 111108 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 616 9 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)(OC)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
11114520 114952 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=S)C[C@H]12 10.1021/jm010898i
CHEMBL3350849 114952 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=S)C[C@H]12 10.1021/jm010898i
19766167 58923 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 420 4 2 3 3.1 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL170293 58923 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 420 4 2 3 3.1 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
44381577 96188 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 840 23 10 10 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@H](CNN[C@@H](Cc1ccccc1)C(N)=O)CC(=O)O 10.1016/S0960-894X(00)80680-0
CHEMBL263525 96188 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 840 23 10 10 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@H](CNN[C@@H](Cc1ccccc1)C(N)=O)CC(=O)O 10.1016/S0960-894X(00)80680-0
44330731 206503 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 946 25 9 11 0.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN1CC[C@H](NC(=O)CCc2ccc(OS(=O)(=O)O)cc2)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL98720 206503 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 946 25 9 11 0.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN1CC[C@H](NC(=O)CCc2ccc(OS(=O)(=O)O)cc2)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
10369805 100086 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL291458 100086 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
10073082 24933 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 462 3 2 3 4.4 CN1C(=O)C(NC(=O)Nc2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL134750 24933 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 462 3 2 3 4.4 CN1C(=O)C(NC(=O)Nc2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44578530 188101 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 556 5 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL504024 188101 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 556 5 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
90663980 106327 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 891 21 8 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Cl)cc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144549 106327 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 891 21 8 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Cl)cc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44301036 197027 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 695 8 4 6 5.4 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)c3ccccc3C)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL58154 197027 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 695 8 4 6 5.4 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)c3ccccc3C)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
44300864 200234 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 681 8 4 6 5.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)c3ccccc3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL60754 200234 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 681 8 4 6 5.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)c3ccccc3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
367892 9441 1 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
CHEMBL112222 9441 1 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
44349027 16647 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 438 7 3 5 2.9 O=C(O)CCC(NC(=O)c1cnc2ccccc2c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL124732 16647 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 438 7 3 5 2.9 O=C(O)CCC(NC(=O)c1cnc2ccccc2c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44349083 117560 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL340463 117560 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44336486 108871 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 669 8 2 6 6.5 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C3(C(F)(F)F)N=N3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
CHEMBL321915 108871 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 669 8 2 6 6.5 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C3(C(F)(F)F)N=N3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
73349789 105657 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 629 12 6 6 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)NO)c1ccccc1 10.1021/jm00092a007
CHEMBL313499 105657 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 629 12 6 6 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)NO)c1ccccc1 10.1021/jm00092a007
73346724 204368 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 681 13 5 9 5.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)NC1N=NN=N1)c1ccccc1 10.1021/jm00092a007
CHEMBL85607 204368 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 681 13 5 9 5.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)NC1N=NN=N1)c1ccccc1 10.1021/jm00092a007
44311923 202796 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 421 4 2 3 4.0 O=C(Cc1ccc(Cl)cc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL72570 202796 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 421 4 2 3 4.0 O=C(Cc1ccc(Cl)cc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
14802536 156789 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@H](NC(=O)CCCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL2112694 156789 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@H](NC(=O)CCCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL407753 156789 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@H](NC(=O)CCCC(=O)O)c1ccccc1 10.1021/jm00105a062
44356799 25859 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 452 3 2 3 4.7 CN1C(=O)C(NC(=O)Nc2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135538 25859 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 452 3 2 3 4.7 CN1C(=O)C(NC(=O)Nc2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10392870 28887 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 552 7 2 5 5.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)OCc2ccccc2)C1=O 10.1021/jm00078a018
CHEMBL138122 28887 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 552 7 2 5 5.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)OCc2ccccc2)C1=O 10.1021/jm00078a018
14208312 77469 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 437 3 1 3 4.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2092865 77469 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 437 3 1 3 4.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44356710 116111 6 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 426 4 2 4 3.9 CC(=O)c1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL336765 116111 6 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 426 4 2 4 3.9 CC(=O)c1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL285995 99430 0 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 741 16 6 11 4.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCNCCSCc3csc(C=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44280225 99501 0 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 743 15 4 7 5.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL286475 99501 0 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 743 15 4 7 5.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
44334278 4632 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 515 9 2 4 5.5 Cc1cccc(NC(=O)N[C@H](CSCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL103457 4632 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 515 9 2 4 5.5 Cc1cccc(NC(=O)N[C@H](CSCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44334224 4986 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 480 7 2 5 3.3 Cc1cccc(NC(=O)N[C@H](COC(=O)N(C)C)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL105303 4986 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 480 7 2 5 3.3 Cc1cccc(NC(=O)N[C@H](COC(=O)N(C)C)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44334176 5001 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 527 9 2 5 4.7 Cc1cccc(NC(=O)N[C@H](CC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL105404 5001 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 527 9 2 5 4.7 Cc1cccc(NC(=O)N[C@H](CC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44334438 108768 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 513 9 2 4 5.2 Cc1cccc(NC(=O)N[C@@H](C(=O)N2CCC(C(=O)c3ccccc3)CC2)[C@@H](C)OCc2ccccc2)c1 10.1016/0960-894X(95)00537-3
CHEMBL321800 108768 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 513 9 2 4 5.2 Cc1cccc(NC(=O)N[C@@H](C(=O)N2CCC(C(=O)c3ccccc3)CC2)[C@@H](C)OCc2ccccc2)c1 10.1016/0960-894X(95)00537-3
44334270 162935 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 437 8 2 4 3.5 CC(=O)C1CCN(C(=O)[C@@H](COCc2ccccc2)NC(=O)Nc2cccc(C)c2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL420098 162935 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 437 8 2 4 3.5 CC(=O)C1CCN(C(=O)[C@@H](COCc2ccccc2)NC(=O)Nc2cccc(C)c2)CC1 10.1016/0960-894X(95)00537-3
44366601 42181 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 11-16 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 11-16 uM
ChEMBL 323 4 0 3 3.5 O=C1CCN(C(=O)OCc2ccccc2)CC1Cc1ccccc1 10.1016/0960-894X(94)80030-8
CHEMBL149905 42181 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 11-16 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 11-16 uM
ChEMBL 323 4 0 3 3.5 O=C1CCN(C(=O)OCc2ccccc2)CC1Cc1ccccc1 10.1016/0960-894X(94)80030-8
44382487 165084 0 None - 0 Mouse 4.9 pIC50 = 4.9 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 518 10 4 4 2.7 CC(C)C[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
CHEMBL424370 165084 0 None - 0 Mouse 4.9 pIC50 = 4.9 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 518 10 4 4 2.7 CC(C)C[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44349023 16178 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 384 8 3 3 3.4 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00079a003
CHEMBL122922 16178 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 384 8 3 3 3.4 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00079a003
15167808 202844 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 4.1 CN(C(=O)c1cc2ccccc2[nH]1)C1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL72894 202844 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 4.1 CN(C(=O)c1cc2ccccc2[nH]1)C1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
19766230 30508 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 499 6 1 4 4.7 COC(C(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C)(c1ccccc1)C(F)(F)F 10.1021/jm00163a069
CHEMBL139520 30508 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 499 6 1 4 4.7 COC(C(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C)(c1ccccc1)C(F)(F)F 10.1021/jm00163a069
45481627 195021 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 419 7 4 4 2.7 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)C1=CC2CCCC2N1 10.1016/j.bmc.2009.05.067
CHEMBL564796 195021 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 419 7 4 4 2.7 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)C1=CC2CCCC2N1 10.1016/j.bmc.2009.05.067
51353551 17950 10 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269257 17950 10 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
16100406 82811 0 None -33 4 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL218600 82811 0 None -33 4 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
10531224 167438 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 575 7 2 4 5.7 CC(C)N(C(=O)CN1C(=O)C(C)(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
CHEMBL432015 167438 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 575 7 2 4 5.7 CC(C)N(C(=O)CN1C(=O)C(C)(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
10531224 167438 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assayDisplacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assay
ChEMBL 575 7 2 4 5.7 CC(C)N(C(=O)CN1C(=O)C(C)(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
CHEMBL432015 167438 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assayDisplacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assay
ChEMBL 575 7 2 4 5.7 CC(C)N(C(=O)CN1C(=O)C(C)(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
11775012 196435 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 439 7 3 4 3.9 O=C(NC(Cc1ccccc1)C(=O)O)c1ccccc1NC(=O)c1nccc2ccccc12 10.1016/j.bmc.2009.05.067
CHEMBL574530 196435 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 439 7 3 4 3.9 O=C(NC(Cc1ccccc1)C(=O)O)c1ccccc1NC(=O)c1nccc2ccccc12 10.1016/j.bmc.2009.05.067
44287088 99748 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 838 22 7 7 5.6 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL288373 99748 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 838 22 7 7 5.6 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
10649606 49349 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
44396785 66842 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 530 7 2 5 4.6 C[C@H]1C(=O)N(Cc2ccccc2)C(=O)N2CCC[C@@H](N[C@@H](Cc3c[nH]c4ccccc34)C(=O)OC(C)(C)C)C12 10.1021/jm0498755
CHEMBL187732 66842 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 530 7 2 5 4.6 C[C@H]1C(=O)N(Cc2ccccc2)C(=O)N2CCC[C@@H](N[C@@H](Cc3c[nH]c4ccccc34)C(=O)OC(C)(C)C)C12 10.1021/jm0498755
44303669 167726 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 573 10 4 5 3.9 O=C(O)CCC(=O)N[C@@H](CNC(=O)C1(NC(=O)OC2C3CC4CC(C3)CC2C4)Cc2ccccc2C1)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL434020 167726 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 573 10 4 5 3.9 O=C(O)CCC(=O)N[C@@H](CNC(=O)C1(NC(=O)OC2C3CC4CC(C3)CC2C4)Cc2ccccc2C1)c1ccccc1 10.1016/S0960-894X(97)00356-9
44349069 117556 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL340413 117556 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
65987 99116 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 440 6 2 3 4.1 O=C(O)CC[C@@H](NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL283820 99116 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 440 6 2 3 4.1 O=C(O)CC[C@@H](NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
65987 99116 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreas
ChEMBL 440 6 2 3 4.1 O=C(O)CC[C@@H](NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1021/jm950372w
CHEMBL283820 99116 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreas
ChEMBL 440 6 2 3 4.1 O=C(O)CC[C@@H](NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1021/jm950372w
15281185 49189 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 484 5 2 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3cnccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL156484 49189 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 484 5 2 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3cnccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
10555164 112257 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 575 7 1 4 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(F)cc1 10.1021/jm970265x
CHEMBL330521 112257 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 575 7 1 4 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(F)cc1 10.1021/jm970265x
44359376 118854 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 6 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1O 10.1021/jm970065l
CHEMBL344380 118854 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 6 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1O 10.1021/jm970065l
10647112 162871 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 447 3 3 4 4.1 Cc1cccc(NC(=O)N[C@@H]2N=C([C@H]3CCC(C)(C)CCN3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL419663 162871 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 447 3 3 4 4.1 Cc1cccc(NC(=O)N[C@@H]2N=C([C@H]3CCC(C)(C)CCN3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
44211353 58744 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 552 9 2 5 3.5 O=C(CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)NCCN1CCOCC1 10.1016/S0960-894X(00)80681-2
CHEMBL169453 58744 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 552 9 2 5 3.5 O=C(CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)NCCN1CCOCC1 10.1016/S0960-894X(00)80681-2
10484212 99417 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/s0960-894x(98)00237-6
CHEMBL285921 99417 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/s0960-894x(98)00237-6
CHEMBL355608 209992 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N1CC(=O)N[C@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
CHEMBL3142924 209392 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None COc1ccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm960509y
10484212 99417 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL285921 99417 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
9823890 26728 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 428 4 3 4 3.3 CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136412 26728 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 428 4 3 4 3.3 CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44578251 181850 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL478604 181850 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
14991568 100244 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 847 20 8 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL292519 100244 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 847 20 8 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14991575 100317 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 852 20 10 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2cc(O)ccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL293026 100317 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 852 20 10 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2cc(O)ccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL434674 211912 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CN[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
44336539 5075 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10675328 111017 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 617 9 1 6 5.7 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)(OC)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL327815 111017 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 617 9 1 6 5.7 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)(OC)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
46235271 73301 2 None - 2 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CCK-2 from rat CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from rat CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL2017835 73301 2 None - 2 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CCK-2 from rat CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from rat CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
44210424 118713 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 423 4 2 4 3.8 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL34335 118713 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 423 4 2 4 3.8 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1016/S0960-894X(00)80683-6
9868877 205932 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 460 8 2 4 3.8 COc1cccc(N(CC(=O)N(C)c2ccccc2)C(=O)CNC(=O)Nc2cccc(C)c2)c1 10.1021/jm970373j
CHEMBL9534 205932 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 460 8 2 4 3.8 COc1cccc(N(CC(=O)N(C)c2ccccc2)C(=O)CNC(=O)Nc2cccc(C)c2)c1 10.1021/jm970373j
10440992 160749 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 28 9 11 1.8 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL412238 160749 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 28 9 11 1.8 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
10440992 160749 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 28 9 11 1.8 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL412238 160749 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 28 9 11 1.8 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
44382735 120250 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 646 13 4 4 6.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL355275 120250 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 646 13 4 4 6.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL2079550 207449 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(C(F)(F)C(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
19910130 119286 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 439 14 3 3 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL348168 119286 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 439 14 3 3 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
44578562 180952 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc3c2OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL476519 180952 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc3c2OCCO3)cc1 10.1016/j.bmcl.2008.06.057
14991540 106319 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 855 23 8 9 3.2 COc1ccc(CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
CHEMBL3144540 106319 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 855 23 8 9 3.2 COc1ccc(CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
90663993 106339 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 901 21 8 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Br)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144562 106339 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 901 21 8 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Br)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
9828961 167423 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 548 6 4 4 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL431919 167423 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 548 6 4 4 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
44382709 58905 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 504 10 4 4 2.9 CCCC[C@H](NC(=O)c1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
CHEMBL170207 58905 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 504 10 4 4 2.9 CCCC[C@H](NC(=O)c1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44368454 120702 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissueConcentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 549 4 3 7 3.5 CC(C)C[C@]1(C)N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/jm020424z
CHEMBL357749 120702 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissueConcentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 549 4 3 7 3.5 CC(C)C[C@]1(C)N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/jm020424z
14208264 101639 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 411 3 2 3 4.5 CC(C)(C)c1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL302282 101639 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 411 3 2 3 4.5 CC(C)(C)c1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
44382560 119811 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 660 14 4 4 6.5 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL352817 119811 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 660 14 4 4 6.5 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCc1ccccc1 10.1016/S0960-894X(00)80687-3
44362745 32837 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL141655 32837 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
10030203 25686 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 540 6 2 6 2.8 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1021/jm00078a018
CHEMBL135371 25686 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 540 6 2 6 2.8 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1021/jm00078a018
44357031 28486 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 585 8 2 9 3.1 COC(=O)[C@H]1CCCN1OC(=O)CN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137779 28486 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 585 8 2 9 3.1 COC(=O)[C@H]1CCCN1OC(=O)CN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
3035433 99009 12 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of cholecystokinin A receptorInhibition of cholecystokinin A receptor
ChEMBL 535 4 3 7 3.1 CC(C)C[C@@H]1N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/np9800102
CHEMBL283117 99009 12 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of cholecystokinin A receptorInhibition of cholecystokinin A receptor
ChEMBL 535 4 3 7 3.1 CC(C)C[C@@H]1N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/np9800102
44334177 109279 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 508 7 3 3 5.3 Cc1cccc(NC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL323127 109279 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 508 7 3 3 5.3 Cc1cccc(NC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
9983680 162772 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 506 7 2 5 3.8 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL418987 162772 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 506 7 2 5 3.8 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44349185 16354 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 421 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCCC2)C1 10.1021/jm00079a003
CHEMBL123720 16354 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 421 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCCC2)C1 10.1021/jm00079a003
13953698 101439 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 464 5 1 5 5.1 CN(C)Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00396a028
CHEMBL300926 101439 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 464 5 1 5 5.1 CN(C)Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00396a028
15614752 118244 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 549 6 3 5 4.6 O=C1Nc2ccccc2C(c2ccccc2F)=NC1CNCC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00163a069
CHEMBL341815 118244 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 549 6 3 5 4.6 O=C1Nc2ccccc2C(c2ccccc2F)=NC1CNCC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00163a069
44286977 99676 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 782 18 7 7 4.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL287712 99676 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 782 18 7 7 4.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
14208264 101639 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 411 3 2 3 4.5 CC(C)(C)c1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL302282 101639 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 411 3 2 3 4.5 CC(C)(C)c1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
10625001 28965 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 7 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(CO)CCCC1 10.1021/jm970065l
CHEMBL138190 28965 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 7 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(CO)CCCC1 10.1021/jm970065l
73349872 88771 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/S0960-894X(97)00107-8
CHEMBL2367718 88771 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/S0960-894X(97)00107-8
CHEMBL2367719 88771 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/S0960-894X(97)00107-8
44376113 119456 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligandThe compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligand
ChEMBL 494 6 3 6 3.9 CC(C)CN1C(=O)[C@@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL349730 119456 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligandThe compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligand
ChEMBL 494 6 3 6 3.9 CC(C)CN1C(=O)[C@@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
10369803 16405 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 7 3 3 5.7 CCC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
CHEMBL123951 16405 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 7 3 3 5.7 CCC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
10481751 112592 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 518 5 3 3 5.3 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
CHEMBL331315 112592 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 518 5 3 3 5.3 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
11741648 26154 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccncc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL135909 26154 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccncc3N(C)C2=O)c1 10.1021/jm00078a018
3452843 119020 13 None - 10 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL345686 119020 13 None - 10 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
122130 4052 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1016/0960-894X(95)00556-9
888 4052 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1016/0960-894X(95)00556-9
CHEMBL115121 4052 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1016/0960-894X(95)00556-9
122130 4052 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1021/jm960669+
888 4052 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1021/jm960669+
CHEMBL115121 4052 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1021/jm960669+
44283150 164693 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 529 9 3 4 4.7 CN(C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(CO)Cc1ccccc1 10.1021/jm00086a017
CHEMBL422941 164693 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 529 9 3 4 4.7 CN(C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(CO)Cc1ccccc1 10.1021/jm00086a017
15104604 108976 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 448 13 2 3 5.1 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccnc1 10.1021/jm00116a002
CHEMBL322031 108976 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 448 13 2 3 5.1 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccnc1 10.1021/jm00116a002
44359338 168101 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 489 6 3 3 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CC2CCC1C2 10.1021/jm970065l
CHEMBL436411 168101 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 489 6 3 3 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CC2CCC1C2 10.1021/jm970065l
11755707 57218 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 8 2 7 4.7 CCOC(=O)c1cccc(NC(=O)NCc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1016/S0960-894X(97)00108-X
CHEMBL166168 57218 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 8 2 7 4.7 CCOC(=O)c1cccc(NC(=O)NCc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1016/S0960-894X(97)00108-X
10345812 18463 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.0 Cc1ccccc1NC(=O)N[C@@H]1C[C@H](c2ccccc2)c2ccccc2N(CC(=O)NC(C)(C)C)C1=O 10.1021/jm00048a015
CHEMBL127687 18463 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.0 Cc1ccccc1NC(=O)N[C@@H]1C[C@H](c2ccccc2)c2ccccc2N(CC(=O)NC(C)(C)C)C1=O 10.1021/jm00048a015
42636923 178253 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 393 7 4 3 3.6 CC(C)C[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL469341 178253 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 393 7 4 3 3.6 CC(C)C[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
15689733 106132 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 870 21 9 10 3.0 COC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
CHEMBL3142905 106132 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 870 21 9 10 3.0 COC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
52943046 17954 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 557 8 0 6 5.8 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Oc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269262 17954 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 557 8 0 6 5.8 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Oc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
14208305 67402 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907846 67402 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208248 202935 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 441 3 2 3 4.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00120a002
CHEMBL73561 202935 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 441 3 2 3 4.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00120a002
10897104 78185 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 573 7 3 5 4.7 C[C@H](c1ccccc1)N1C(=O)C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
CHEMBL2112237 78185 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 573 7 3 5 4.7 C[C@H](c1ccccc1)N1C(=O)C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
14991582 199564 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 871 21 7 8 4.3 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(Cl)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL60385 199564 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 871 21 7 8 4.3 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(Cl)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14208248 202935 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 441 3 2 3 4.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00047a021
CHEMBL73561 202935 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 441 3 2 3 4.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00047a021
52949124 863 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10008654 127094 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
71456294 79248 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL2115133 79248 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm010813d
136055866 56223 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 468 4 3 7 3.4 CN1C(=O)[C@H](NC(=O)Nc2ccc(-c3noc(O)n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL163610 56223 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 468 4 3 7 3.4 CN1C(=O)[C@H](NC(=O)Nc2ccc(-c3noc(O)n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
10509945 88954 0 None - 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL2369816 88954 0 None - 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44215880 69065 0 None - 2 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)NC(CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933100 69065 0 None - 2 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)NC(CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10507561 120488 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 585 7 2 4 5.4 CC(C)N(C(=O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
CHEMBL356408 120488 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 585 7 2 4 5.4 CC(C)N(C(=O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
CHEMBL2372623 208532 0 None -16 4 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
44310934 202699 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 575 7 3 6 4.1 COc1ccc(N2C(=O)CC3C(NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
CHEMBL71996 202699 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 575 7 3 6 4.1 COc1ccc(N2C(=O)CC3C(NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
10462874 98380 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 766 16 6 5 7.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCCNC(=O)Nc1ccccc1Cl 10.1016/s0960-894x(00)00198-0
CHEMBL278780 98380 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 766 16 6 5 7.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCCNC(=O)Nc1ccccc1Cl 10.1016/s0960-894x(00)00198-0
15666987 206456 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL98446 206456 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
15667019 206488 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 905 26 9 10 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCNC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL98631 206488 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 905 26 9 10 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCNC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
14208217 202449 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 379 3 2 4 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccsc1 10.1021/jm00120a002
CHEMBL70550 202449 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 379 3 2 4 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccsc1 10.1021/jm00120a002
44381914 12893 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 14 1 4 4.7 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80681-2
CHEMBL1189721 12893 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 14 1 4 4.7 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80681-2
CHEMBL539320 12893 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 14 1 4 4.7 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80681-2
73354295 105466 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 643 13 5 6 4.5 CONC(=O)CCC(=O)N[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1021/jm00092a007
CHEMBL312894 105466 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 643 13 5 6 4.5 CONC(=O)CCC(=O)N[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1021/jm00092a007
44311626 202443 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 4 2 4 4.8 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(SC(F)(F)F)cc1 10.1021/jm00120a002
CHEMBL70499 202443 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 4 2 4 4.8 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(SC(F)(F)F)cc1 10.1021/jm00120a002
15104623 9925 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 476 13 3 2 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1cccc(C)c1 10.1021/jm00116a002
CHEMBL114997 9925 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 476 13 3 2 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1cccc(C)c1 10.1021/jm00116a002
15104625 110033 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 651 16 2 6 8.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c(Sc2ccccc2[N+](=O)[O-])[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL325067 110033 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 651 16 2 6 8.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c(Sc2ccccc2[N+](=O)[O-])[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
44334225 4919 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 522 7 2 6 3.1 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCOCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL104958 4919 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 522 7 2 6 3.1 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCOCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
71452639 78042 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 542 9 2 5 4.0 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCN(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL2111654 78042 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 542 9 2 5 4.0 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCN(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
10673078 28874 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 502 6 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1C#N 10.1021/jm970065l
CHEMBL138112 28874 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 502 6 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1C#N 10.1021/jm970065l
CHEMBL406978 210884 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
CHEMBL2372073 208435 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@H]1CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2007.05.067
44359840 164896 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 395 4 2 5 3.5 O=C1Nc2ccccc2C(c2ccccc2F)=NC1CNc1cnc(Cl)cn1 10.1021/jm00163a069
CHEMBL423918 164896 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 395 4 2 5 3.5 O=C1Nc2ccccc2C(c2ccccc2F)=NC1CNc1cnc(Cl)cn1 10.1021/jm00163a069
44280373 98929 0 None - 1 Mouse 4.8 pIC50 = 4.8 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 5.4 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL282646 98929 0 None - 1 Mouse 4.8 pIC50 = 4.8 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 5.4 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
10839347 30047 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 7 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(CO)CCCCC1 10.1021/jm970065l
CHEMBL139101 30047 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 7 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(CO)CCCCC1 10.1021/jm970065l
45482481 196200 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)N[C@H](Cc1ccccc1)C(=O)O)c1cc2cc(F)ccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL572649 196200 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)N[C@H](Cc1ccccc1)C(=O)O)c1cc2cc(F)ccc2[nH]1 10.1016/j.bmc.2009.05.067
44336539 5075 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10156187 102632 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00120a002
CHEMBL307659 102632 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00120a002
10156187 102632 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00047a021
CHEMBL307659 102632 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00047a021
10249484 22453 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 385 3 2 4 3.0 CN1C(=O)C(NC(=O)Nc2ccncc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL132699 22453 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 385 3 2 4 3.0 CN1C(=O)C(NC(=O)Nc2ccncc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10672231 204241 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 475 5 3 4 4.9 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
CHEMBL84433 204241 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 475 5 3 4 4.9 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
14208195 15090 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 4 2 4 4.8 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(SC(F)(F)F)c1 10.1021/jm00047a021
CHEMBL121210 15090 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 4 2 4 4.8 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(SC(F)(F)F)c1 10.1021/jm00047a021
10673570 29942 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 521 7 4 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(C(=O)O)CCCCC1 10.1021/jm970065l
CHEMBL139001 29942 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 521 7 4 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(C(=O)O)CCCCC1 10.1021/jm970065l
10719765 77958 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 487 6 4 7 3.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CNc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm9506736
CHEMBL2110202 77958 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 487 6 4 7 3.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CNc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm9506736
44336539 5075 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
44368562 121449 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 588 12 5 5 4.3 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL359076 121449 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 588 12 5 5 4.3 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00057a005
10698109 106812 0 None 5 2 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
CHEMBL317181 106812 0 None 5 2 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
10698109 106812 0 None 5 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assayDisplacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assay
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
CHEMBL317181 106812 0 None 5 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assayDisplacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assay
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
10790099 205543 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 459 7 3 7 4.3 COc1ccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)cc1 10.1021/jm970373j
CHEMBL9311 205543 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 459 7 3 7 4.3 COc1ccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)cc1 10.1021/jm970373j
44341327 162780 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 504 13 3 2 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00116a002
CHEMBL419031 162780 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 504 13 3 2 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00116a002
15637206 78491 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 428 4 3 4 3.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(C(=O)O)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL2112932 78491 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 428 4 3 4 3.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(C(=O)O)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
9866980 4588 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 423 3 2 4 4.6 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N3C[C@H](C)N=C23)c1 10.1016/0960-894X(95)00530-0
CHEMBL103119 4588 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 423 3 2 4 4.6 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N3C[C@H](C)N=C23)c1 10.1016/0960-894X(95)00530-0
10577834 116244 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 518 6 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CC2CCC(CC2)C1 10.1021/jm970065l
CHEMBL337529 116244 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 518 6 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CC2CCC(CC2)C1 10.1021/jm970065l
10768419 28895 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 525 10 5 5 3.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(CC(=O)O)CC(=O)O 10.1021/jm970065l
CHEMBL138127 28895 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 525 10 5 5 3.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(CC(=O)O)CC(=O)O 10.1021/jm970065l
15291593 112354 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 537 6 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCC3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL330933 112354 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 537 6 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCC3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
5311201 205663 30 None -1174 6 Human 6.8 pIC50 = 6.8 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00001a027
CHEMBL9387 205663 30 None -1174 6 Human 6.8 pIC50 = 6.8 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00001a027
14208215 103323 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc2ccccc12 10.1021/jm00047a021
CHEMBL309017 103323 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc2ccccc12 10.1021/jm00047a021
10531430 111855 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1ccccc1N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)C(C)C 10.1021/jm970265x
CHEMBL329407 111855 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1ccccc1N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)C(C)C 10.1021/jm970265x
10391834 37990 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL 516 11 3 4 4.5 CC(C)N(C(=O)CN(C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1ccccc1)c1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00062-0
CHEMBL146206 37990 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL 516 11 3 4 4.5 CC(C)N(C(=O)CN(C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1ccccc1)c1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00062-0
45482491 196733 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL576957 196733 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
44283151 118662 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 531 9 4 4 5.6 O=C(NC(Cc1c[nH]c2ccccc12)/C(S)=N/C(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL34300 118662 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 531 9 4 4 5.6 O=C(NC(Cc1c[nH]c2ccccc12)/C(S)=N/C(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
15689739 106110 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142683 106110 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
15689738 106121 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142705 106121 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL98468 214150 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None Cc1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm00113a023
44286653 147053 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 794 17 7 7 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H]1CC(=O)N([C@@H](Cc2ccccc2)C(N)=O)C1 10.1021/jm00037a005
CHEMBL39310 147053 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 794 17 7 7 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H]1CC(=O)N([C@@H](Cc2ccccc2)C(N)=O)C1 10.1021/jm00037a005
CHEMBL98468 214150 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None Cc1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
CHEMBL98468 214150 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm00173a006
44381479 59212 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 824 21 8 9 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL171593 59212 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 824 21 8 9 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
44458112 98254 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 374 4 2 3 2.7 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL277661 98254 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 374 4 2 3 2.7 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL2310857 207744 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N1CC(OS(=O)(=O)O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
44578422 180980 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5n4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476739 180980 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5n4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
90663974 106314 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144536 106314 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
155550911 173356 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1884 70 16 23 3.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4540877 173356 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1884 70 16 23 3.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL160753 207066 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CN[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
52949124 863 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
54586174 61586 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 514 5 0 5 6.2 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774034 61586 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 514 5 0 5 6.2 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
11801911 111027 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 613 8 1 5 6.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C2CCCC2)cc1 10.1021/jm970265x
CHEMBL327849 111027 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 613 8 1 5 6.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C2CCCC2)cc1 10.1021/jm970265x
15689728 106119 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1c(Cl)cccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142703 106119 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1c(Cl)cccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44336583 109555 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 665 9 2 5 6.6 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)c3ccccc3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
CHEMBL323512 109555 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 665 9 2 5 6.6 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)c3ccccc3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
44293971 188446 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 611 6 3 5 4.8 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(C(=O)O)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL50926 188446 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 611 6 3 5 4.8 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(C(=O)O)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
9802550 118671 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 426 4 2 3 4.4 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1cc2ccccc2[nH]1 10.1021/jm00163a069
CHEMBL343066 118671 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 426 4 2 3 4.4 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1cc2ccccc2[nH]1 10.1021/jm00163a069
10047370 78407 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 413 4 3 4 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(CN)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2112754 78407 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 413 4 3 4 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(CN)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44578529 182192 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 7 0 5 6.8 CCCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479030 182192 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 7 0 5 6.8 CCCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
14991544 106322 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 857 22 10 10 2.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(O)c(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144543 106322 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 857 22 10 10 2.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(O)c(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44381481 120122 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 841 22 9 9 3.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CNN[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL354670 120122 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 841 22 9 9 3.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CNN[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
14208288 67341 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 349 2 1 3 3.0 CN1C(=O)[C@@H](NC(=O)C(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907660 67341 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 349 2 1 3 3.0 CN1C(=O)[C@@H](NC(=O)C(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14208215 103323 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc2ccccc12 10.1021/jm00120a002
CHEMBL309017 103323 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc2ccccc12 10.1021/jm00120a002
10673039 57956 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 501 5 3 7 3.8 Cc1ccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)cc1N(C)c1nn[nH]n1 10.1021/jm9506736
CHEMBL168253 57956 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 501 5 3 7 3.8 Cc1ccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)cc1N(C)c1nn[nH]n1 10.1021/jm9506736
162672110 182278 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assayInhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assay
ChEMBL 848 22 9 9 2.0 CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00530
CHEMBL4791620 182278 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assayInhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assay
ChEMBL 848 22 9 9 2.0 CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00530
132980 2209 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm9608523
881 2209 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm9608523
CHEMBL420783 2209 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm9608523
44348850 17766 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 986 24 11 11 2.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL126008 17766 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 986 24 11 11 2.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
3040489 44310 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 12-20 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 12-20 uM
ChEMBL 318 4 1 2 3.8 O=C1CCN(Cc2ccccc2)CC1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL151990 44310 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 12-20 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 12-20 uM
ChEMBL 318 4 1 2 3.8 O=C1CCN(Cc2ccccc2)CC1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
15167783 67380 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 409 4 3 3 4.3 O=C(O)c1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc21 10.1021/jm00390a019
CHEMBL1907735 67380 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 409 4 3 3 4.3 O=C(O)c1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc21 10.1021/jm00390a019
44370406 49617 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 529 16 2 4 6.6 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCc1ccccc1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL156814 49617 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 529 16 2 4 6.6 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCc1ccccc1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
132980 2209 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm00032a002
881 2209 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm00032a002
CHEMBL420783 2209 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm00032a002
132980 2209 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1016/0960-894X(95)00530-0
881 2209 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1016/0960-894X(95)00530-0
CHEMBL420783 2209 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1016/0960-894X(95)00530-0
71456223 78356 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1006 25 11 11 1.8 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C[C@@H]1CCCC[C@@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL2112635 78356 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1006 25 11 11 1.8 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C[C@@H]1CCCC[C@@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
10530003 96555 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 520 7 2 5 5.3 CC(C)Oc1cccc(-n2c(CCNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL266598 96555 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 520 7 2 5 5.3 CC(C)Oc1cccc(-n2c(CCNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
44283031 99527 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 613 13 2 5 6.4 CCOC(=O)CCC(=O)N(CCc1ccccc1)CC(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL286664 99527 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 613 13 2 5 6.4 CCOC(=O)CCC(=O)N(CCc1ccccc1)CC(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10530003 96555 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 520 7 2 5 5.3 CC(C)Oc1cccc(-n2c(CCNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL266598 96555 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 520 7 2 5 5.3 CC(C)Oc1cccc(-n2c(CCNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
136000594 61538 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 517 4 2 7 5.0 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc(O)c(O)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773890 61538 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 517 4 2 7 5.0 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc(O)c(O)c2)cc1 10.1016/j.bmcl.2011.03.069
44379911 58565 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 442 6 2 5 4.8 Cc1cccc(NC(=O)NCc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1016/S0960-894X(97)00108-X
CHEMBL168875 58565 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 442 6 2 5 4.8 Cc1cccc(NC(=O)NCc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1016/S0960-894X(97)00108-X
136060576 87064 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Displacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assay
ChEMBL 571 5 1 5 8.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(-c4ccccc4)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL233457 87064 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Displacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assay
ChEMBL 571 5 1 5 8.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(-c4ccccc4)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
10071178 74146 1 None - 2 Guinea pig 4.8 pIC50 = 4.8 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL202861 74146 1 None - 2 Guinea pig 4.8 pIC50 = 4.8 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
54580265 61532 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccccc1-c1cnc(C(=O)N2CCN(c3cnc4ccccc4c3)CC2)nc1-c1ccc(C)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773884 61532 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccccc1-c1cnc(C(=O)N2CCN(c3cnc4ccccc4c3)CC2)nc1-c1ccc(C)cc1 10.1016/j.bmcl.2011.03.069
15104632 110051 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 520 9 3 5 4.5 CCOC(=O)[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
CHEMBL325161 110051 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 520 9 3 5 4.5 CCOC(=O)[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
11734332 78182 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 551 6 3 5 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(C3CCCCC3)C(=O)C[C@H]12 10.1021/jm010813d
CHEMBL2112233 78182 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 551 6 3 5 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(C3CCCCC3)C(=O)C[C@H]12 10.1021/jm010813d
10047411 28393 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
CHEMBL137684 28393 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
71459887 78073 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1006 25 11 11 1.8 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C[C@H]1CCCC[C@@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL2111823 78073 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1006 25 11 11 1.8 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C[C@H]1CCCC[C@@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
52949124 863 2 None -2 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
155542545 172549 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1770 70 16 21 3.9 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4520699 172549 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1770 70 16 21 3.9 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44281204 99388 0 None - 1 Mouse 5.8 pIC50 = 5.8 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 871 18 4 10 5.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL285719 99388 0 None - 1 Mouse 5.8 pIC50 = 5.8 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 871 18 4 10 5.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
10649296 30560 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 6 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H]1CCCCC[C@@H]1O 10.1021/jm970065l
CHEMBL139601 30560 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 6 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H]1CCCCC[C@@H]1O 10.1021/jm970065l
10391769 17556 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 514 6 3 4 4.7 COc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1021/jm00048a015
CHEMBL125863 17556 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 514 6 3 4 4.7 COc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1021/jm00048a015
10601831 96057 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 511 6 3 7 5.0 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2Cl)c1 10.1021/jm970373j
CHEMBL262569 96057 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 511 6 3 7 5.0 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2Cl)c1 10.1021/jm970373j
44336539 5075 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10047172 78405 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 410 4 2 3 4.3 C=Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL2112752 78405 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 410 4 2 3 4.3 C=Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
70689619 73291 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 592 6 1 5 6.5 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017825 73291 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 592 6 1 5 6.5 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
46235271 73301 2 None - 2 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counterDisplacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None - 2 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counterDisplacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
44592045 178327 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 441 8 4 3 4.2 O=C(O)CC(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL469979 178327 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 441 8 4 3 4.2 O=C(O)CC(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
14208252 67411 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL1907854 67411 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
14208256 202824 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 433 5 2 5 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1OC 10.1021/jm00047a021
CHEMBL72727 202824 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 433 5 2 5 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1OC 10.1021/jm00047a021
10341247 119585 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 405 2 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(N3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL350853 119585 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 405 2 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(N3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
44286672 99910 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 836 18 6 7 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1CC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL289804 99910 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 836 18 6 7 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1CC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
52946666 17952 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269260 17952 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
10056643 108720 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 918 21 8 8 5.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL321653 108720 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 918 21 8 8 5.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44293810 101283 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 581 5 2 4 5.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL299800 101283 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 581 5 2 4 5.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
44578399 181372 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 492 5 1 6 4.7 COc1cccc(-n2cc(C(=O)N3CCN(c4nc5ccccc5[nH]4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL477996 181372 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 492 5 1 6 4.7 COc1cccc(-n2cc(C(=O)N3CCN(c4nc5ccccc5[nH]4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44382329 120114 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 475 3 2 2 5.9 O=C1NN(C(=S)Nc2ccc(Cl)c(C(F)(F)F)c2)[C@H](c2ccccc2)[C@H]1c1ccccc1 10.1016/S0960-894X(00)80684-8
CHEMBL354633 120114 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 475 3 2 2 5.9 O=C1NN(C(=S)Nc2ccc(Cl)c(C(F)(F)F)c2)[C@H](c2ccccc2)[C@H]1c1ccccc1 10.1016/S0960-894X(00)80684-8
10603713 111157 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4cccc(F)c34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL328586 111157 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4cccc(F)c34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10770092 111042 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 614 8 0 5 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3cn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL327909 111042 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 614 8 0 5 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3cn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
54582287 61540 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 501 5 0 6 5.3 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773892 61540 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 501 5 0 6 5.3 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.03.069
15689725 106120 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142704 106120 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142689 209385 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44458114 84974 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 393 4 2 4 2.2 O=C(N[C@@H]1C(=O)N(c2ccccc2F)C[C@@H]1C(=O)O)c1cnc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL22630 84974 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 393 4 2 4 2.2 O=C(N[C@@H]1C(=O)N(c2ccccc2F)C[C@@H]1C(=O)O)c1cnc2ccccc2c1 10.1016/S0960-894X(00)80224-3
3960 2313 20 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1039/C6MD00052E
891 2313 20 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1039/C6MD00052E
CHEMBL24938 2313 20 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1039/C6MD00052E
10463229 119304 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 840 20 9 8 3.8 CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)Nc1ccccc1C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1021/jm00031a013
CHEMBL348346 119304 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 840 20 9 8 3.8 CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)Nc1ccccc1C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1021/jm00031a013
14888714 76896 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1067 30 11 12 0.9 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(C(F)(F)C(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079602 76896 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1067 30 11 12 0.9 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(C(F)(F)C(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44370461 119061 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL346070 119061 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
10075097 28432 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 511 6 2 5 3.6 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1021/jm00078a018
CHEMBL137726 28432 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 511 6 2 5 3.6 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1021/jm00078a018
19766160 58201 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 456 4 2 3 3.9 O=C(Nc1cccc2ccccc12)NC1CCc2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1016/S0960-894X(00)80683-6
CHEMBL168386 58201 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 456 4 2 3 3.9 O=C(Nc1cccc2ccccc12)NC1CCc2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1016/S0960-894X(00)80683-6
71449079 78217 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 639 11 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)Cc1cc(O)no1)c1ccccc1 10.1021/jm00092a007
CHEMBL2112334 78217 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 639 11 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)Cc1cc(O)no1)c1ccccc1 10.1021/jm00092a007
73348230 204639 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 634 11 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CP(C)(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL87470 204639 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 634 11 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CP(C)(=O)O)c1ccccc1 10.1021/jm00092a007
14208252 67411 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907854 67411 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14208256 202824 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 433 5 2 5 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1OC 10.1021/jm00120a002
CHEMBL72727 202824 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 433 5 2 5 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1OC 10.1021/jm00120a002
15104631 112350 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 520 9 3 5 4.5 CCOC(=O)[C@@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
CHEMBL330918 112350 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 520 9 3 5 4.5 CCOC(=O)[C@@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
44280114 5041 0 None 1 2 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 567 7 2 4 6.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL105618 5041 0 None 1 2 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 567 7 2 4 6.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
14208197 202931 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 537 6 4 5 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL73535 202931 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 537 6 4 5 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
15614734 67375 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 411 3 0 3 4.7 CN1C(=O)[C@@H](Cc2cn(C)c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907729 67375 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 411 3 0 3 4.7 CN1C(=O)[C@@H](Cc2cn(C)c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
10031700 12084 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 486 7 2 4 3.7 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC[N+](C)(C)C)C2=O)c1 10.1021/jm00078a018
CHEMBL1184246 12084 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 486 7 2 4 3.7 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC[N+](C)(C)C)C2=O)c1 10.1021/jm00078a018
CHEMBL340975 12084 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 486 7 2 4 3.7 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC[N+](C)(C)C)C2=O)c1 10.1021/jm00078a018
10007047 16742 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 524 5 3 3 5.8 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](C2CCCCC2)c2ccccc21 10.1021/jm00048a015
CHEMBL125253 16742 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 524 5 3 3 5.8 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](C2CCCCC2)c2ccccc21 10.1021/jm00048a015
44381641 168076 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
CHEMBL436253 168076 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
10646538 96918 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 435 6 3 6 4.1 CC(C)Oc1cccc(-n2c(NNC(=O)NC3CCCCC3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL269606 96918 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 435 6 3 6 4.1 CC(C)Oc1cccc(-n2c(NNC(=O)NC3CCCCC3)nc3ccccc3c2=O)c1 10.1021/jm970373j
54586149 61542 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(C)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773894 61542 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(C)c2)cc1 10.1016/j.bmcl.2011.03.069
9853654 22588 37 None - 2 Rat 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00079a003
CHEMBL1328 22588 37 None - 2 Rat 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00079a003
44318235 11971 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 513 7 2 4 3.0 CCN(CC)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C(c2cccc[n+]2C)c2ccccc21 10.1021/jm9608523
CHEMBL1183721 11971 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 513 7 2 4 3.0 CCN(CC)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C(c2cccc[n+]2C)c2ccccc21 10.1021/jm9608523
CHEMBL314846 11971 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 513 7 2 4 3.0 CCN(CC)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C(c2cccc[n+]2C)c2ccccc21 10.1021/jm9608523
10369805 100086 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL291458 100086 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
14208266 103901 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 371 3 3 4 2.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(O)cc1 10.1021/jm00047a021
CHEMBL310250 103901 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 371 3 3 4 2.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(O)cc1 10.1021/jm00047a021
45482484 196303 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 455 9 4 3 4.2 O=C(CCc1c[nH]c2ccccc12)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1016/j.bmc.2009.05.067
CHEMBL573555 196303 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 455 9 4 3 4.2 O=C(CCc1c[nH]c2ccccc12)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1016/j.bmc.2009.05.067
9953071 197387 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL58699 197387 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
9953071 197387 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
CHEMBL58699 197387 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
71460027 79305 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 541 9 4 4 5.3 O=C(O)C[C@H](Cc1ccccc1)NC(=O)C(=Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
CHEMBL2115544 79305 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 541 9 4 4 5.3 O=C(O)C[C@H](Cc1ccccc1)NC(=O)C(=Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
10009450 99404 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 649 7 3 7 4.5 CCc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/s0960-894x(98)00237-6
CHEMBL285850 99404 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 649 7 3 7 4.5 CCc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/s0960-894x(98)00237-6
14208259 202456 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 545 4 1 4 5.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2N(C(=O)c2ccc(Cl)cc2)C1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
CHEMBL70593 202456 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 545 4 1 4 5.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2N(C(=O)c2ccc(Cl)cc2)C1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
10260012 109161 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 858 22 8 7 3.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL322391 109161 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 858 22 8 7 3.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
3960 2313 20 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
891 2313 20 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
CHEMBL24938 2313 20 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
10074366 120087 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3349028 120087 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3545866 120087 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
44359879 32804 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 445 7 1 5 4.4 COC(=O)CC(NCC1CN=C(c2ccccc2F)c2ccccc2N1C)c1ccccc1 10.1021/jm00163a069
CHEMBL141629 32804 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 445 7 1 5 4.4 COC(=O)CC(NCC1CN=C(c2ccccc2F)c2ccccc2N1C)c1ccccc1 10.1021/jm00163a069
44458049 98640 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 363 4 3 3 2.0 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1cc2ccccc2[nH]1 10.1016/S0960-894X(00)80224-3
CHEMBL280733 98640 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 363 4 3 3 2.0 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1cc2ccccc2[nH]1 10.1016/S0960-894X(00)80224-3
44372113 10173 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
In vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 1105 30 11 13 2.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC 10.1021/jm00031a013
CHEMBL1161390 10173 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
In vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 1105 30 11 13 2.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC 10.1021/jm00031a013
10369805 100086 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL291458 100086 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
15104630 9474 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 462 7 3 3 4.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
CHEMBL112387 9474 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 462 7 3 3 4.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
44362746 118486 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL342520 118486 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
10252412 25568 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 435 3 2 4 4.2 CN1C(=O)C(NC(=O)Nc2ccc3ccccc3n2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135289 25568 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 435 3 2 4 4.2 CN1C(=O)C(NC(=O)Nc2ccc3ccccc3n2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991537 106313 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 921 24 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1cccc(OS(=O)(=O)O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144535 106313 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 921 24 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1cccc(OS(=O)(=O)O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3143668 209433 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/0960-894X(96)00160-6
CHEMBL64605 214079 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
Compound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pigCompound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pig
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a068
44381749 12789 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 540 14 1 4 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80681-2
CHEMBL1188959 12789 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 540 14 1 4 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80681-2
CHEMBL537834 12789 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 540 14 1 4 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80681-2
CHEMBL64605 214079 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
CHEMBL64605 214079 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL64605 214079 6 None - 3 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050689o
14208266 103901 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 371 3 3 4 2.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(O)cc1 10.1021/jm00120a002
CHEMBL310250 103901 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 371 3 3 4 2.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(O)cc1 10.1021/jm00120a002
CHEMBL64605 214079 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assayInhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00530
9953071 197387 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL58699 197387 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL64605 214079 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44334258 4398 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 451 8 3 4 3.5 Cc1cccc(NC(=O)N[C@H](CCC(=O)O)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL101752 4398 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 451 8 3 4 3.5 Cc1cccc(NC(=O)N[C@H](CCC(=O)O)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44334452 4491 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 497 9 2 3 5.6 Cc1cccc(NC(=O)N[C@H](CCCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL102461 4491 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 497 9 2 3 5.6 Cc1cccc(NC(=O)N[C@H](CCCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL64605 214079 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to guinea pig cortical Cholecystokinin type A receptorTested for the inhibition of specific [3H]propionyl-CCK-8 binding to guinea pig cortical Cholecystokinin type A receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
15673181 85569 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 900 to 1900The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 900 to 1900
ChEMBL 629 12 6 6 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)NO)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304156 85569 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 900 to 1900The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 900 to 1900
ChEMBL 629 12 6 6 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)NO)c1ccccc1 10.1016/S0960-894X(00)80652-6
44354125 22949 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL133101 22949 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
14802539 76199 1 None - 1 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL2062144 76199 1 None - 1 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80685-X
44286962 100012 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 810 21 8 7 4.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL290896 100012 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 810 21 8 7 4.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44368521 46033 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 576 12 5 5 4.6 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00057a005
CHEMBL153557 46033 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 576 12 5 5 4.6 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00057a005
23844130 10019 12 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 484 5 3 6 3.6 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
CHEMBL115612 10019 12 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 484 5 3 6 3.6 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
45482479 196167 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 461 7 4 3 4.5 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL572412 196167 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 461 7 4 3 4.5 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmc.2009.05.067
71719689 85562 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 500 8 3 4 4.8 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccn1 10.1016/S0960-894X(01)80769-1
CHEMBL2304063 85562 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 500 8 3 4 4.8 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccn1 10.1016/S0960-894X(01)80769-1
44381925 12743 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 538 11 2 4 4.5 CCN(CC)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1188615 12743 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 538 11 2 4 4.5 CCN(CC)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL536938 12743 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 538 11 2 4 4.5 CCN(CC)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
5311347 106872 3 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL317675 106872 3 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
5311347 32807 3 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL141630 32807 3 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
5311347 106872 3 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL317675 106872 3 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm00057a005
5311347 32807 3 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm970065l
CHEMBL141630 32807 3 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm970065l
45482097 196685 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(NC(Cc1ccccc1)C(=O)O)c1ccccc1NC(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2009.05.067
CHEMBL576584 196685 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(NC(Cc1ccccc1)C(=O)O)c1ccccc1NC(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2009.05.067
10649606 49349 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
44349024 16950 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 402 8 3 3 3.5 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00079a003
CHEMBL125551 16950 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 402 8 3 3 3.5 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00079a003
44381851 119872 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(=O)O 10.1016/S0960-894X(97)00107-8
CHEMBL353305 119872 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(=O)O 10.1016/S0960-894X(97)00107-8
44283500 138733 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 516 9 3 5 4.8 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)OC(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL37903 138733 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 516 9 3 5 4.8 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)OC(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
11753772 25786 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 455 6 2 4 3.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCN(C)C)C2=O)c1 10.1021/jm00078a018
CHEMBL135447 25786 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 455 6 2 4 3.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCN(C)C)C2=O)c1 10.1021/jm00078a018
15689734 106127 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 854 21 9 9 3.5 CC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm00113a023
CHEMBL3142899 106127 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 854 21 9 9 3.5 CC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm00113a023
367892 9441 1 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
CHEMBL112222 9441 1 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
44287094 99837 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 20 6 7 5.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL289209 99837 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 20 6 7 5.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
15689734 106127 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 854 21 9 9 3.5 CC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
CHEMBL3142899 106127 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 854 21 9 9 3.5 CC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
54584255 61588 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774036 61588 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
14208275 67405 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 3 1 3 4.7 CN1C(=O)[C@@H](NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907849 67405 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 3 1 3 4.7 CN1C(=O)[C@@H](NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208226 77475 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 3 3.9 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL2092871 77475 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 3 3.9 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10011017 108245 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 916 22 8 7 5.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL320854 108245 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 916 22 8 7 5.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
367892 9441 1 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
CHEMBL112222 9441 1 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
14991579 100521 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 862 21 9 8 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL294304 100521 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 862 21 9 8 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14208275 67405 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 443 3 1 3 4.7 CN1C(=O)[C@@H](NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL1907849 67405 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 443 3 1 3 4.7 CN1C(=O)[C@@H](NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
155531277 171065 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1821 72 18 23 2.1 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4465747 171065 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1821 72 18 23 2.1 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
52944224 17951 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 586 8 2 7 5.6 CC(C)N(C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269259 17951 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 586 8 2 7 5.6 CC(C)N(C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
10478703 119407 1 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(NC(=O)NC2N=C(N3CC4CCC(CC4)C3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL349291 119407 1 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(NC(=O)NC2N=C(N3CC4CCC(CC4)C3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
14208271 102422 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 3 1 3 4.4 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL305951 102422 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 3 1 3 4.4 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
14208214 164696 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc2ccccc2c1 10.1021/jm00047a021
CHEMBL422951 164696 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc2ccccc2c1 10.1021/jm00047a021
44306744 102193 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 782 20 9 7 2.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL304524 102193 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 782 20 9 7 2.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL1172253 206843 0 None -138 4 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
CHEMBL319438 209471 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00017a022
44304324 199019 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required for 50% inhibition of cholecystokinin A(CCK A)Concentration required for 50% inhibition of cholecystokinin A(CCK A)
ChEMBL 515 13 2 2 7.0 CCCCCN(CCCCC)C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(97)00353-3
CHEMBL59993 199019 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required for 50% inhibition of cholecystokinin A(CCK A)Concentration required for 50% inhibition of cholecystokinin A(CCK A)
ChEMBL 515 13 2 2 7.0 CCCCCN(CCCCC)C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(97)00353-3
444998 207574 26 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
CHEMBL216166 207574 26 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
44382563 120239 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 742 15 5 7 5.3 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccc(OS(=O)(=O)O)cc1 10.1016/S0960-894X(00)80687-3
CHEMBL355052 120239 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 742 15 5 7 5.3 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccc(OS(=O)(=O)O)cc1 10.1016/S0960-894X(00)80687-3
15104599 9920 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 515 13 2 2 7.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00116a002
CHEMBL114980 9920 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 515 13 2 2 7.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00116a002
11757086 25472 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 541 10 2 6 4.2 CCN(CC)CC(=O)OCCN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135218 25472 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 541 10 2 6 4.2 CCN(CC)CC(=O)OCCN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44578456 189005 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5cnccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL514716 189005 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5cnccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44279811 96477 0 None - 1 Mouse 6.7 pIC50 = 6.7 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 743 15 4 7 5.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL265987 96477 0 None - 1 Mouse 6.7 pIC50 = 6.7 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 743 15 4 7 5.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44280028 98720 0 None - 1 Mouse 6.7 pIC50 = 6.7 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 768 17 6 9 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL281318 98720 0 None - 1 Mouse 6.7 pIC50 = 6.7 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 768 17 6 9 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44333341 107300 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 448 4 2 5 2.9 CCCN1C(=O)[C@@H](NC(=O)Nc2cccc(C)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
CHEMBL319180 107300 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 448 4 2 5 2.9 CCCN1C(=O)[C@@H](NC(=O)Nc2cccc(C)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
13809514 202404 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 5 2 4 2.5 CN1C(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL70259 202404 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 5 2 4 2.5 CN1C(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
121964 205 28 None - 2 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against cholecystokinin type A receptor from bovine striatal binding assayInhibitory activity against cholecystokinin type A receptor from bovine striatal binding assay
ChEMBL None None None None 10.1021/jm00100a033
858 205 28 None - 2 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against cholecystokinin type A receptor from bovine striatal binding assayInhibitory activity against cholecystokinin type A receptor from bovine striatal binding assay
ChEMBL None None None None 10.1021/jm00100a033
CHEMBL323521 205 28 None - 2 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against cholecystokinin type A receptor from bovine striatal binding assayInhibitory activity against cholecystokinin type A receptor from bovine striatal binding assay
ChEMBL None None None None 10.1021/jm00100a033
44334345 163302 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 504 8 2 4 4.0 Cc1cccc(NC(=O)N[C@H](CCC(=O)N2CCCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL420658 163302 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 504 8 2 4 4.0 Cc1cccc(NC(=O)N[C@H](CCC(=O)N2CCCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
367893 51344 1 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
CHEMBL158362 51344 1 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
44408526 136422 0 None -2344 4 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL374325 136422 0 None -2344 4 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
16100409 82821 0 None -870 3 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL218651 82821 0 None -870 3 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
44303251 101764 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 618 12 5 5 4.6 O=C(O)CCC(=O)N[C@@H](CNC(=O)C(Cc1c[nH]c2ccc(F)cc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL303020 101764 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 618 12 5 5 4.6 O=C(O)CCC(=O)N[C@@H](CNC(=O)C(Cc1c[nH]c2ccc(F)cc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1016/S0960-894X(97)00356-9
44349325 167983 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 465 7 3 4 3.1 O=C(O)CCC(NC(=O)c1cccc(Br)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL435587 167983 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 465 7 3 4 3.1 O=C(O)CCC(NC(=O)c1cccc(Br)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
9827037 78419 6 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 6 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H]1CCCC[C@@H]1O 10.1021/jm970065l
CHEMBL2112795 78419 6 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 6 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H]1CCCC[C@@H]1O 10.1021/jm970065l
CHEMBL379405 210518 0 None -11 4 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
1614 2317 60 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 10.1021/jm051050n
60182 2317 60 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 10.1021/jm051050n
892 2317 60 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 10.1021/jm051050n
CHEMBL206025 2317 60 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 10.1021/jm051050n
44368368 120564 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 481 8 3 3 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)NCCc1ccccc1 10.1021/jm00057a005
CHEMBL357027 120564 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 481 8 3 3 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)NCCc1ccccc1 10.1021/jm00057a005
10071178 74146 1 None 501 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm051050n
CHEMBL202861 74146 1 None 501 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm051050n
136060576 87064 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assay
ChEMBL 571 5 1 5 8.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(-c4ccccc4)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL233457 87064 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assay
ChEMBL 571 5 1 5 8.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(-c4ccccc4)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
10071178 74146 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL202861 74146 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10071178 74146 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL202861 74146 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
10071178 74146 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL202861 74146 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
44283081 99409 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 9 3 3 6.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(O)CCCc1ccccc1 10.1021/jm00086a017
CHEMBL2112071 99409 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 9 3 3 6.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(O)CCCc1ccccc1 10.1021/jm00086a017
CHEMBL285880 99409 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 9 3 3 6.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(O)CCCc1ccccc1 10.1021/jm00086a017
44327456 206107 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 585 11 2 5 5.7 COC(=O)CCN(CCc1ccccc1)C(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
CHEMBL96401 206107 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 585 11 2 5 5.7 COC(=O)CCN(CCc1ccccc1)C(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
44303652 199006 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 570 8 2 3 7.2 CC(Cc1ccc2c(c1)C(C)(C)CCC2(C)C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL59985 199006 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 570 8 2 3 7.2 CC(Cc1ccc2c(c1)C(C)(C)CCC2(C)C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
10530400 118830 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 535 7 3 5 5.0 COC(=O)C1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)CCCCC1 10.1021/jm970065l
CHEMBL344220 118830 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 535 7 3 5 5.0 COC(=O)C1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)CCCCC1 10.1021/jm970065l
14208235 102665 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 442 4 3 4 3.9 COc1ccc2[nH]c(C(=O)NC3N=C(c4ccccc4F)c4ccccc4NC3=O)cc2c1 10.1021/jm00047a021
CHEMBL307878 102665 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 442 4 3 4 3.9 COc1ccc2[nH]c(C(=O)NC3N=C(c4ccccc4F)c4ccccc4NC3=O)cc2c1 10.1021/jm00047a021
10746778 47296 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 646 8 2 6 5.2 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(N2CCOCC2)cc1 10.1021/jm950626d
CHEMBL154615 47296 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 646 8 2 6 5.2 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(N2CCOCC2)cc1 10.1021/jm950626d
14208201 202875 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 436 6 3 3 4.4 O=C(CCCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL73110 202875 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 436 6 3 3 4.4 O=C(CCCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
52942901 17953 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269261 17953 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
54583298 61594 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774042 61594 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
10079035 163309 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 796 21 8 7 2.9 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL420667 163309 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 796 21 8 7 2.9 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
5311201 205663 30 None -2570 6 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00164a020
CHEMBL9387 205663 30 None -2570 6 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00164a020
10476766 102526 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 412 3 3 3 3.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00047a021
CHEMBL306806 102526 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 412 3 3 3 3.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00047a021
15667016 85691 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 960 25 9 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL2310856 85691 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 960 25 9 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
10476766 102526 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 3 3 3 3.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00120a002
CHEMBL306806 102526 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 3 3 3 3.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00120a002
10008654 127094 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptorInhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127094 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptorInhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44348650 112607 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 986 24 11 11 2.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL331408 112607 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 986 24 11 11 2.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
10011110 160782 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 948 24 8 7 5.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL412544 160782 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 948 24 8 7 5.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44329343 111838 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 556 7 3 4 5.6 COc1ccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)cc1 10.1016/S0960-894X(01)80832-5
CHEMBL329286 111838 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 556 7 3 4 5.6 COc1ccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)cc1 10.1016/S0960-894X(01)80832-5
155546692 173070 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1861 72 19 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4534236 173070 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1861 72 19 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
10454890 154603 1 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL40211 154603 1 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
10454890 154603 1 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL40211 154603 1 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL106722 206730 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
24784941 189126 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 516 6 0 5 6.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515616 189126 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 516 6 0 5 6.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL263155 208815 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
54587150 61535 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773887 61535 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
54580266 61536 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 529 6 0 6 6.0 CCOc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773888 61536 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 529 6 0 6 6.0 CCOc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
14208241 67409 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907852 67409 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
24784940 182205 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479046 182205 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
14208269 77473 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 447 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL2092869 77473 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 447 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL2079549 207448 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(CC(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
155551968 173445 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1793 69 16 20 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4542927 173445 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1793 69 16 20 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44348901 141296 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1000 24 11 11 2.3 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)c1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL386376 141296 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1000 24 11 11 2.3 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)c1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
44344743 163021 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 555 11 4 3 5.3 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)CC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm000937a
CHEMBL420320 163021 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 555 11 4 3 5.3 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)CC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm000937a
904 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
9915756 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL2111204 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL356898 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
904 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
9915756 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
CHEMBL2111204 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
CHEMBL356898 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
44329486 112102 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3ccc(F)cc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL330197 112102 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3ccc(F)cc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
904 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
9915756 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
CHEMBL2111204 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
CHEMBL356898 2977 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
44398261 123867 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11103804 114955 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=S)C[C@@H]12 10.1021/jm010898i
CHEMBL3350855 114955 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=S)C[C@@H]12 10.1021/jm010898i
14208241 67409 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL1907852 67409 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
10320031 77472 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
CHEMBL2092868 77472 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
14208269 77473 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 447 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL2092869 77473 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 447 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
10973734 78025 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
CHEMBL2111549 78025 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
14991570 201127 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 943 22 9 11 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2cc(OS(=O)(=O)O)ccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL62345 201127 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 943 22 9 11 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2cc(OS(=O)(=O)O)ccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44382008 58741 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
CHEMBL169438 58741 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
13503154 99803 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL 363 9 4 6 0.1 CSCC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
CHEMBL288892 99803 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL 363 9 4 6 0.1 CSCC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
72707158 140221 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 265 3 1 2 2.5 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
CHEMBL3818215 140221 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 265 3 1 2 2.5 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
14208271 102422 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 3 1 3 4.4 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL305951 102422 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 3 1 3 4.4 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208214 164696 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc2ccccc2c1 10.1021/jm00120a002
CHEMBL422951 164696 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc2ccccc2c1 10.1021/jm00120a002
10074366 120087 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3349028 120087 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3545866 120087 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
46235271 73301 2 None 2 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL2017835 73301 2 None 2 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
14208249 202926 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 387 3 2 3 3.7 Cc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL73510 202926 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 387 3 2 3 3.7 Cc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
10603714 155977 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4c(F)cccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL406790 155977 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4c(F)cccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
367893 51344 1 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
CHEMBL158362 51344 1 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
13953692 101251 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 407 3 1 4 5.0 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nncn2-c2ccccc21 10.1021/jm00396a028
CHEMBL299538 101251 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 407 3 1 4 5.0 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nncn2-c2ccccc21 10.1021/jm00396a028
89913094 140250 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 251 2 1 2 2.2 CC(C)N1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
CHEMBL3818578 140250 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 251 2 1 2 2.2 CC(C)N1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
14208235 102665 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 442 4 3 4 3.9 COc1ccc2[nH]c(C(=O)NC3N=C(c4ccccc4F)c4ccccc4NC3=O)cc2c1 10.1021/jm00120a002
CHEMBL307878 102665 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 442 4 3 4 3.9 COc1ccc2[nH]c(C(=O)NC3N=C(c4ccccc4F)c4ccccc4NC3=O)cc2c1 10.1021/jm00120a002
11798691 57963 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 473 5 4 7 3.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(Nc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm9506736
CHEMBL168263 57963 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 473 5 4 7 3.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(Nc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm9506736
10962743 78187 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccc(N2C(=O)C[C@@H]3[C@@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
CHEMBL2112239 78187 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccc(N2C(=O)C[C@@H]3[C@@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
44370505 51005 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 543 10 2 4 6.3 O=C(CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1)OCc1ccccc1 10.1021/jm00164a020
CHEMBL158078 51005 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 543 10 2 4 6.3 O=C(CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1)OCc1ccccc1 10.1021/jm00164a020
10029582 26958 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 517 7 2 4 4.5 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136608 26958 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 517 7 2 4 4.5 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44356717 116280 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 513 5 3 5 4.7 CN1C(=O)C(NC(=O)Nc2cccc(CNC(=O)OC(C)(C)C)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL337722 116280 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 513 5 3 5 4.7 CN1C(=O)C(NC(=O)Nc2cccc(CNC(=O)OC(C)(C)C)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44578531 171994 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 570 6 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OCC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL448597 171994 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 570 6 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OCC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
44334332 108399 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 574 10 3 4 5.6 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(Cc2ccccc2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL321072 108399 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 574 10 3 4 5.6 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(Cc2ccccc2)CC1 10.1016/0960-894X(95)00537-3
44349028 116719 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 437 7 3 4 3.5 O=C(O)CCC(NC(=O)c1ccc2ccccc2c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL339453 116719 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 437 7 3 4 3.5 O=C(O)CCC(NC(=O)c1ccc2ccccc2c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
89913112 140271 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 257 1 1 2 2.1 CN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
CHEMBL3818822 140271 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 257 1 1 2 2.1 CN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
44280215 99369 0 None - 1 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 756 15 6 10 3.3 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL285586 99369 0 None - 1 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 756 15 6 10 3.3 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44334379 108286 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 435 7 2 3 4.7 Cc1cccc(NC(=O)N[C@H](CC(C)C)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL320901 108286 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 435 7 2 3 4.7 Cc1cccc(NC(=O)N[C@H](CC(C)C)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
19766161 58871 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 403 4 3 3 3.4 O=C(O)CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL170068 58871 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 403 4 3 3 3.4 O=C(O)CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
14208201 202875 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 436 6 3 3 4.4 O=C(CCCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL73110 202875 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 436 6 3 3 4.4 O=C(CCCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
44356972 27449 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 555 7 3 7 3.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)ON3CCC[C@@H]3C(=O)O)C2=O)c1 10.1021/jm00078a018
CHEMBL136990 27449 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 555 7 3 7 3.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)ON3CCC[C@@H]3C(=O)O)C2=O)c1 10.1021/jm00078a018
52945789 18100 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 541 7 0 5 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1270487 18100 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 541 7 0 5 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
2802894 2371 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1021/jm000937a
3509 2371 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1021/jm000937a
CHEMBL333081 2371 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1021/jm000937a
2802894 2371 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1016/S0960-894X(00)80684-8
3509 2371 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1016/S0960-894X(00)80684-8
CHEMBL333081 2371 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1016/S0960-894X(00)80684-8
45482487 196924 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 441 7 4 3 4.2 Cc1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)[nH]c2ccccc12 10.1016/j.bmc.2009.05.067
CHEMBL578652 196924 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 441 7 4 3 4.2 Cc1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)[nH]c2ccccc12 10.1016/j.bmc.2009.05.067
10768071 9741 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 512 6 3 5 4.3 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL113988 9741 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 512 6 3 5 4.3 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
44591977 178481 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 443 7 5 4 3.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccc(O)cc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL471464 178481 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 443 7 5 4 3.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccc(O)cc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
44349336 163962 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cccc(Cl)c1Cl)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL421474 163962 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cccc(Cl)c1Cl)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
10813333 104874 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 447 5 2 4 4.2 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCCCN2C)c2ccccc21 10.1021/jm9608523
CHEMBL311638 104874 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 447 5 2 4 4.2 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCCCN2C)c2ccccc21 10.1021/jm9608523
CHEMBL3142682 209381 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NC1CCCCC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
52940616 17955 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269263 17955 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
14208249 202926 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 387 3 2 3 3.7 Cc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL73510 202926 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 387 3 2 3 3.7 Cc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
9914964 9540 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 530 13 4 5 5.7 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(O)c2cccc(O)c2n1 10.1021/jm00116a002
CHEMBL112682 9540 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 530 13 4 5 5.7 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(O)c2cccc(O)c2n1 10.1021/jm00116a002
44293892 161138 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 613 6 2 5 5.8 CSc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL413267 161138 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 613 6 2 5 5.8 CSc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
14888709 76897 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1031 30 11 12 0.3 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(CC(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079603 76897 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1031 30 11 12 0.3 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(CC(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
71449099 78404 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 3 4 3.0 CN1C(=O)[C@H](NC(=O)NCc2cccc(O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2112751 78404 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 3 4 3.0 CN1C(=O)[C@H](NC(=O)NCc2cccc(O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991578 161166 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 824 21 8 9 2.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL413548 161166 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 824 21 8 9 2.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14208203 113964 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 425 3 2 3 4.3 CC1C(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)=Cc2ccccc21 10.1021/jm00047a021
CHEMBL333459 113964 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 425 3 2 3 4.3 CC1C(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)=Cc2ccccc21 10.1021/jm00047a021
14888706 76898 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1017 29 11 12 0.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(C(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079604 76898 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1017 29 11 12 0.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(C(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
10455302 27790 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 429 4 2 5 3.6 CN1C(=O)C(NC(=O)Nc2ccc([N+](=O)[O-])cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137240 27790 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 429 4 2 5 3.6 CN1C(=O)C(NC(=O)Nc2ccc([N+](=O)[O-])cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
19766170 58845 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 383 5 3 4 2.2 COc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)O)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL169931 58845 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 383 5 3 4 2.2 COc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)O)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL2370879 208196 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Compound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pigCompound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pig
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a068
44356697 25418 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 456 5 2 5 3.4 COC(=O)Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL135166 25418 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 456 5 2 5 3.4 COC(=O)Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
9870046 26143 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 486 5 3 6 3.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(Cc2nn[nH]n2)C1=O 10.1021/jm00078a018
CHEMBL135901 26143 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 486 5 3 6 3.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(Cc2nn[nH]n2)C1=O 10.1021/jm00078a018
10005779 116164 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 489 6 3 4 3.8 CCNC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL337065 116164 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 489 6 3 4 3.8 CCNC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44280214 106818 0 None - 1 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 770 16 6 10 3.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL31726 106818 0 None - 1 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 770 16 6 10 3.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL292097 209140 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Compound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranesCompound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(01)81005-2
5279366 103684 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 401 4 2 4 4.0 CSc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL309575 103684 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 401 4 2 4 4.0 CSc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
155564367 174584 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 72 18 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4570130 174584 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 72 18 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44303527 96042 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 632 12 5 5 5.0 CC(Cc1c[nH]c2ccc(F)cc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL262456 96042 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 632 12 5 5 5.0 CC(Cc1c[nH]c2ccc(F)cc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(97)00356-9
136794946 106130 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
15689731 106130 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142903 106130 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
136794946 106130 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
15689731 106130 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
CHEMBL3142903 106130 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
3960 2313 20 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1016/S0960-894X(00)80224-3
891 2313 20 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1016/S0960-894X(00)80224-3
CHEMBL24938 2313 20 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1016/S0960-894X(00)80224-3
44311642 202448 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 425 3 2 3 4.0 CC1(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)C=Cc2ccccc21 10.1021/jm00120a002
CHEMBL70549 202448 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 425 3 2 3 4.0 CC1(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)C=Cc2ccccc21 10.1021/jm00120a002
24784942 180761 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 488 4 1 5 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(O)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL476297 180761 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 488 4 1 5 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(O)c2)cc1 10.1016/j.bmcl.2008.06.057
90663975 106315 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1cccc(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144537 106315 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1cccc(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44303224 141403 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 933 23 8 11 2.8 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL387073 141403 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 933 23 8 11 2.8 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44348637 163958 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 966 27 11 11 1.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL421471 163958 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 966 27 11 11 1.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
52949124 863 2 None -2 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10507071 113111 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
CHEMBL332261 113111 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
44396744 123528 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 516 7 2 5 4.4 CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
CHEMBL363106 123528 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 516 7 2 5 4.4 CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
10626665 10164 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm010898i
CHEMBL116127 10164 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm010898i
10626665 10164 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm010813d
CHEMBL116127 10164 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm010813d
5311148 1865 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm960249k
865 1865 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm960249k
CHEMBL293226 1865 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm960249k
5311148 1865 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm970265x
865 1865 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm970265x
CHEMBL293226 1865 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm970265x
44300891 197873 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 586 7 4 6 5.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2CC1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL59234 197873 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 586 7 4 6 5.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2CC1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL3142698 209388 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None Cc1ccccc1/N=C(/S)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
10075014 162431 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 508 6 2 5 4.4 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
CHEMBL417521 162431 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 508 6 2 5 4.4 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
13822924 101474 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 427 4 1 6 4.2 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)OCc1ccccc1 10.1021/jm00396a028
CHEMBL301172 101474 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 427 4 1 6 4.2 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)OCc1ccccc1 10.1021/jm00396a028
5279366 103684 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 401 4 2 4 4.0 CSc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL309575 103684 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 401 4 2 4 4.0 CSc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
10078285 120993 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL358334 120993 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
10075014 162431 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 508 6 2 5 4.4 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00078a018
CHEMBL417521 162431 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 508 6 2 5 4.4 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00078a018
90663983 106330 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 891 21 8 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144552 106330 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 891 21 8 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
3960 2313 20 None - 1 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
891 2313 20 None - 1 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
CHEMBL24938 2313 20 None - 1 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
19766234 32120 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 427 4 1 3 5.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNc1cccc(C(F)(F)F)c1 10.1021/jm00163a069
CHEMBL141051 32120 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 427 4 1 3 5.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNc1cccc(C(F)(F)F)c1 10.1021/jm00163a069
10319892 58782 2 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL169661 58782 2 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44334250 4528 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 514 9 3 4 4.6 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCCC(C(=O)Nc3ccccc3)C2)c1 10.1016/0960-894X(95)00537-3
CHEMBL102703 4528 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 514 9 3 4 4.6 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCCC(C(=O)Nc3ccccc3)C2)c1 10.1016/0960-894X(95)00537-3
44334434 5022 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 483 8 2 3 5.2 Cc1cccc(NC(=O)N[C@H](CCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL105527 5022 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 483 8 2 3 5.2 Cc1cccc(NC(=O)N[C@H](CCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
13953696 101492 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 483 4 1 4 6.7 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1021/jm00396a028
CHEMBL301331 101492 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 483 4 1 4 6.7 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1021/jm00396a028
15104615 172180 0 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 545 13 2 4 6.1 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
CHEMBL450883 172180 0 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 545 13 2 4 6.1 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
15614749 32029 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 393 4 2 4 3.5 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccsc1 10.1021/jm00163a069
CHEMBL140984 32029 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 393 4 2 4 3.5 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccsc1 10.1021/jm00163a069
20063245 114843 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 417 5 2 4 3.9 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)OCc1ccccc1 10.1021/jm00163a069
CHEMBL334933 114843 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 417 5 2 4 3.9 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)OCc1ccccc1 10.1021/jm00163a069
44349011 116360 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 373 8 4 3 2.7 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00079a003
CHEMBL338134 116360 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 373 8 4 3 2.7 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00079a003
10555387 29880 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 589 10 3 3 7.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(Cc1ccccc1)Cc1ccccc1 10.1021/jm970065l
CHEMBL138952 29880 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 589 10 3 3 7.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(Cc1ccccc1)Cc1ccccc1 10.1021/jm970065l
10720107 204956 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 497 6 3 6 5.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(F)(F)F)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL8954 204956 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 497 6 3 6 5.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(F)(F)F)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
44361556 116221 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 571 4 2 5 4.3 CC(C)(C)OC(=O)N1Cc2[nH]c3ccccc3c2CC1C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
CHEMBL337362 116221 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 571 4 2 5 4.3 CC(C)(C)OC(=O)N1Cc2[nH]c3ccccc3c2CC1C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
10032956 167473 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
CHEMBL432258 167473 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
15689730 106114 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 854 21 9 8 4.4 CC(C)c1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142694 106114 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 854 21 9 8 4.4 CC(C)c1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL100609 206710 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None COc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL100609 206710 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None COc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
CHEMBL100609 206710 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None COc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
15667017 206435 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 974 28 10 11 1.7 CCCC[C@H](NC(=O)/C=C/c1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL98332 206435 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 974 28 10 11 1.7 CCCC[C@H](NC(=O)/C=C/c1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
15104594 10028 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL115656 10028 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL2370119 208040 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL None None None CSCC[C@H](NC(=O)C(Cc1cccc(CC(=O)O)c1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
52949124 863 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
9055 863 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
CHEMBL1269258 863 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
DB12694 863 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
CHEMBL3142687 209384 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
5311201 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00092a007
CHEMBL9387 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00092a007
5311201 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00105a062
CHEMBL9387 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00105a062
44382244 58883 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 618 11 4 4 6.4 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)Nc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL170129 58883 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 618 11 4 4 6.4 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)Nc1ccccc1 10.1016/S0960-894X(00)80687-3
367893 51344 1 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL158362 51344 1 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
5311201 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00057a005
CHEMBL9387 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00057a005
9828961 167423 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 548 6 4 4 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL431919 167423 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 548 6 4 4 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
10046475 115008 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3cccnc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL335241 115008 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3cccnc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
44349087 117945 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 420 7 3 3 3.8 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCC2CCCCC2C1 10.1021/jm00079a003
CHEMBL341143 117945 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 420 7 3 3 3.8 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCC2CCCCC2C1 10.1021/jm00079a003
15167776 67374 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 441 5 2 3 4.2 O=C(O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907728 67374 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 441 5 2 3 4.2 O=C(O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
15282007 167745 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 472 5 3 5 3.7 Cc1cccc(NC(=O)NC2N=C(c3c[nH]cn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL434126 167745 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 472 5 3 5 3.7 Cc1cccc(NC(=O)NC2N=C(c3c[nH]cn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
44336539 5075 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10838217 205603 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 473 7 3 8 3.7 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC)c2)c1 10.1021/jm970373j
CHEMBL9354 205603 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 473 7 3 8 3.7 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC)c2)c1 10.1021/jm970373j
44327420 111097 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 571 10 2 5 5.3 COC(=O)CN(CCc1ccccc1)C(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
CHEMBL328213 111097 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 571 10 2 5 5.3 COC(=O)CN(CCc1ccccc1)C(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
10438352 9706 0 None - 1 Rat 5.6 pIC50 = 5.6 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 588 8 3 6 3.9 COC(=O)[C@@]1(Cc2ccccc2)C[C@@H]2[C@@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1016/0960-894X(96)00160-6
CHEMBL113699 9706 0 None - 1 Rat 5.6 pIC50 = 5.6 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 588 8 3 6 3.9 COC(=O)[C@@]1(Cc2ccccc2)C[C@@H]2[C@@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1016/0960-894X(96)00160-6
44286821 167289 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 822 18 7 7 5.0 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1CC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL430937 167289 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 822 18 7 7 5.0 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1CC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
15104608 108340 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ncccc2c1 10.1021/jm00116a002
CHEMBL320976 108340 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ncccc2c1 10.1021/jm00116a002
14208260 101649 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.3 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00047a021
CHEMBL302359 101649 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.3 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00047a021
19754257 119871 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 340 3 3 2 4.3 O=C(Cc1c[nH]c2ccccc12)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
CHEMBL353304 119871 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 340 3 3 2 4.3 O=C(Cc1c[nH]c2ccccc12)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
52942901 17953 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269261 17953 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
44336539 5075 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
14208260 101649 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 423 3 2 3 4.3 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00120a002
CHEMBL302359 101649 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 423 3 2 3 4.3 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00120a002
10453004 25920 6 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 390 3 2 3 3.5 CN1C(=O)C(NC(=O)NC2CCCCC2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135618 25920 6 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 390 3 2 3 3.5 CN1C(=O)C(NC(=O)NC2CCCCC2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10482726 25936 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 551 7 3 4 5.0 O=C(CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21)NCc1ccccc1 10.1021/jm00078a018
CHEMBL135638 25936 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 551 7 3 4 5.0 O=C(CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21)NCc1ccccc1 10.1021/jm00078a018
44334704 4550 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 499 9 2 4 4.8 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL102862 4550 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 499 9 2 4 4.8 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
10552615 29100 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 477 6 3 3 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1 10.1021/jm970065l
CHEMBL138311 29100 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 477 6 3 3 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1 10.1021/jm970065l
44382805 58900 0 None - 0 Mouse 4.6 pIC50 = 4.6 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 536 9 3 5 3.4 CC(C)C[C@H](NC(=O)C(NC(=O)OC(C)(C)C)c1ccccc1)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
CHEMBL170197 58900 0 None - 0 Mouse 4.6 pIC50 = 4.6 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 536 9 3 5 3.4 CC(C)C[C@H](NC(=O)C(NC(=O)OC(C)(C)C)c1ccccc1)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
44359866 116038 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 557 9 3 7 3.3 CC(=O)NCSCC(NC(=O)OC(C)(C)C)C(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
CHEMBL336256 116038 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 557 9 3 7 3.3 CC(=O)NCSCC(NC(=O)OC(C)(C)C)C(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
10837829 98112 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 463 6 3 6 5.0 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(Cl)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL276627 98112 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 463 6 3 6 5.0 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(Cl)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
52946667 17956 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 580 7 1 5 6.3 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@H](c2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269264 17956 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 580 7 1 5 6.3 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@H](c2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
613843 202873 28 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 250 1 0 2 2.5 CN1C(=O)CN=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL73096 202873 28 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 250 1 0 2 2.5 CN1C(=O)CN=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL2372077 208438 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@H]1CNC(=O)CNC(=O)[C@H](CCCCNCc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2007.05.067
70685411 73290 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 606 6 1 5 6.8 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017824 73290 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 606 6 1 5 6.8 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
54581261 61534 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 529 6 0 6 6.0 CCOc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773886 61534 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 529 6 0 6 6.0 CCOc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
44348922 16065 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 992 25 11 11 1.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC1CCC[C@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL122438 16065 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 992 25 11 11 1.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC1CCC[C@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
903 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm000937a
9850711 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm000937a
CHEMBL138534 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm000937a
CHEMBL2111312 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm000937a
904 2977 7 None - 1 Rat 7.6 pIC50 = 7.6 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
9915756 2977 7 None - 1 Rat 7.6 pIC50 = 7.6 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL2111204 2977 7 None - 1 Rat 7.6 pIC50 = 7.6 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL356898 2977 7 None - 1 Rat 7.6 pIC50 = 7.6 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
903 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
9850711 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL138534 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL2111312 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
903 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
9850711 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
CHEMBL138534 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
CHEMBL2111312 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
903 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm970065l
9850711 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm970065l
CHEMBL138534 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm970065l
CHEMBL2111312 2975 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm970065l
11714635 72122 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
CHEMBL198902 72122 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
44300889 100294 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 532 6 4 6 3.8 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2C(C)C 10.1016/0960-894X(95)00327-P
CHEMBL292856 100294 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 532 6 4 6 3.8 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2C(C)C 10.1016/0960-894X(95)00327-P
10507109 108740 0 None - 2 Rat 6.6 pIC50 = 6.6 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
CHEMBL321761 108740 0 None - 2 Rat 6.6 pIC50 = 6.6 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
44381593 119966 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 854 23 9 10 3.3 CN(C(=O)[C@H](CC(=O)O)NNC[C@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL354171 119966 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 854 23 9 10 3.3 CN(C(=O)[C@H](CC(=O)O)NNC[C@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
14208309 67345 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 439 7 1 3 5.0 CCCCCc1ccc(C(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
CHEMBL1907664 67345 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 439 7 1 3 5.0 CCCCCc1ccc(C(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
44370393 119139 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 492 14 2 3 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCCC1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL346784 119139 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 492 14 2 3 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCCC1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
14991541 106325 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 843 22 8 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144546 106325 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 843 22 8 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
10369442 108060 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 521 7 3 5 3.6 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCCC2)C(=O)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL320154 108060 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 521 7 3 5 3.6 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCCC2)C(=O)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44367000 119191 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 494 6 2 4 5.1 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL347329 119191 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 494 6 2 4 5.1 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
89913427 140193 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 311 2 1 2 3.4 O=C1C=C(Cl)C(O)(c2ccc(Cl)cc2)N1C1CCCC1 10.1039/C6MD00052E
CHEMBL3817873 140193 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 311 2 1 2 3.4 O=C1C=C(Cl)C(O)(c2ccc(Cl)cc2)N1C1CCCC1 10.1039/C6MD00052E
89913617 140216 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 223 1 1 2 1.4 CN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
CHEMBL3818165 140216 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 223 1 1 2 1.4 CN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
71458029 78380 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL2112692 78380 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
15104620 110872 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 476 13 3 2 6.4 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccc(C)cc1 10.1021/jm00116a002
CHEMBL326979 110872 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 476 13 3 2 6.4 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccc(C)cc1 10.1021/jm00116a002
14802537 58774 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL169615 58774 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80685-X
10052234 67420 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)N[C@H]1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
CHEMBL1907927 67420 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)N[C@H]1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
44280115 106743 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 658 11 3 6 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL31671 106743 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 658 11 3 6 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44329519 107801 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 594 6 3 3 6.6 Cc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C(F)(F)F)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
CHEMBL319748 107801 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 594 6 3 3 6.6 Cc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C(F)(F)F)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
44334259 4405 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 435 8 2 3 4.8 CCCC[C@@H](NC(=O)Nc1cccc(C)c1)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL101803 4405 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 435 8 2 3 4.8 CCCC[C@@H](NC(=O)Nc1cccc(C)c1)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
13953694 188779 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 523 3 1 4 6.8 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nnc(C(Cl)(Cl)Cl)n2-c2ccccc21 10.1021/jm00396a028
CHEMBL51280 188779 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 523 3 1 4 6.8 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nnc(C(Cl)(Cl)Cl)n2-c2ccccc21 10.1021/jm00396a028
44368567 168170 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL437039 168170 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
44365359 120775 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL 546 12 3 5 4.5 COc1ccc(N(C(=O)CN(C(=O)[C@@H](CCC(=O)O)NC(=O)Nc2ccccc2)c2ccccc2)C(C)C)cc1 10.1016/S0960-894X(97)00062-0
CHEMBL357983 120775 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL 546 12 3 5 4.5 COc1ccc(N(C(=O)CN(C(=O)[C@@H](CCC(=O)O)NC(=O)Nc2ccccc2)c2ccccc2)C(C)C)cc1 10.1016/S0960-894X(97)00062-0
44283246 99500 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 527 8 2 4 6.8 O=C(NC(Cc1c[nH]c2ccccc12)C1CN=C(CCc2ccccc2)S1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL286442 99500 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 527 8 2 4 6.8 O=C(NC(Cc1c[nH]c2ccccc12)C1CN=C(CCc2ccccc2)S1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10722372 119076 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(C(=O)O)cc1 10.1021/jm950626d
CHEMBL346179 119076 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(C(=O)O)cc1 10.1021/jm950626d
CHEMBL1172251 206841 0 None -229 4 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
44327698 205740 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 572 10 2 6 4.7 COC(=O)CN(CCc1ccccn1)C(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
CHEMBL94298 205740 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 572 10 2 6 4.7 COC(=O)CN(CCc1ccccn1)C(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
44348869 16230 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 407 7 3 4 2.6 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)C1 10.1021/jm00079a003
CHEMBL123089 16230 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 407 7 3 4 2.6 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)C1 10.1021/jm00079a003
9850184 110382 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 538 6 2 6 4.6 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCC3)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
CHEMBL326102 110382 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 538 6 2 6 4.6 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCC3)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
11154528 196259 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 426 7 3 3 3.7 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)C1=Cc2ccccc2C1 10.1016/j.bmc.2009.05.067
CHEMBL573136 196259 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 426 7 3 3 3.7 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)C1=Cc2ccccc2C1 10.1016/j.bmc.2009.05.067
44349391 116549 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 422 9 3 3 4.2 CCC1(CC)CCC(NC(=O)C(CCC(=O)O)NC(=O)c2cccc(Cl)c2)CC1 10.1021/jm00079a003
CHEMBL339115 116549 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 422 9 3 3 4.2 CCC1(CC)CCC(NC(=O)C(CCC(=O)O)NC(=O)c2cccc(Cl)c2)CC1 10.1021/jm00079a003
10814373 205374 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 474 7 3 8 4.2 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc([N+](=O)[O-])c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9203 205374 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 474 7 3 8 4.2 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc([N+](=O)[O-])c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
11234811 196706 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 394 7 3 4 3.4 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cccs1 10.1016/j.bmc.2009.05.067
CHEMBL576731 196706 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 394 7 3 4 3.4 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cccs1 10.1016/j.bmc.2009.05.067
10005159 114909 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 475 5 3 4 5.4 CN1C(=O)C(NC(=O)Nc2cccc(Nc3ccccc3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL335017 114909 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 475 5 3 4 5.4 CN1C(=O)C(NC(=O)Nc2cccc(Nc3ccccc3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10550527 205645 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 429 6 3 6 4.2 CCOc1cccc(-n2c(NNC(=O)Nc3cccc(C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9377 205645 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 429 6 3 6 4.2 CCOc1cccc(-n2c(NNC(=O)Nc3cccc(C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
155517868 169644 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1893 76 19 24 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4445353 169644 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1893 76 19 24 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
10027443 116032 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 464 5 3 4 4.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(Cc3ncc[nH]3)C2=O)c1 10.1021/jm00078a018
CHEMBL336221 116032 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 464 5 3 4 4.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(Cc3ncc[nH]3)C2=O)c1 10.1021/jm00078a018
44283246 99500 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 527 8 2 4 6.8 O=C(NC(Cc1c[nH]c2ccccc12)C1CN=C(CCc2ccccc2)S1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL286442 99500 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 527 8 2 4 6.8 O=C(NC(Cc1c[nH]c2ccccc12)C1CN=C(CCc2ccccc2)S1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10649606 49349 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
15689733 106132 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 870 21 9 10 3.0 COC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm00113a023
CHEMBL3142905 106132 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 870 21 9 10 3.0 COC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm00113a023
CHEMBL319814 209477 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44373740 119387 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Compound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasCompound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 569 8 3 5 5.2 COC(=O)[C@@]1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
CHEMBL349079 119387 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Compound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasCompound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 569 8 3 5 5.2 COC(=O)[C@@]1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
10070678 120242 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
CHEMBL355092 120242 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
CHEMBL319814 209477 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
14888736 97635 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 974 29 10 11 1.2 CSCC[C@H](NC(=O)CCc1ccc(CC(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL273344 97635 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 974 29 10 11 1.2 CSCC[C@H](NC(=O)CCc1ccc(CC(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
10479056 25981 11 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 452 3 2 3 5.0 CN1C(=O)C(NC(=O)Nc2ccc(Cl)c(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135702 25981 11 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 452 3 2 3 5.0 CN1C(=O)C(NC(=O)Nc2ccc(Cl)c(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10070678 120242 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL355092 120242 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
44336539 5075 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
52949124 863 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
14519977 119444 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00124a003
CHEMBL349640 119444 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00124a003
44310001 202189 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 415 4 1 3 4.5 Cc1ccc(C(=O)NC[C@H]2CN=C(c3ccc(F)cc3)c3ccc(C)cc3N2C)cc1 10.1021/jm00163a069
CHEMBL68870 202189 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 415 4 1 3 4.5 Cc1ccc(C(=O)NC[C@H]2CN=C(c3ccc(F)cc3)c3ccc(C)cc3N2C)cc1 10.1021/jm00163a069
21842325 119617 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 495 6 2 5 4.5 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL351144 119617 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 495 6 2 5 4.5 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00557-A
135837528 119731 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 472 5 3 5 3.7 Cc1cccc(NC(=O)NC2N=C(c3ncc[nH]3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL352217 119731 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 472 5 3 5 3.7 Cc1cccc(NC(=O)NC2N=C(c3ncc[nH]3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL2372075 208436 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@H]1CNC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2007.05.067
10349938 162369 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 722 14 4 6 6.7 CC(Cc1c[nH]c2ccc(F)cc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)OCc1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL417412 162369 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 722 14 4 6 6.7 CC(Cc1c[nH]c2ccc(F)cc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)OCc1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00356-9
44287086 100023 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 782 18 7 7 4.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL290975 100023 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 782 18 7 7 4.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44368382 45084 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 511 9 4 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL152682 45084 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 511 9 4 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
10719721 205697 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 486 7 3 8 3.8 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N(C)C)c2)c1 10.1021/jm970373j
CHEMBL9406 205697 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 486 7 3 8 3.8 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N(C)C)c2)c1 10.1021/jm970373j
44368567 168170 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL437039 168170 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL2372076 208437 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@H]1CNC(=O)CCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2007.05.067
14208255 202962 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 416 4 2 4 3.4 CN(C)c1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL73745 202962 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 416 4 2 4 3.4 CN(C)c1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
52949124 863 2 None -2 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
44286816 160227 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 810 20 7 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL41142 160227 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 810 20 7 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44286695 160419 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 796 19 7 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL41157 160419 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 796 19 7 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44592082 178564 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 411 8 4 4 3.4 CSCC[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL472079 178564 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 411 8 4 4 3.4 CSCC[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
44300551 195719 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 390 3 2 3 4.1 Cc1cccc(NC(=O)NC2N=C(C3CCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
CHEMBL56944 195719 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 390 3 2 3 4.1 Cc1cccc(NC(=O)NC2N=C(C3CCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
46235271 73301 2 None 2 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
15689737 106117 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC/N=C(\S)Nc1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142701 106117 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC/N=C(\S)Nc1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL354363 209984 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
14208255 202962 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 416 4 2 4 3.4 CN(C)c1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL73745 202962 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 416 4 2 4 3.4 CN(C)c1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
443375 205872 40 None - 5 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00164a020
CHEMBL9506 205872 40 None - 5 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00164a020
9845465 118354 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 428 5 3 4 3.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCO)C2=O)c1 10.1021/jm00078a018
CHEMBL342201 118354 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 428 5 3 4 3.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCO)C2=O)c1 10.1021/jm00078a018
44303664 100242 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranesCompound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranes
ChEMBL 661 16 7 7 0.3 CCCC1C[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)N(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)CN)C1 10.1016/S0960-894X(01)81005-2
CHEMBL292493 100242 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranesCompound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranes
ChEMBL 661 16 7 7 0.3 CCCC1C[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)N(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)CN)C1 10.1016/S0960-894X(01)81005-2
CHEMBL3143186 209393 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Compound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pigCompound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pig
ChEMBL None None None CCC[C@@H]1CCN(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)[C@@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a068
73354293 106074 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 650 12 6 5 4.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCP(=O)(O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL314178 106074 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 650 12 6 5 4.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCP(=O)(O)O)c1ccccc1 10.1021/jm00092a007
44312041 103222 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 498 6 3 5 4.1 CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL308769 103222 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 498 6 3 5 4.1 CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
44382243 59210 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 632 12 4 4 6.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL171562 59210 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 632 12 4 4 6.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCc1ccccc1 10.1016/S0960-894X(00)80687-3
162666759 181738 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Inhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assayInhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assay
ChEMBL 846 23 9 9 2.9 CC(C)C[C@@H](/C=C/NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)NC(=O)OC(C)(C)C 10.1021/acs.jmedchem.0c00530
CHEMBL4784305 181738 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Inhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assayInhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assay
ChEMBL 846 23 9 9 2.9 CC(C)C[C@@H](/C=C/NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)NC(=O)OC(C)(C)C 10.1021/acs.jmedchem.0c00530
15673154 85568 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 2300 to 3500The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 2300 to 3500
ChEMBL 650 12 6 5 4.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCP(=O)(O)O)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304155 85568 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 2300 to 3500The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 2300 to 3500
ChEMBL 650 12 6 5 4.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCP(=O)(O)O)c1ccccc1 10.1016/S0960-894X(00)80652-6
14208263 203009 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 425 7 2 3 5.0 CCCCCc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL74170 203009 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 425 7 2 3 5.0 CCCCCc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
14720389 164531 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL422701 164531 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
44381609 128590 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 610 15 6 7 2.5 N#C[C@H](N[C@H](CC(=O)NC(Cc1ccccc1)C(N)=O)C(=O)O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
CHEMBL367057 128590 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 610 15 6 7 2.5 N#C[C@H](N[C@H](CC(=O)NC(Cc1ccccc1)C(N)=O)C(=O)O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
44349298 16450 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 429 8 3 4 3.5 CC(C)c1ccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)cc1 10.1021/jm00079a003
CHEMBL124155 16450 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 429 8 3 4 3.5 CC(C)c1ccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)cc1 10.1021/jm00079a003
44349101 16665 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 468 7 3 3 5.0 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NC1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL124805 16665 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 468 7 3 3 5.0 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NC1CCC2(CCCCC2)CC1 10.1021/jm00079a003
44592485 187243 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 379 6 4 3 3.3 CC(C)C(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL496066 187243 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 379 6 4 3 3.3 CC(C)C(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
42636922 178534 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 411 8 4 4 3.4 CSCC[C@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL471870 178534 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 411 8 4 4 3.4 CSCC[C@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
11799462 161467 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 497 6 3 6 5.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL415965 161467 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 497 6 3 6 5.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
10553146 116213 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 491 6 3 3 5.7 CC1CCCCC1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
CHEMBL337310 116213 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 491 6 3 3 5.7 CC1CCCCC1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
9821357 17097 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 382 9 3 3 3.2 CC(C)(C)CCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL125703 17097 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 382 9 3 3 3.2 CC(C)(C)CCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
45482486 196627 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 441 7 4 3 4.2 Cc1ccc2[nH]c(C(=O)Nc3ccccc3C(=O)NC(Cc3ccccc3)C(=O)O)cc2c1 10.1016/j.bmc.2009.05.067
CHEMBL576020 196627 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 441 7 4 3 4.2 Cc1ccc2[nH]c(C(=O)Nc3ccccc3C(=O)NC(Cc3ccccc3)C(=O)O)cc2c1 10.1016/j.bmc.2009.05.067
44382371 119995 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 436 5 2 4 2.8 COc1cccc(NC(=O)N[C@@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL354442 119995 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 436 5 2 4 2.8 COc1cccc(NC(=O)N[C@@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
14208216 102230 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 393 3 1 4 3.5 CN1C(=O)C(NC(=O)c2ccsc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL304768 102230 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 393 3 1 4 3.5 CN1C(=O)C(NC(=O)c2ccsc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
44286378 167552 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
In vitro binding for half maximal inhibition of [125I]- Bolton-Hunter-CCK-8 in guinea pig pancreasIn vitro binding for half maximal inhibition of [125I]- Bolton-Hunter-CCK-8 in guinea pig pancreas
ChEMBL 838 21 7 9 3.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1cccnc1)NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00037a006
CHEMBL432864 167552 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
In vitro binding for half maximal inhibition of [125I]- Bolton-Hunter-CCK-8 in guinea pig pancreasIn vitro binding for half maximal inhibition of [125I]- Bolton-Hunter-CCK-8 in guinea pig pancreas
ChEMBL 838 21 7 9 3.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1cccnc1)NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00037a006
14991586 100172 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 838 21 7 9 3.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1cccnc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL292071 100172 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 838 21 7 9 3.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1cccnc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
5279119 203045 1 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00047a021
CHEMBL74515 203045 1 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00047a021
5311201 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Concentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissueConcentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm020424z
CHEMBL9387 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Concentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissueConcentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm020424z
5311201 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00121a004
CHEMBL9387 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00121a004
5311201 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm000937a
CHEMBL9387 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm000937a
5311201 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL9387 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00609-9
5311201 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00164a020
CHEMBL9387 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00164a020
5311201 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(00)80684-8
CHEMBL9387 205663 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(00)80684-8
CHEMBL172135 207107 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44409521 139640 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 351 5 4 3 2.6 CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1021/jm051050n
CHEMBL380355 139640 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 351 5 4 3 2.6 CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1021/jm051050n
70697534 77494 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 367 3 2 3 4.4 O=C1Nc2ccccc2C(c2ccccc2)=NC1C[C@H]1CNc2ccccc21 10.1021/jm00390a019
CHEMBL2092989 77494 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 367 3 2 3 4.4 O=C1Nc2ccccc2C(c2ccccc2)=NC1C[C@H]1CNc2ccccc21 10.1021/jm00390a019
15167797 31441 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 5 2 4 4.4 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)OCc1ccccc1 10.1021/jm00163a069
CHEMBL140495 31441 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 5 2 4 4.4 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)OCc1ccccc1 10.1021/jm00163a069
44303233 100188 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 632 12 5 5 5.0 C[C@](Cc1c[nH]c2ccc(F)cc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL292194 100188 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 632 12 5 5 5.0 C[C@](Cc1c[nH]c2ccc(F)cc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(97)00356-9
9985099 116775 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2cc(Cl)ccc21 10.1021/jm00048a015
CHEMBL339515 116775 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2cc(Cl)ccc21 10.1021/jm00048a015
44592485 187243 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 379 6 4 3 3.3 CC(C)C(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL496066 187243 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 379 6 4 3 3.3 CC(C)C(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
10255357 18332 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.0 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1021/jm00048a015
CHEMBL127397 18332 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.0 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1021/jm00048a015
10074366 120087 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3349028 120087 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3545866 120087 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
44368567 168170 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL437039 168170 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
44349393 16655 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 422 7 3 3 4.3 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCCCCC1 10.1021/jm00079a003
CHEMBL124764 16655 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 422 7 3 3 4.3 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCCCCC1 10.1021/jm00079a003
44381550 164681 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 842 23 11 10 3.0 Cc1ccccc1NC(=O)NCCCC[C@@H](CNN[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)NNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL422919 164681 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 842 23 11 10 3.0 Cc1ccccc1NC(=O)NCCCC[C@@H](CNN[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)NNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
5279119 203045 1 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00120a002
CHEMBL74515 203045 1 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00120a002
15104606 9366 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 497 13 2 2 6.9 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ccccc2c1 10.1021/jm00116a002
CHEMBL111837 9366 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 497 13 2 2 6.9 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ccccc2c1 10.1021/jm00116a002
44309988 102195 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 415 4 1 3 4.5 Cc1ccc(C(=O)NC[C@@H]2CN=C(c3ccc(F)cc3)c3ccc(C)cc3N2C)cc1 10.1021/jm00163a069
CHEMBL304546 102195 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 415 4 1 3 4.5 Cc1ccc(C(=O)NC[C@@H]2CN=C(c3ccc(F)cc3)c3ccc(C)cc3N2C)cc1 10.1021/jm00163a069
10698905 205145 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4cc(F)ccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL90697 205145 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4cc(F)ccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10077842 108600 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 637 8 2 5 5.8 CN(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)c3ccccc3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
CHEMBL321321 108600 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 637 8 2 5 5.8 CN(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)c3ccccc3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
44458068 85335 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 374 4 2 3 2.7 O=C(N[C@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL22918 85335 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 374 4 2 3 2.7 O=C(N[C@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
10047669 78108 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2111924 78108 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991543 106323 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 22 8 8 3.5 Cc1ccc(CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
CHEMBL3144544 106323 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 22 8 8 3.5 Cc1ccc(CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
44334248 4612 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 528 8 3 5 4.9 Cc1cccc(NC(=O)N[C@H](COC(=O)Nc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL103312 4612 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 528 8 3 5 4.9 Cc1cccc(NC(=O)N[C@H](COC(=O)Nc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
20190195 30572 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 405 4 1 3 4.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1ccccc1F 10.1021/jm00163a069
CHEMBL139615 30572 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 405 4 1 3 4.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1ccccc1F 10.1021/jm00163a069
44356619 118291 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 415 4 2 5 3.1 COc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cn1 10.1021/jm00078a018
CHEMBL342142 118291 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 415 4 2 5 3.1 COc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cn1 10.1021/jm00078a018
11799359 28838 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 6 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H]1CCCC[C@H]1O 10.1021/jm970065l
CHEMBL138084 28838 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 6 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H]1CCCC[C@H]1O 10.1021/jm970065l
54580264 61529 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 514 5 0 5 6.2 COc1cccc(-c2ncc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773880 61529 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 514 5 0 5 6.2 COc1cccc(-c2ncc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
21842340 43840 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 508 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3(C)CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL151483 43840 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 508 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3(C)CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
45482489 196750 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccc(F)cc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL577161 196750 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccc(F)cc2[nH]1 10.1016/j.bmc.2009.05.067
135703408 142304 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Displacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assay
ChEMBL 511 4 2 6 6.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(O)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL389311 142304 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Displacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assay
ChEMBL 511 4 2 6 6.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(O)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
9936789 204863 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 529 7 3 8 5.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(=O)OC(C)(C)C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL8890 204863 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 529 7 3 8 5.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(=O)OC(C)(C)C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
9887120 202426 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00121a004
CHEMBL70380 202426 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00121a004
9887120 202426 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm000937a
CHEMBL70380 202426 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm000937a
14208237 202512 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 498 6 2 5 3.8 CCOC(=O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL70883 202512 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 498 6 2 5 3.8 CCOC(=O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10079315 167305 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 859 21 9 7 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL431065 167305 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 859 21 9 7 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL156559 207062 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
14888718 76899 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1041 29 11 14 -0.1 CSCC[C@H](NC(=O)[C@H](Cc1ccc(-c2nn[nH]n2)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079606 76899 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1041 29 11 14 -0.1 CSCC[C@H](NC(=O)[C@H](Cc1ccc(-c2nn[nH]n2)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
10253366 115845 11 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 452 3 2 3 5.0 CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL335951 115845 11 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 452 3 2 3 5.0 CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10094138 167767 6 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 429 4 2 5 3.6 CN1C(=O)C(NC(=O)Nc2ccccc2[N+](=O)[O-])N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL434255 167767 6 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 429 4 2 5 3.6 CN1C(=O)C(NC(=O)Nc2ccccc2[N+](=O)[O-])N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
9887120 202426 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(00)80684-8
CHEMBL70380 202426 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(00)80684-8
155540394 172367 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1820 69 17 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4516794 172367 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1820 69 17 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24785179 180954 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 502 6 0 5 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476520 180954 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 502 6 0 5 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2)c1 10.1016/j.bmcl.2008.06.057
14991585 100557 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 919 21 7 10 4.3 CC(=O)Oc1ccc2cc(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc3ccccc3)C(N)=O)ccc2c1 10.1021/jm00089a010
CHEMBL294542 100557 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 919 21 7 10 4.3 CC(=O)Oc1ccc2cc(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc3ccccc3)C(N)=O)ccc2c1 10.1021/jm00089a010
14208292 203014 1 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 465 3 1 3 4.2 CN1C(=O)C(NC(=O)c2cccc(Br)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL74228 203014 1 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 465 3 1 3 4.2 CN1C(=O)C(NC(=O)c2cccc(Br)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
14208293 67408 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 3 1 3 4.2 CN1C(=O)[C@@H](NC(=O)c2cccc(Br)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907851 67408 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 3 1 3 4.2 CN1C(=O)[C@@H](NC(=O)c2cccc(Br)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
15689729 106115 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 890 20 9 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1Br)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142695 106115 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 890 20 9 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1Br)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44386048 61188 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 541 9 4 4 5.3 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)/C(=C/c1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
CHEMBL177081 61188 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 541 9 4 4 5.3 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)/C(=C/c1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
CHEMBL156559 207062 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
44381480 59143 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 825 20 7 8 4.6 Cc1ccccc1NC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL171227 59143 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 825 20 7 8 4.6 Cc1ccccc1NC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL156559 207062 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL156559 207062 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL319340 209470 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL320868 209483 0 None - 2 Guinea pig 8.4 pIC50 = 8.4 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL320868 209483 0 None - 2 Guinea pig 8.4 pIC50 = 8.4 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
CHEMBL319340 209470 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
CHEMBL320868 209483 0 None - 2 Guinea pig 8.4 pIC50 = 8.4 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
44381695 120325 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 811 20 8 8 4.3 Cc1ccccc1NC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL355836 120325 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 811 20 8 8 4.3 Cc1ccccc1NC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL320868 209483 0 None - 2 Guinea pig 8.4 pIC50 = 8.4 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
44398261 123867 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptorInhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptor
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 123867 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptorInhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptor
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL319340 209470 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80687-3
14991584 161193 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 877 20 8 9 4.1 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)c1ccc2cc(O)ccc2c1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL413768 161193 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 877 20 8 9 4.1 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)c1ccc2cc(O)ccc2c1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
71452818 79304 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 541 9 4 4 5.3 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)C(=Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
CHEMBL2115543 79304 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 541 9 4 4 5.3 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)C(=Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
CHEMBL317477 209457 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None COC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
10074366 120087 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3349028 120087 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3545866 120087 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
11146119 78026 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1cccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)c1 10.1021/jm010813d
CHEMBL2111550 78026 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1cccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)c1 10.1021/jm010813d
44382038 119954 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 420 4 2 3 3.1 Cc1cccc(NC(=O)N[C@@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL354040 119954 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 420 4 2 3 3.1 Cc1cccc(NC(=O)N[C@@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
903 2975 6 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80273-5
9850711 2975 6 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80273-5
CHEMBL138534 2975 6 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80273-5
CHEMBL2111312 2975 6 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80273-5
178143 16673 2 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00079a003
CHEMBL124832 16673 2 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00079a003
44381915 58747 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 454 15 2 3 5.4 CCCCCN(CCCCC)C(=O)[C@@H](CCCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80681-2
CHEMBL169466 58747 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 454 15 2 3 5.4 CCCCCN(CCCCC)C(=O)[C@@H](CCCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80681-2
CHEMBL2079548 207447 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
24785430 181702 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 6 0 5 6.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(C)C)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL478397 181702 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 6 0 5 6.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(C)C)c2)cc1 10.1016/j.bmcl.2008.06.057
14991581 101964 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 855 22 8 9 3.2 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)CCc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL303994 101964 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 855 22 8 9 3.2 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)CCc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
90663985 106332 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 853 22 8 9 3.3 COc1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
CHEMBL3144554 106332 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 853 22 8 9 3.3 COc1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
44349268 16607 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 399 9 3 4 3.1 CC(C)(C)CCCNC(=O)C(CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00079a003
CHEMBL124509 16607 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 399 9 3 4 3.1 CC(C)(C)CCCNC(=O)C(CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00079a003
44381482 58764 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 827 22 10 9 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@H](CNN[C@@H](Cc1ccccc1)C(N)=O)CC(=O)O 10.1016/S0960-894X(00)80680-0
CHEMBL169567 58764 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 827 22 10 9 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@H](CNN[C@@H](Cc1ccccc1)C(N)=O)CC(=O)O 10.1016/S0960-894X(00)80680-0
13822916 189134 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 421 3 1 4 5.3 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00396a028
CHEMBL51569 189134 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 421 3 1 4 5.3 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00396a028
89913710 140290 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 285 2 1 2 2.9 CC(C)N1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
CHEMBL3819054 140290 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 285 2 1 2 2.9 CC(C)N1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
73349790 105695 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 725 14 5 6 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNS(=O)(=O)c1ccccc1)c1ccccc1 10.1021/jm00092a007
CHEMBL313756 105695 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 725 14 5 6 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNS(=O)(=O)c1ccccc1)c1ccccc1 10.1021/jm00092a007
14208205 202517 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 425 3 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ncc2ccccc2n1 10.1021/jm00120a002
CHEMBL70896 202517 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 425 3 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ncc2ccccc2n1 10.1021/jm00120a002
14208238 202432 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 394 5 3 3 4.1 O=C1Nc2ccccc2C(c2ccccc2)=NC1NCCc1c[nH]c2ccccc12 10.1021/jm00120a002
CHEMBL70405 202432 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 394 5 3 3 4.1 O=C1Nc2ccccc2C(c2ccccc2)=NC1NCCc1c[nH]c2ccccc12 10.1021/jm00120a002
10648445 58605 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 481 6 4 7 2.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(CNc3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
CHEMBL168903 58605 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 481 6 4 7 2.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(CNc3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
10695559 58728 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 467 5 4 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(Nc3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
CHEMBL169362 58728 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 467 5 4 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(Nc3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
10576729 58918 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 481 5 4 7 3.2 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1Nc1nn[nH]n1 10.1021/jm9506736
CHEMBL170275 58918 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 481 5 4 7 3.2 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1Nc1nn[nH]n1 10.1021/jm9506736
10814625 83054 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 481 5 3 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(N(C)c3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
CHEMBL22003 83054 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 481 5 3 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(N(C)c3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
10815094 119893 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 495 5 3 7 3.2 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1N(C)c1nn[nH]n1 10.1021/jm9506736
CHEMBL353509 119893 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 495 5 3 7 3.2 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1N(C)c1nn[nH]n1 10.1021/jm9506736
44356620 28449 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 400 3 3 5 2.6 CN1C(=O)C(NC(=O)Nc2ccc(N)nc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137748 28449 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 400 3 3 5 2.6 CN1C(=O)C(NC(=O)Nc2ccc(N)nc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10765241 103503 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 433 5 3 4 3.8 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCCCN2)c2ccccc21 10.1021/jm9608523
CHEMBL309299 103503 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 433 5 3 4 3.8 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCCCN2)c2ccccc21 10.1021/jm9608523
10717652 105677 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 433 5 3 4 3.8 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@@H]2CCCCN2)c2ccccc21 10.1021/jm9608523
CHEMBL313653 105677 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 433 5 3 4 3.8 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@@H]2CCCCN2)c2ccccc21 10.1021/jm9608523
CHEMBL44345 212174 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
15167802 67370 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 436 5 1 3 5.0 N#CCCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907720 67370 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 436 5 1 3 5.0 N#CCCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
15614820 67382 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 437 5 1 2 5.5 O=C1[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc2N1CC1CC1 10.1021/jm00390a019
CHEMBL1907737 67382 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 437 5 1 2 5.5 O=C1[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc2N1CC1CC1 10.1021/jm00390a019
15614818 67386 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 411 4 1 2 5.1 CCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907742 67386 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 411 4 1 2 5.1 CCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
44370505 51005 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 543 10 2 4 6.3 O=C(CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1)OCc1ccccc1 10.1021/jm00164a020
CHEMBL158078 51005 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 543 10 2 4 6.3 O=C(CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1)OCc1ccccc1 10.1021/jm00164a020
24039375 9794 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 540 8 2 6 4.9 CCN(CC)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL114277 9794 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 540 8 2 6 4.9 CCN(CC)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
10575687 205510 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 453 4 3 5 5.2 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2Cl)c1 10.1021/jm970373j
CHEMBL9287 205510 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 453 4 3 5 5.2 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2Cl)c1 10.1021/jm970373j
45482483 196520 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)N[C@@H](Cc1ccccc1)C(=O)O)c1cc2cc(F)ccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL575160 196520 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)N[C@@H](Cc1ccccc1)C(=O)O)c1cc2cc(F)ccc2[nH]1 10.1016/j.bmc.2009.05.067
14208205 202517 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 425 3 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ncc2ccccc2n1 10.1021/jm00047a021
CHEMBL70896 202517 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 425 3 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ncc2ccccc2n1 10.1021/jm00047a021
10649606 49349 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
9805700 118650 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 492 6 3 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCCCC1 10.1021/jm970065l
CHEMBL342932 118650 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 492 6 3 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCCCC1 10.1021/jm970065l
44381319 120213 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 495 11 4 5 3.6 N#C[C@H](N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
CHEMBL354817 120213 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 495 11 4 5 3.6 N#C[C@H](N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
10556460 205012 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 677 10 0 6 7.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(Cc4ccccc4)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
CHEMBL89953 205012 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 677 10 0 6 7.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(Cc4ccccc4)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
10556460 205012 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 677 10 0 6 7.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(Cc4ccccc4)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL89953 205012 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 677 10 0 6 7.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(Cc4ccccc4)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10344702 28418 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 471 7 2 5 3.6 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCN(C)C)C2=O)c1 10.1021/jm00078a018
CHEMBL137714 28418 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 471 7 2 5 3.6 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCN(C)C)C2=O)c1 10.1021/jm00078a018
10837729 105964 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 461 5 3 4 4.5 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
CHEMBL313983 105964 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 461 5 3 4 4.5 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
14519983 119471 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ncccc2c1 10.1021/jm00124a003
CHEMBL349857 119471 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ncccc2c1 10.1021/jm00124a003
44306360 157333 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2C)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL408395 157333 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2C)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL1172249 206840 0 None -5 4 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
52949124 863 2 None -2 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
9055 863 2 None -2 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
CHEMBL1269258 863 2 None -2 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
DB12694 863 2 None -2 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
44301034 101116 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 556 6 3 5 4.8 COC(=O)c1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccc(C)cc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00327-P
CHEMBL298627 101116 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 556 6 3 5 4.8 COC(=O)c1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccc(C)cc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00327-P
44336585 110193 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 641 7 2 6 5.7 CN(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C3(C(F)(F)F)N=N3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
CHEMBL325987 110193 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 641 7 2 6 5.7 CN(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C3(C(F)(F)F)N=N3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
10252890 25419 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 444 5 2 5 3.7 COc1cc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc(OC)c1 10.1021/jm00078a018
CHEMBL135167 25419 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 444 5 2 5 3.7 COc1cc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc(OC)c1 10.1021/jm00078a018
44356868 25771 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 412 3 2 3 4.3 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1C 10.1021/jm00078a018
CHEMBL135433 25771 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 412 3 2 3 4.3 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1C 10.1021/jm00078a018
10071645 27785 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 435 3 2 4 4.2 CN1C(=O)C(NC(=O)Nc2ccc3ncccc3c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137238 27785 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 435 3 2 4 4.2 CN1C(=O)C(NC(=O)Nc2ccc3ncccc3c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991534 106309 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 825 22 8 8 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144531 106309 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 825 22 8 8 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14991566 167670 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 831 22 8 8 3.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCC1CCCCC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL433636 167670 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 831 22 8 8 3.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCC1CCCCC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44280741 156021 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 759 15 4 8 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL406844 156021 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 759 15 4 8 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44312020 102732 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 398 5 3 4 2.5 N[C@H](Cc1ccccc1)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL308404 102732 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 398 5 3 4 2.5 N[C@H](Cc1ccccc1)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
71452652 78095 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL2111884 78095 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
14802539 76199 1 None - 1 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL2062144 76199 1 None - 1 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(01)80769-1
44382561 167743 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 662 13 5 5 5.8 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccc(O)cc1 10.1016/S0960-894X(00)80687-3
CHEMBL434113 167743 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 662 13 5 5 5.8 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccc(O)cc1 10.1016/S0960-894X(00)80687-3
14802538 96241 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL263969 96241 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80685-X
19756868 28205 1 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 409 3 2 4 3.5 CN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137520 28205 1 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 409 3 2 4 3.5 CN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10475990 115498 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
CHEMBL33554 115498 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
44379627 57824 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 520 7 2 5 4.9 CC(C)Oc1cccc(-n2c(CNC(=O)NCc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL167758 57824 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 520 7 2 5 4.9 CC(C)Oc1cccc(-n2c(CNC(=O)NCc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL432671 167532 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 784 15 7 12 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCNC(=O)CC(=O)NCCSCc3csc(C=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
14802538 96241 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm970065l
CHEMBL263969 96241 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm970065l
53465843 69067 0 None - 2 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933103 69067 0 None - 2 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
11178152 196670 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 439 7 3 4 3.9 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cnc2ccccc2c1 10.1016/j.bmc.2009.05.067
CHEMBL576380 196670 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 439 7 3 4 3.9 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cnc2ccccc2c1 10.1016/j.bmc.2009.05.067
44349152 18375 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 354 10 3 3 2.6 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)cc1 10.1021/jm00079a003
CHEMBL127604 18375 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 354 10 3 3 2.6 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)cc1 10.1021/jm00079a003
44381892 12170 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 510 9 2 4 3.7 CN(C)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1184772 12170 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 510 9 2 4 3.7 CN(C)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL368133 12170 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 510 9 2 4 3.7 CN(C)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL385727 210614 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N1CSC(C)(C)[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
10049168 196199 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cc(F)ccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL572648 196199 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cc(F)ccc2[nH]1 10.1016/j.bmc.2009.05.067
44592009 178326 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 397 6 3 2 4.8 CC(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL469974 178326 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 397 6 3 2 4.8 CC(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL206974 207438 0 None -72 5 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
10649606 49349 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
10744012 96930 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 501 8 3 8 4.5 CCOC(=O)c1ccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)cc1 10.1021/jm970373j
CHEMBL269662 96930 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 501 8 3 8 4.5 CCOC(=O)c1ccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)cc1 10.1021/jm970373j
CHEMBL407057 210888 0 None -1513 4 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O 10.1021/jm050921q
44365304 164200 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL 444 8 2 3 4.3 CC(C)N(C(=O)CN(C(=O)CNC(=O)Nc1ccccc1)c1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00062-0
CHEMBL421778 164200 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL 444 8 2 3 4.3 CC(C)N(C(=O)CN(C(=O)CNC(=O)Nc1ccccc1)c1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00062-0
53465781 69063 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 413 6 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(C(=O)O)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933099 69063 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 413 6 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(C(=O)O)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm200438b
10030027 17764 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)[C@@H](c1ccccc1)C[C@@H](NC(=O)Nc1cccc(Cl)c1)C(=O)N2CC(=O)NC(C)(C)C 10.1021/jm00048a015
CHEMBL126002 17764 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)[C@@H](c1ccccc1)C[C@@H](NC(=O)Nc1cccc(Cl)c1)C(=O)N2CC(=O)NC(C)(C)C 10.1021/jm00048a015
CHEMBL2372072 208434 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CN)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](CCC(=O)O)N(CCN(CCC(=O)O)CCC(=O)O)CCN(CCC(=O)O)CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmc.2007.05.067
14208247 202945 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 5 2 4 3.5 O=C(O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL73621 202945 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 5 2 4 3.5 O=C(O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10323690 100032 0 None - 2 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00086a017
CHEMBL2114401 100032 0 None - 2 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00086a017
CHEMBL291033 100032 0 None - 2 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00086a017
10674587 78431 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 570 8 3 6 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)[C@@H](C#N)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
CHEMBL2112825 78431 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 570 8 3 6 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)[C@@H](C#N)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
44301016 157433 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 673 7 4 6 4.5 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)C(F)(F)F)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL408490 157433 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 673 7 4 6 4.5 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)C(F)(F)F)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
14519979 9439 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cccc2ccccc12 10.1021/jm00124a003
CHEMBL112215 9439 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cccc2ccccc12 10.1021/jm00124a003
10099144 114043 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccc(Cl)cc21 10.1021/jm00048a015
CHEMBL333671 114043 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccc(Cl)cc21 10.1021/jm00048a015
14519979 9439 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cccc2ccccc12 10.1021/jm00116a002
CHEMBL112215 9439 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cccc2ccccc12 10.1021/jm00116a002
21467078 4359 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 448 4 2 5 2.9 CCCN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
CHEMBL101528 4359 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 448 4 2 5 2.9 CCCN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
44210428 58802 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 485 4 2 4 3.1 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3cccc4ccccc34)CCc3ccccc32)CC1 10.1016/S0960-894X(00)80683-6
CHEMBL169794 58802 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 485 4 2 4 3.1 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3cccc4ccccc34)CCc3ccccc32)CC1 10.1016/S0960-894X(00)80683-6
14519977 119444 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00124a003
CHEMBL349640 119444 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00124a003
10601173 30978 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 491 6 3 3 5.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCCC1 10.1021/jm970065l
CHEMBL140073 30978 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 491 6 3 3 5.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCCC1 10.1021/jm970065l
10372508 98109 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 694 13 6 6 4.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(01)00630-8
CHEMBL276613 98109 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 694 13 6 6 4.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(01)00630-8
44409521 139640 4 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 351 5 4 3 2.6 CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL380355 139640 4 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 351 5 4 3 2.6 CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
44349383 16588 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 480 9 3 3 4.7 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
CHEMBL124396 16588 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 480 9 3 3 4.7 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
54587149 61531 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 514 5 0 5 6.2 COc1cccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773883 61531 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 514 5 0 5 6.2 COc1cccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
90663982 106329 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 855 21 10 10 2.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)c(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144551 106329 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 855 21 10 10 2.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)c(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14991572 162630 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 848 20 8 9 3.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cnc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL418123 162630 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 848 20 8 9 3.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cnc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
10649606 49349 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
57393204 67347 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 431 5 1 4 3.3 COc1cccc(CC(=O)N[C@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)c1 10.1021/jm00120a002
CHEMBL1907666 67347 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 431 5 1 4 3.3 COc1cccc(CC(=O)N[C@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)c1 10.1021/jm00120a002
44280029 95994 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 740 15 6 9 3.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL262125 95994 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 740 15 6 9 3.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44279810 103367 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 757 16 4 7 5.7 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL30917 103367 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 757 16 4 7 5.7 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44209154 58785 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 315 4 2 2 4.2 O=C(CCc1ccccc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
CHEMBL169675 58785 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 315 4 2 2 4.2 O=C(CCc1ccccc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
15167795 73730 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 344 2 0 3 4.6 CN1C(=O)/C(=C\c2ccsc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
CHEMBL20223 73730 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 344 2 0 3 4.6 CN1C(=O)/C(=C\c2ccsc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
44336539 5075 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
44349082 17593 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 446 9 3 3 4.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
CHEMBL125874 17593 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 446 9 3 3 4.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
44359614 31652 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 491 8 3 4 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)CNC1CCCCC1 10.1021/jm970065l
CHEMBL140701 31652 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 491 8 3 4 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)CNC1CCCCC1 10.1021/jm970065l
44382327 59045 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 436 5 2 4 2.8 COc1cccc(NC(=O)N[C@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL170777 59045 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 436 5 2 4 2.8 COc1cccc(NC(=O)N[C@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
44327450 167638 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 558 10 3 5 4.6 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccn1)CC(=O)O 10.1016/S0960-894X(01)80769-1
CHEMBL433384 167638 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 558 10 3 5 4.6 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccn1)CC(=O)O 10.1016/S0960-894X(01)80769-1
14208250 167487 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL432334 167487 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
11327818 196427 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 428 7 4 4 3.2 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1nc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL574488 196427 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 428 7 4 4 3.2 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1nc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
44300890 101420 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 580 7 4 6 4.3 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2Cc1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL300776 101420 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 580 7 4 6 4.3 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2Cc1ccccc1 10.1016/0960-894X(95)00327-P
15689732 106133 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 870 21 9 10 3.0 COC(=O)c1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142906 106133 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 870 21 9 10 3.0 COC(=O)c1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
15689732 106133 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 870 21 9 10 3.0 COC(=O)c1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
CHEMBL3142906 106133 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 870 21 9 10 3.0 COC(=O)c1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
44349572 114561 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 533 5 2 4 6.0 Cc1ccc2c(c1)N(CC(=O)OC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL334305 114561 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 533 5 2 4 6.0 Cc1ccc2c(c1)N(CC(=O)OC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
10455303 114721 6 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 429 4 2 5 3.6 CN1C(=O)C(NC(=O)Nc2cccc([N+](=O)[O-])c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL334592 114721 6 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 429 4 2 5 3.6 CN1C(=O)C(NC(=O)Nc2cccc([N+](=O)[O-])c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10604135 78429 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 637 8 3 5 5.1 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12)OC1C2CC3CC(C2)CC1C3 10.1021/jm991078x
CHEMBL2112823 78429 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 637 8 3 5 5.1 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12)OC1C2CC3CC(C2)CC1C3 10.1021/jm991078x
70693814 73296 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccncc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017830 73296 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccncc1 10.1016/j.bmcl.2012.02.049
44311939 202790 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 530 6 2 5 4.2 CN1C(=O)C(NC(=O)[C@H](Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL72526 202790 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 530 6 2 5 4.2 CN1C(=O)C(NC(=O)[C@H](Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
44396765 67038 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 594 8 2 5 5.4 O=C(OC1C2CC3CC(C2)CC1C3)[C@H](Cc1c[nH]c2ccccc12)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
CHEMBL188667 67038 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 594 8 2 5 5.4 O=C(OC1C2CC3CC(C2)CC1C3)[C@H](Cc1c[nH]c2ccccc12)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
10074702 27407 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 500 8 2 6 4.0 CCOC(=O)CCN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136966 27407 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 500 8 2 6 4.0 CCOC(=O)CCN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44279809 98510 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 785 18 4 7 6.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL279778 98510 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 785 18 4 7 6.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
14208317 67348 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907667 67348 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208250 167487 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL432334 167487 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
9865694 202475 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin receptor
ChEMBL 399 3 2 2 5.2 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00120a002
CHEMBL70728 202475 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin receptor
ChEMBL 399 3 2 2 5.2 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00120a002
44280122 99039 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreas
ChEMBL 640 10 3 4 5.7 CN(C(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)[C@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm950372w
CHEMBL283276 99039 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreas
ChEMBL 640 10 3 4 5.7 CN(C(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)[C@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm950372w
44370497 164641 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 453 8 3 3 4.6 O=C(O)CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1 10.1021/jm00164a020
CHEMBL422873 164641 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 453 8 3 3 4.6 O=C(O)CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1 10.1021/jm00164a020
44334325 167411 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 485 9 2 3 5.2 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(Cc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL431812 167411 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 485 9 2 3 5.2 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(Cc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
1043 1552 13 None - 28 Mouse 4.5 pIC50 = 4.5 Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/S0960-894X(00)80644-7
149 1552 13 None - 28 Mouse 4.5 pIC50 = 4.5 Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/S0960-894X(00)80644-7
8223 1552 13 None - 28 Mouse 4.5 pIC50 = 4.5 Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/S0960-894X(00)80644-7
CHEMBL442 1552 13 None - 28 Mouse 4.5 pIC50 = 4.5 Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/S0960-894X(00)80644-7
DB00696 1552 13 None - 28 Mouse 4.5 pIC50 = 4.5 Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/S0960-894X(00)80644-7
15167794 98442 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 344 2 0 3 4.6 CN1C(=O)/C(=C/c2ccsc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
CHEMBL279237 98442 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 344 2 0 3 4.6 CN1C(=O)/C(=C/c2ccsc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
10649303 205723 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 507 6 3 6 5.1 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9422 205723 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 507 6 3 6 5.1 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
10625474 29013 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 508 8 3 5 4.2 COC[C@H]1CCCN1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
CHEMBL138233 29013 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 508 8 3 5 4.2 COC[C@H]1CCCN1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
44381610 119983 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 610 15 6 7 2.5 N#C[C@@H](N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
CHEMBL354359 119983 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 610 15 6 7 2.5 N#C[C@@H](N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
10791546 205354 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 501 8 3 8 4.5 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
CHEMBL9188 205354 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 501 8 3 8 4.5 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
46235271 73301 2 None 2 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
54581260 61530 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 513 5 0 4 6.8 COc1cccc(-c2ccc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773882 61530 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 513 5 0 4 6.8 COc1cccc(-c2ccc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
54586147 61533 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773885 61533 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
54580267 61543 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 535 5 0 6 6.0 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2Cl)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773895 61543 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 535 5 0 6 6.0 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2Cl)cc1 10.1016/j.bmcl.2011.03.069
14888738 97902 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 984 28 10 13 0.8 CSCC[C@H](NC(=O)CCc1ccc(-c2nn[nH]n2)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL275167 97902 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 984 28 10 13 0.8 CSCC[C@H](NC(=O)CCc1ccc(-c2nn[nH]n2)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44578611 189066 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2cccc(F)c2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515160 189066 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2cccc(F)c2)c1 10.1016/j.bmcl.2008.06.057
19766169 165014 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 443 4 2 4 4.2 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL424211 165014 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 443 4 2 4 4.2 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
44336509 106869 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL317668 106869 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/s0960-894x(98)00548-4
9980735 177871 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 441 7 3 4 3.9 Cn1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)cc2ccccc21 10.1016/j.bmc.2009.05.067
CHEMBL466135 177871 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 441 7 3 4 3.9 Cn1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)cc2ccccc21 10.1016/j.bmc.2009.05.067
15104626 110128 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 448 7 3 3 4.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL325662 110128 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 448 7 3 3 4.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1)c1cnc2ccccc2c1 10.1021/jm00116a002
3081191 9457 9 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00124a003
CHEMBL112307 9457 9 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00124a003
44272229 98291 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 635 15 6 6 3.5 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NCCc1ccccc1 10.1016/S0960-894X(00)80644-7
CHEMBL278032 98291 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 635 15 6 6 3.5 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NCCc1ccccc1 10.1016/S0960-894X(00)80644-7
44272229 98291 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 635 15 6 6 3.5 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NCCc1ccccc1 10.1016/S0960-894X(01)80253-5
CHEMBL278032 98291 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 635 15 6 6 3.5 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NCCc1ccccc1 10.1016/S0960-894X(01)80253-5
19754254 119844 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 321 2 2 2 4.6 O=C(Nc1cc2c3ccccc3nc-2c[nH]1)c1ccc(Cl)cc1 10.1016/S0960-894X(00)80682-4
CHEMBL353088 119844 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 321 2 2 2 4.6 O=C(Nc1cc2c3ccccc3nc-2c[nH]1)c1ccc(Cl)cc1 10.1016/S0960-894X(00)80682-4
44349102 167766 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 434 7 3 3 4.3 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL434250 167766 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 434 7 3 3 4.3 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCC2(CCCCC2)CC1 10.1021/jm00079a003
10817407 106647 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 601 7 1 6 5.6 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc2c(c1)OCO2 10.1021/jm970265x
CHEMBL316106 106647 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 601 7 1 6 5.6 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc2c(c1)OCO2 10.1021/jm970265x
10767360 204130 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 489 5 2 4 5.2 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCC(C)(C)CCN2C)c2ccccc21 10.1021/jm9608523
CHEMBL83591 204130 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 489 5 2 4 5.2 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCC(C)(C)CCN2C)c2ccccc21 10.1021/jm9608523
44408590 161177 0 None - 2 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL413644 161177 0 None - 2 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
44418923 161236 0 None - 2 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL414087 161236 0 None - 2 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
45482480 196198 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 472 8 4 5 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cc([N+](=O)[O-])ccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL572647 196198 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 472 8 4 5 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cc([N+](=O)[O-])ccc2[nH]1 10.1016/j.bmc.2009.05.067
45482477 196402 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)N[C@@H](Cc1ccccc1)C(=O)O)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL574292 196402 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)N[C@@H](Cc1ccccc1)C(=O)O)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
44211352 13872 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1196916 13872 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL558614 13872 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
10671800 205016 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 463 6 3 6 5.0 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccc(Cl)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL8997 205016 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 463 6 3 6 5.0 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccc(Cl)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
70691750 73299 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 621 7 1 6 6.1 O=C1[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017833 73299 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 621 7 1 6 6.1 O=C1[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
44336539 5075 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10555363 96040 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 588 9 1 4 6.6 CCC1(CC(=O)Nc2ccccc2)C(=O)N(CC(=O)N(c2ccccc2)C(C)C)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm960205b
CHEMBL262444 96040 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 588 9 1 4 6.6 CCC1(CC(=O)Nc2ccccc2)C(=O)N(CC(=O)N(c2ccccc2)C(C)C)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm960205b
155553502 173603 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 72 19 22 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OP(=O)(O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4547294 173603 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 72 19 22 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OP(=O)(O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44303511 159213 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranesCompound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranes
ChEMBL 750 18 4 10 5.7 CCCC[C@@H](C(=O)N[C@@H](CC(=O)OCc1ccccc1)[C@@H](Cc1ccccc1)C(N)=O)n1nnnc1[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(01)81005-2
CHEMBL410511 159213 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranesCompound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranes
ChEMBL 750 18 4 10 5.7 CCCC[C@@H](C(=O)N[C@@H](CC(=O)OCc1ccccc1)[C@@H](Cc1ccccc1)C(N)=O)n1nnnc1[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(01)81005-2
70695922 73248 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 558 6 1 5 5.9 CCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017691 73248 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 558 6 1 5 5.9 CCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
44458101 167583 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 363 4 3 3 2.0 O=C(N[C@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1cc2ccccc2[nH]1 10.1016/S0960-894X(00)80224-3
CHEMBL433032 167583 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 363 4 3 3 2.0 O=C(N[C@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1cc2ccccc2[nH]1 10.1016/S0960-894X(00)80224-3
72947518 140266 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 277 2 1 2 2.7 O=C1C=C(Cl)C(O)(c2ccccc2)N1C1CCCC1 10.1039/C6MD00052E
CHEMBL3818781 140266 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 277 2 1 2 2.7 O=C1C=C(Cl)C(O)(c2ccccc2)N1C1CCCC1 10.1039/C6MD00052E
44348764 168067 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 980 28 11 11 1.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL436199 168067 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 980 28 11 11 1.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL435339 211917 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1C[C@@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
89913059 140192 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 327 6 1 2 4.0 CCCCCCN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
CHEMBL3817870 140192 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 327 6 1 2 4.0 CCCCCCN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
14208261 103212 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 397 5 2 3 4.2 CCCc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL308756 103212 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 397 5 2 3 4.2 CCCc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
44280371 102554 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 815 19 4 8 6.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL30701 102554 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 815 19 4 8 6.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44281020 116144 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 6.2 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL33698 116144 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 6.2 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
13822910 67422 0 None - 0 Guinea pig 4.4 pIC50 = 4.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 383 3 2 2 4.7 O=C1Nc2ccccc2C(c2ccccc2F)=N[C@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
CHEMBL1907930 67422 0 None - 0 Guinea pig 4.4 pIC50 = 4.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 383 3 2 2 4.7 O=C1Nc2ccccc2C(c2ccccc2F)=N[C@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
44303488 100590 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 501 8 2 6 4.1 CC(Cn1nnc2ccccc21)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL294735 100590 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 501 8 2 6 4.1 CC(Cn1nnc2ccccc21)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
10369806 116320 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@@H](NC(=O)Nc1cccc(Cl)c1)C[C@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL337937 116320 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@@H](NC(=O)Nc1cccc(Cl)c1)C[C@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL218763 207654 0 None -3630 4 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
44303722 100382 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Compound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranesCompound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranes
ChEMBL 807 20 5 11 4.8 CCCC[C@@H](C(=O)N[C@@H](CC(=O)OCc1ccccc1)[C@@H](Cc1ccccc1)C(N)=O)n1nnnc1[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)OC(C)(C)C 10.1016/S0960-894X(01)81005-2
CHEMBL293456 100382 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Compound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranesCompound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranes
ChEMBL 807 20 5 11 4.8 CCCC[C@@H](C(=O)N[C@@H](CC(=O)OCc1ccccc1)[C@@H](Cc1ccccc1)C(N)=O)n1nnnc1[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)OC(C)(C)C 10.1016/S0960-894X(01)81005-2
11756709 22674 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 528 9 3 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)CCC(=O)O)C2=O)c1 10.1021/jm00078a018
CHEMBL132875 22674 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 528 9 3 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)CCC(=O)O)C2=O)c1 10.1021/jm00078a018
52949124 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10435698 140876 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL38404 140876 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80683-6
44300745 196674 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 562 6 3 5 5.3 COC(=O)c1cccc(NC(=O)N[C@@H]2C[C@H](C3CCCCC3)c3ccc(C)cc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00327-P
CHEMBL57643 196674 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 562 6 3 5 5.3 COC(=O)c1cccc(NC(=O)N[C@@H]2C[C@H](C3CCCCC3)c3ccc(C)cc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00327-P
10435698 140876 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
CHEMBL38404 140876 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
15104597 110061 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 481 13 2 2 6.4 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
CHEMBL325220 110061 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 481 13 2 2 6.4 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
11028229 114956 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 8 3 5 4.6 CO[C@@H]1C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C(=O)N1Cc1ccccc1 10.1021/jm010898i
CHEMBL3350856 114956 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 8 3 5 4.6 CO[C@@H]1C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C(=O)N1Cc1ccccc1 10.1021/jm010898i
10435698 140876 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL38404 140876 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14720390 49125 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL156415 49125 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
70695933 73289 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 607 7 1 6 5.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
CHEMBL2017823 73289 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 607 7 1 6 5.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
10413618 201103 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL62205 201103 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(01)80769-1
10323690 100032 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00057a005
CHEMBL2114401 100032 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00057a005
CHEMBL291033 100032 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00057a005
11224455 196596 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 440 7 3 3 4.1 CC1=C(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)Cc2ccccc21 10.1016/j.bmc.2009.05.067
CHEMBL575814 196596 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 440 7 3 3 4.1 CC1=C(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)Cc2ccccc21 10.1016/j.bmc.2009.05.067
44376132 119741 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 494 6 3 6 3.9 CC(C)CN1C(=O)[C@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL352264 119741 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 494 6 3 6 3.9 CC(C)CN1C(=O)[C@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
90663978 106321 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 883 23 8 10 3.3 COc1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c(OC)c1 10.1021/jm00089a010
CHEMBL3144542 106321 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 883 23 8 10 3.3 COc1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c(OC)c1 10.1021/jm00089a010
70695934 73297 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 595 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017831 73297 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 595 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
44283029 99592 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 627 11 3 7 5.2 COC(=O)/C=C/C(=O)N[C@H](COC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)c1ccccc1 10.1021/jm00086a017
CHEMBL287079 99592 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 627 11 3 7 5.2 COC(=O)/C=C/C(=O)N[C@H](COC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)c1ccccc1 10.1021/jm00086a017
10793883 106646 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 615 8 0 6 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL316104 106646 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 615 8 0 6 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10323690 100032 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
CHEMBL2114401 100032 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
CHEMBL291033 100032 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
14888722 76895 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1055 30 11 14 -0.2 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(Cc2nnn[nH]2)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079601 76895 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1055 30 11 14 -0.2 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(Cc2nnn[nH]2)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44280495 98669 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 641 10 5 8 3.7 CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL280980 98669 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 641 10 5 8 3.7 CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
10413618 201103 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1021/jm970065l
CHEMBL62205 201103 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1021/jm970065l
44349074 116535 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 426 7 4 4 2.8 O=C(O)CCC(NC(=O)c1cc2ccccc2[nH]1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL339041 116535 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 426 7 4 4 2.8 O=C(O)CCC(NC(=O)c1cc2ccccc2[nH]1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44333305 4982 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 502 4 2 5 3.6 CCCN1C(=O)C(NC(=O)Nc2cccc(C(F)(F)F)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
CHEMBL105273 4982 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 502 4 2 5 3.6 CCCN1C(=O)C(NC(=O)Nc2cccc(C(F)(F)F)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
10430103 78105 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 384 3 3 3 3.9 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3NC2=O)c1 10.1021/jm00078a018
CHEMBL2111921 78105 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 384 3 3 3 3.9 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3NC2=O)c1 10.1021/jm00078a018
44281004 99617 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 15 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
CHEMBL287295 99617 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 15 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
10838382 118826 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 478 6 3 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCCC1 10.1021/jm970065l
CHEMBL344211 118826 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 478 6 3 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCCC1 10.1021/jm970065l
71449051 78076 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CC[C@H](NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL2111827 78076 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CC[C@H](NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44381819 58307 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
CHEMBL168435 58307 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
10322621 57254 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 473 7 2 7 4.4 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc([N+](=O)[O-])cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL166443 57254 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 473 7 2 7 4.4 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc([N+](=O)[O-])cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
15514018 78186 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 546 6 3 6 3.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(c3ccncc3)C(=O)C[C@H]12 10.1021/jm010813d
CHEMBL2112238 78186 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 546 6 3 6 3.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(c3ccncc3)C(=O)C[C@H]12 10.1021/jm010813d
10580108 5042 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 650 10 1 4 7.4 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)(Cc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
CHEMBL105619 5042 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 650 10 1 4 7.4 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)(Cc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
14991574 100236 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 836 20 9 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL292471 100236 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 836 20 9 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
90663996 106342 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 919 23 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1cccc(OS(=O)(=O)O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144565 106342 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 919 23 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1cccc(OS(=O)(=O)O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
10415786 169151 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 577 7 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(O)cc1 10.1021/jm950626d
CHEMBL443825 169151 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 577 7 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(O)cc1 10.1021/jm950626d
44336539 5075 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL105775 5075 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/s0960-894x(98)00548-4
15104612 109296 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 514 13 3 4 6.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2cccc(O)c2n1 10.1021/jm00116a002
CHEMBL323249 109296 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 514 13 3 4 6.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2cccc(O)c2n1 10.1021/jm00116a002
CHEMBL2370120 208041 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL None None None CSCC[C@@H](NC(=O)[C@H](Cc1ccc(CCC(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
10318742 24803 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccncc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL134657 24803 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccncc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
14991542 106324 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 893 22 8 8 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144545 106324 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 893 22 8 8 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44280714 99571 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 726 14 6 9 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL286908 99571 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 726 14 6 9 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
5556 201569 26 None - 1 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 342 1 0 4 4.2 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1Cl)=NC2 10.1021/jm00396a028
CHEMBL646 201569 26 None - 1 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 342 1 0 4 4.2 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1Cl)=NC2 10.1021/jm00396a028
13822916 189134 0 None - 0 Guinea pig 4.4 pIC50 = 4.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 421 3 1 4 5.3 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00390a019
CHEMBL51569 189134 0 None - 0 Guinea pig 4.4 pIC50 = 4.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 421 3 1 4 5.3 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00390a019
44368541 168051 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 590 13 5 5 4.5 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL436065 168051 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 590 13 5 5 4.5 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
44286815 162717 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 810 20 7 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL418622 162717 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 810 20 7 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
155558199 174197 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1894 75 19 24 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4561184 174197 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1894 75 19 24 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
10346551 114138 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 518 5 3 3 5.3 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
CHEMBL333813 114138 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 518 5 3 3 5.3 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
10485763 109188 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 860 21 8 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Oc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL322635 109188 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 860 21 8 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Oc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44381815 58698 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 838 21 7 9 4.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL169126 58698 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 838 21 7 9 4.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
15667003 96890 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 1016 27 8 11 2.3 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(CCC)[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL269355 96890 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 1016 27 8 11 2.3 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(CCC)[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
10346998 17926 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 2 3 5.7 CN(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21)C(C)(C)C 10.1021/jm00048a015
CHEMBL126865 17926 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 2 3 5.7 CN(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21)C(C)(C)C 10.1021/jm00048a015
9962694 167671 3 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 853 21 8 9 3.3 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL433640 167671 3 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 853 21 8 9 3.3 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
46234969 73294 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 626 7 1 5 7.4 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1CC1CCCCC1 10.1016/j.bmcl.2012.02.049
CHEMBL2017828 73294 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 626 7 1 5 7.4 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1CC1CCCCC1 10.1016/j.bmcl.2012.02.049
155548381 173160 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1720 69 15 20 3.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)[C@@H](C)CC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4536393 173160 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1720 69 15 20 3.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)[C@@H](C)CC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL156559 207062 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
44396672 67176 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 545 7 2 6 4.5 CN(C)c1ccc(N2C(=O)CC3[C@@H](N[C@@H](Cc4c[nH]c5ccccc45)C(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm0498755
CHEMBL189549 67176 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 545 7 2 6 4.5 CN(C)c1ccc(N2C(=O)CC3[C@@H](N[C@@H](Cc4c[nH]c5ccccc45)C(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm0498755
10918992 79133 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 588 7 3 6 4.2 CN(C)c1ccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
CHEMBL2114079 79133 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 588 7 3 6 4.2 CN(C)c1ccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
13822921 101157 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 431 3 1 5 4.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)c1ccc(Cl)cc1 10.1021/jm00396a028
CHEMBL298948 101157 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 431 3 1 5 4.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)c1ccc(Cl)cc1 10.1021/jm00396a028
10389657 24454 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 462 3 2 3 4.4 CN1C(=O)C(NC(=O)Nc2cccc(Br)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL134340 24454 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 462 3 2 3 4.4 CN1C(=O)C(NC(=O)Nc2cccc(Br)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44329150 111908 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 580 7 3 3 6.8 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC3(C)CCCCC3)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL329735 111908 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 580 7 3 3 6.8 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC3(C)CCCCC3)C2=O)c1 10.1016/S0960-894X(01)80832-5
10053472 78434 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 557 8 3 4 4.1 CC(C)(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
CHEMBL2112829 78434 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 557 8 3 4 4.1 CC(C)(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
52949124 863 2 None -2 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
15689726 106112 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc(Cl)c1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142691 106112 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc(Cl)c1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44370451 50518 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL157658 50518 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
14991569 98343 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 863 20 9 9 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2cc(O)ccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL278447 98343 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 863 20 9 9 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2cc(O)ccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14208192 102522 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00047a021
CHEMBL306760 102522 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00047a021
14208236 202975 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 4 3.9 Cn1c(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc2ccccc21 10.1021/jm00047a021
CHEMBL73885 202975 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 4 3.9 Cn1c(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc2ccccc21 10.1021/jm00047a021
10030842 98141 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 566 8 4 5 3.5 O=C(N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm050689o
CHEMBL276837 98141 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 566 8 4 5 3.5 O=C(N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm050689o
54581302 61593 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc(N2CCN(C(=O)c3ncc(-c4ccc(OC)cc4)c(-c4ccc(C)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2011.03.069
CHEMBL1774041 61593 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc(N2CCN(C(=O)c3ncc(-c4ccc(OC)cc4)c(-c4ccc(C)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2011.03.069
15667012 168484 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 28 10 11 1.5 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL439591 168484 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 28 10 11 1.5 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
14208192 102522 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00120a002
CHEMBL306760 102522 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00120a002
14208236 202975 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 4 3.9 Cn1c(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc2ccccc21 10.1021/jm00120a002
CHEMBL73885 202975 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 4 3.9 Cn1c(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc2ccccc21 10.1021/jm00120a002
15667012 168484 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 976 28 10 11 1.5 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL439591 168484 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 976 28 10 11 1.5 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
10030842 98141 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 566 8 4 5 3.5 O=C(N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm000959x
CHEMBL276837 98141 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 566 8 4 5 3.5 O=C(N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm000959x
10030842 98141 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 566 8 4 5 3.5 O=C(N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1016/s0960-894x(01)00630-8
CHEMBL276837 98141 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 566 8 4 5 3.5 O=C(N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1016/s0960-894x(01)00630-8
9887120 202426 3 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL70380 202426 3 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL319438 209471 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44348651 167674 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 952 26 11 11 0.6 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL433647 167674 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 952 26 11 11 0.6 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
44381578 120002 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 840 23 10 10 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)CNN[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL354512 120002 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 840 23 10 10 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)CNN[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
90663979 106326 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 883 23 8 10 3.3 COc1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1OC 10.1021/jm00089a010
CHEMBL3144548 106326 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 883 23 8 10 3.3 COc1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1OC 10.1021/jm00089a010
44209151 59122 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 301 3 2 2 3.8 O=C(Cc1ccccc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
CHEMBL171108 59122 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 301 3 2 2 3.8 O=C(Cc1ccccc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
44336539 5075 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
14208245 203051 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00047a021
CHEMBL74580 203051 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00047a021
155553269 173555 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1818 68 15 22 3.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N1CCC[C@@H]1C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4545970 173555 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1818 68 15 22 3.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N1CCC[C@@H]1C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44348870 114330 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 452 7 3 5 3.3 O=C(O)CCC(NC(=O)c1cnc2ccccc2c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL334171 114330 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 452 7 3 5 3.3 O=C(O)CCC(NC(=O)c1cnc2ccccc2c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
44348887 117586 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 469 7 3 4 4.0 O=C(O)CCC(NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL340630 117586 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 469 7 3 4 4.0 O=C(O)CCC(NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
880 2208 3 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 487 5 3 7 3.5 O=C(N[C@@H]1N=C(C2CCCCC2)c2c(N(C1=O)C)cccc2)Nc1cccc(c1)N(c1n[nH]nn1)C 10.1021/jm9506736
9935175 2208 3 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 487 5 3 7 3.5 O=C(N[C@@H]1N=C(C2CCCCC2)c2c(N(C1=O)C)cccc2)Nc1cccc(c1)N(c1n[nH]nn1)C 10.1021/jm9506736
CHEMBL2093059 2208 3 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 487 5 3 7 3.5 O=C(N[C@@H]1N=C(C2CCCCC2)c2c(N(C1=O)C)cccc2)Nc1cccc(c1)N(c1n[nH]nn1)C 10.1021/jm9506736
15104628 9910 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 534 10 2 5 4.6 CCOC(=O)CN(Cc1ccccc1)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL114926 9910 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 534 10 2 5 4.6 CCOC(=O)CN(Cc1ccccc1)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
10369336 116255 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 517 7 2 4 4.5 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL337574 116255 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 517 7 2 4 4.5 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991535 106312 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 841 22 9 9 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1cccc(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144534 106312 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 841 22 9 9 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1cccc(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44366563 119165 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.5-4.6 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.5-4.6 uM
ChEMBL 447 6 2 2 5.8 O=C1C(Cc2c[nH]c3ccccc23)CN(Cc2ccccc2)C[C@@H]1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL347058 119165 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.5-4.6 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.5-4.6 uM
ChEMBL 447 6 2 2 5.8 O=C1C(Cc2c[nH]c3ccccc23)CN(Cc2ccccc2)C[C@@H]1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL169054 207092 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Compound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pigCompound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a068
11200806 137837 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 414 8 3 3 3.8 O=C(/C=C/c1ccccc1)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1021/jm051050n
CHEMBL377157 137837 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 414 8 3 3 3.8 O=C(/C=C/c1ccccc1)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1021/jm051050n
89913436 140257 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 283 2 1 2 2.6 O=C1C=C(Cl)C(O)(c2ccc(Cl)cc2)N1C1CC1 10.1039/C6MD00052E
CHEMBL3818705 140257 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 283 2 1 2 2.6 O=C1C=C(Cl)C(O)(c2ccc(Cl)cc2)N1C1CC1 10.1039/C6MD00052E
15167800 32500 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 412 4 3 3 4.4 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)c1cc2ccccc2[nH]1 10.1021/jm00163a069
CHEMBL141365 32500 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 412 4 3 3 4.4 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)c1cc2ccccc2[nH]1 10.1021/jm00163a069
10369346 24764 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 518 6 3 5 4.4 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)Nc3ccncc3)C2=O)cc1 10.1021/jm00078a018
CHEMBL134618 24764 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 518 6 3 5 4.4 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)Nc3ccncc3)C2=O)cc1 10.1021/jm00078a018
CHEMBL169054 207092 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to guinea pig cortical Cholecystokinin type A receptorTested for the inhibition of specific [3H]propionyl-CCK-8 binding to guinea pig cortical Cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
14208211 202709 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 311 2 2 3 2.1 CC(=O)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL72057 202709 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 311 2 2 3 2.1 CC(=O)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
11200806 137837 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 414 8 3 3 3.8 O=C(/C=C/c1ccccc1)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1016/j.bmc.2009.05.067
CHEMBL377157 137837 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 414 8 3 3 3.8 O=C(/C=C/c1ccccc1)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1016/j.bmc.2009.05.067
44300550 100429 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 376 3 2 3 3.7 Cc1cccc(NC(=O)NC2N=C(C3CCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
CHEMBL293786 100429 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 376 3 2 3 3.7 Cc1cccc(NC(=O)NC2N=C(C3CCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
44356801 164959 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 408 3 2 3 3.6 C#Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL424076 164959 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 408 3 2 3 3.6 C#Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
10696336 203624 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 487 5 3 4 4.6 CCCN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)CCC3)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
CHEMBL79565 203624 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 487 5 3 4 4.6 CCCN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)CCC3)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
71461592 78077 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 421 7 3 4 3.0 O=C(O)CC[C@H](NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL2111828 78077 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 421 7 3 4 3.0 O=C(O)CC[C@H](NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44357068 164330 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 456 5 3 4 3.6 CN1C(=O)C(NC(=O)NCc2cccc(C(C)(C)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL422102 164330 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 456 5 3 4 3.6 CN1C(=O)C(NC(=O)NCc2cccc(C(C)(C)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44408524 155164 0 None -169 4 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL405192 155164 0 None -169 4 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
10323431 57447 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 493 4 3 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)N(c2nn[nH]n2)CC3)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
CHEMBL166941 57447 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 493 4 3 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)N(c2nn[nH]n2)CC3)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
10056421 106145 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
CHEMBL3143025 106145 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
14208245 203051 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
CHEMBL74580 203051 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
CHEMBL317755 209459 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NS(C)(=O)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44578772 182214 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-c2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nn2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479063 182214 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-c2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nn2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
52949124 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
44336565 108728 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 671 8 2 7 5.7 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C4(C(F)(F)F)N=N4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL321700 108728 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 671 8 2 7 5.7 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C4(C(F)(F)F)N=N4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/s0960-894x(98)00548-4
10346957 26747 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 531 7 2 4 4.9 CCN(CC)C(=O)C(C)N1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136436 26747 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 531 7 2 4 4.9 CCN(CC)C(=O)C(C)N1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10002123 78401 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2112748 78401 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991539 106311 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 859 22 8 8 3.8 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144533 106311 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 859 22 8 8 3.8 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44366345 118980 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.3-5.4 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.3-5.4 uM
ChEMBL 447 6 2 2 5.8 O=C1[C@@H](Cc2c[nH]c3ccccc23)CN(Cc2ccccc2)C[C@H]1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL345327 118980 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.3-5.4 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.3-5.4 uM
ChEMBL 447 6 2 2 5.8 O=C1[C@@H](Cc2c[nH]c3ccccc23)CN(Cc2ccccc2)C[C@H]1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
19766221 118384 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 569 7 3 5 5.2 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1021/jm00163a069
CHEMBL342256 118384 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 569 7 3 5 5.2 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1021/jm00163a069
44280116 99171 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 672 12 3 6 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL284183 99171 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 672 12 3 6 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
10392698 116803 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 546 5 3 3 5.9 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(Cl)c3)C(=O)N(CC(=O)NC(C)(C)C)c3cc(C)ccc32)cc1 10.1021/jm00048a015
CHEMBL339678 116803 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 546 5 3 3 5.9 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(Cl)c3)C(=O)N(CC(=O)NC(C)(C)C)c3cc(C)ccc32)cc1 10.1021/jm00048a015
53465906 69069 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 456 8 5 4 3.7 O=C(Nc1ccccc1C(=O)NC(CCc1ccccc1)C(=O)NO)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933108 69069 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 456 8 5 4 3.7 O=C(Nc1ccccc1C(=O)NC(CCc1ccccc1)C(=O)NO)c1cc2ccccc2[nH]1 10.1021/jm200438b
44152863 119857 4 None - 0 Rat 7.4 pIC50 = 7.4 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 475 3 2 2 5.9 O=C1NN(C(=S)Nc2ccc(Cl)c(C(F)(F)F)c2)C(c2ccccc2)C1c1ccccc1 10.1016/S0960-894X(00)80684-8
CHEMBL353189 119857 4 None - 0 Rat 7.4 pIC50 = 7.4 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 475 3 2 2 5.9 O=C1NN(C(=S)Nc2ccc(Cl)c(C(F)(F)F)c2)C(c2ccccc2)C1c1ccccc1 10.1016/S0960-894X(00)80684-8
71450860 78189 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 1147 14 6 10 9.0 CC(C)(C)OC(=O)N[C@@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12.CC(C)(C)OC(=O)N[C@@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
CHEMBL2112273 78189 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 1147 14 6 10 9.0 CC(C)(C)OC(=O)N[C@@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12.CC(C)(C)OC(=O)N[C@@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
14208301 105174 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 412 3 1 4 3.3 CN1C(=O)C(NC(=O)c2ccc(C#N)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL312524 105174 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 412 3 1 4 3.3 CN1C(=O)C(NC(=O)c2ccc(C#N)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
10555571 104098 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 601 8 0 6 5.9 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
CHEMBL310466 104098 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 601 8 0 6 5.9 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
52949124 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
46235271 73301 2 None 2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
155533520 171262 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 910 26 8 9 2.5 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4468598 171262 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 910 26 8 9 2.5 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
10555571 104098 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 601 8 0 6 5.9 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL310466 104098 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 601 8 0 6 5.9 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10841358 205687 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccc(F)cc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL94005 205687 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccc(F)cc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
44334354 4553 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 517 9 2 4 5.0 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(C(=O)c3ccc(F)cc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL102879 4553 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 517 9 2 4 5.0 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(C(=O)c3ccc(F)cc3)CC2)c1 10.1016/0960-894X(95)00537-3
44300744 101483 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 542 6 4 4 4.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)O)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL301261 101483 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 542 6 4 4 4.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)O)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
10623795 205553 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 459 7 3 7 4.3 COc1ccccc1NC(=O)NNc1nc2ccccc2c(=O)n1-c1cccc(OC(C)C)c1 10.1021/jm970373j
CHEMBL9319 205553 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 459 7 3 7 4.3 COc1ccccc1NC(=O)NNc1nc2ccccc2c(=O)n1-c1cccc(OC(C)C)c1 10.1021/jm970373j
10478431 9806 7 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00124a003
CHEMBL114325 9806 7 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00124a003
14519981 9965 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00124a003
CHEMBL115269 9965 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00124a003
15104618 108554 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 496 13 3 2 6.8 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00116a002
CHEMBL321265 108554 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 496 13 3 2 6.8 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00116a002
44281078 99282 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 5.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL284975 99282 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 5.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
193319 20576 5 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 268 1 0 2 2.6 CN1C(=O)CN=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL13095 20576 5 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 268 1 0 2 2.6 CN1C(=O)CN=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL120632 206863 30 None - 3 Rat 5.4 pIC50 = 5.4 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasConcentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/0960-894X(94)85022-4
11729474 4603 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 420 2 2 5 2.1 Cc1cccc(NC(=O)NC2N=C(N3CCN(C)CC3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00530-0
CHEMBL103229 4603 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 420 2 2 5 2.1 Cc1cccc(NC(=O)NC2N=C(N3CCN(C)CC3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00530-0
14208302 67403 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 3 1 4 3.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C#N)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907847 67403 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 3 1 4 3.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C#N)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
24785432 180979 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 7 0 5 6.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(CC)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476725 180979 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 7 0 5 6.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(CC)cc2)c1 10.1016/j.bmcl.2008.06.057
24785176 180981 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 500 5 0 4 6.5 CCc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476747 180981 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 500 5 0 4 6.5 CCc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL169178 207094 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
15104613 109826 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00116a002
CHEMBL323854 109826 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00116a002
10364355 27743 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 412 4 2 3 3.9 C[C@H](NC(=O)NC1N=C(c2ccccc2)c2ccccc2N(C)C1=O)c1ccccc1 10.1021/jm00078a018
CHEMBL137208 27743 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 412 4 2 3 3.9 C[C@H](NC(=O)NC1N=C(c2ccccc2)c2ccccc2N(C)C1=O)c1ccccc1 10.1021/jm00078a018
44280266 98322 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 729 14 4 7 5.0 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL278217 98322 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 729 14 4 7 5.0 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
108187 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80273-5
873 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80273-5
CHEMBL2062154 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80273-5
CHEMBL287735 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80273-5
59923871 73612 1 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 1200-8500Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 1200-8500
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCC(NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80156-0
CHEMBL2021374 73612 1 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 1200-8500Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 1200-8500
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCC(NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80156-0
108187 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00105a062
873 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00105a062
CHEMBL2062154 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00105a062
CHEMBL287735 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00105a062
14802537 85561 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL2304062 85561 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(01)80769-1
108187 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80685-X
873 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80685-X
CHEMBL2062154 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80685-X
CHEMBL287735 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80685-X
14802538 96241 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/s0960-894x(98)00677-5
CHEMBL263969 96241 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/s0960-894x(98)00677-5
108187 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(97)00356-9
873 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(97)00356-9
CHEMBL2062154 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(97)00356-9
CHEMBL287735 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(97)00356-9
44368727 119000 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 598 12 5 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00057a005
CHEMBL345511 119000 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 598 12 5 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00057a005
44153340 31459 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 413 3 0 4 3.8 CN1c2ccccc2C(c2ccccc2F)=NCC1CN1C(=O)c2ccccc2C1=O 10.1021/jm00163a069
CHEMBL140516 31459 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 413 3 0 4 3.8 CN1c2ccccc2C(c2ccccc2F)=NCC1CN1C(=O)c2ccccc2C1=O 10.1021/jm00163a069
108187 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm970065l
873 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm970065l
CHEMBL2062154 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm970065l
CHEMBL287735 913 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm970065l
14802539 76199 1 None - 1 Rat 5.4 pIC50 = 5.4 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1200-8500The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1200-8500
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2062144 76199 1 None - 1 Rat 5.4 pIC50 = 5.4 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1200-8500The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1200-8500
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80652-6
136060577 87248 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Displacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assay
ChEMBL 495 4 1 5 6.3 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccccc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL233647 87248 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Displacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assay
ChEMBL 495 4 1 5 6.3 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccccc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
44369595 167962 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 475 7 2 7 4.2 Cc1cccc(NCNC2N=C(c3nccs3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL435447 167962 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 475 7 2 7 4.2 Cc1cccc(NCNC2N=C(c3nccs3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
9978270 78402 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 3 4 3.2 CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2112749 78402 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 3 4 3.2 CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10323637 105705 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 498 7 2 5 3.6 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm00078a018
CHEMBL313813 105705 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 498 7 2 5 3.6 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm00078a018
10323637 105705 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 498 7 2 5 3.6 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm9608523
CHEMBL313813 105705 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 498 7 2 5 3.6 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm9608523
10973981 78024 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 590 7 3 7 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc([N+](=O)[O-])c3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL2111548 78024 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 590 7 3 7 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc([N+](=O)[O-])c3)C(=O)C[C@@H]12 10.1021/jm010813d
46234970 73293 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 620 7 1 5 6.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017827 73293 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 620 7 1 5 6.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
10051431 120613 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 494 6 2 4 5.1 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL357502 120613 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 494 6 2 4 5.1 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
44336487 110512 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 699 9 2 7 6.5 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C4(C(F)(F)F)N=N4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL326251 110512 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 699 9 2 7 6.5 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C4(C(F)(F)F)N=N4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
14802525 116227 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 626 12 5 5 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL337384 116227 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 626 12 5 5 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00105a062
44368613 120489 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 610 12 5 4 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL356419 120489 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 610 12 5 4 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00057a005
73351319 167601 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 648 12 5 5 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCP(C)(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL433148 167601 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 648 12 5 5 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCP(C)(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL282175 98863 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 769 16 6 11 4.6 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCSCc3csc(C=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00249-1
44591882 178397 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 466 7 5 3 4.3 O=C(Nc1ccccc1C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL470622 178397 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 466 7 5 3 4.3 O=C(Nc1ccccc1C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
10789229 97928 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 440 6 3 7 3.8 CCOc1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL275307 97928 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 440 6 3 7 3.8 CCOc1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
10091467 116205 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 385 3 2 4 3.0 CN1C(=O)C(NC(=O)Nc2ccccn2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL337285 116205 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 385 3 2 4 3.0 CN1C(=O)C(NC(=O)Nc2ccccn2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44362744 34447 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 546 7 4 5 3.5 CC(C)(C)OC(=O)N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](CC(=O)O)Cc3ccccc3)N2C1=O 10.1016/s0960-894x(98)00677-5
CHEMBL143012 34447 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 546 7 4 5 3.5 CC(C)(C)OC(=O)N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](CC(=O)O)Cc3ccccc3)N2C1=O 10.1016/s0960-894x(98)00677-5
40875375 198366 1 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Concentration required for binding affinity to neuropeptide (CCK-A) receptor in rat pancreaConcentration required for binding affinity to neuropeptide (CCK-A) receptor in rat pancrea
ChEMBL 480 9 4 3 4.8 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1c[nH]c2ccccc12)OCc1ccccc1 10.1016/S0960-894X(97)00346-6
CHEMBL59561 198366 1 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Concentration required for binding affinity to neuropeptide (CCK-A) receptor in rat pancreaConcentration required for binding affinity to neuropeptide (CCK-A) receptor in rat pancrea
ChEMBL 480 9 4 3 4.8 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1c[nH]c2ccccc12)OCc1ccccc1 10.1016/S0960-894X(97)00346-6
11801355 116368 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 580 8 3 6 3.6 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@@H](NC(=O)OCc3ccccc3)C(=O)N21 10.1021/jm000959x
CHEMBL338186 116368 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 580 8 3 6 3.6 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@@H](NC(=O)OCc3ccccc3)C(=O)N21 10.1021/jm000959x
44360340 32485 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 457 5 1 4 5.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1cccc2sccc12 10.1021/jm00163a069
CHEMBL141354 32485 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 457 5 1 4 5.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1cccc2sccc12 10.1021/jm00163a069
89913625 140230 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 293 6 1 2 3.4 CCCCCCN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
CHEMBL3818303 140230 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 293 6 1 2 3.4 CCCCCCN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
14802538 96241 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL263969 96241 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00092a007
44334033 107319 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 475 6 2 4 4.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL319196 107319 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 475 6 2 4 4.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
57390472 67413 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 431 5 1 4 3.3 COc1cccc(CC(=O)N[C@@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)c1 10.1021/jm00120a002
CHEMBL1907856 67413 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 431 5 1 4 3.3 COc1cccc(CC(=O)N[C@@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)c1 10.1021/jm00120a002
44359881 118797 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 473 8 1 5 4.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)CCC(=O)OCc1ccccc1 10.1021/jm00163a069
CHEMBL343969 118797 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 473 8 1 5 4.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)CCC(=O)OCc1ccccc1 10.1021/jm00163a069
10574611 205520 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 429 6 3 6 4.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccccc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9291 205520 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 429 6 3 6 4.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccccc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL171310 207104 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CC(=O)N[C@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
10010811 106126 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 854 21 9 9 3.5 CC(=O)c1ccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm960509y
CHEMBL3142898 106126 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 854 21 9 9 3.5 CC(=O)c1ccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm960509y
42636923 178253 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 393 7 4 3 3.6 CC(C)C[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL469341 178253 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 393 7 4 3 3.6 CC(C)C[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
15104624 9905 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 514 13 2 4 5.7 CCCCCN(CCCCC)C(=O)[C@@H](CC1C(=O)Nc2ccccc21)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL114913 9905 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 514 13 2 4 5.7 CCCCCN(CCCCC)C(=O)[C@@H](CC1C(=O)Nc2ccccc21)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
10341040 116109 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 402 3 2 3 3.8 CN1C(=O)C(NC(=O)Nc2ccc(F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL336749 116109 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 402 3 2 3 3.8 CN1C(=O)C(NC(=O)Nc2ccc(F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44336539 5075 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10393441 171147 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 580 7 3 3 6.5 CC(C)(NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm00048a015
CHEMBL446682 171147 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 580 7 3 3 6.5 CC(C)(NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm00048a015
44362685 121327 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL358989 121327 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
14720386 48060 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 463 12 2 4 4.4 CCCN(CCC)C(=O)[C@H](CCC(=O)OCc1ccccc1)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL155406 48060 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 463 12 2 4 4.4 CCCN(CCC)C(=O)[C@H](CCC(=O)OCc1ccccc1)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
44281005 116231 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00249-1
CHEMBL33743 116231 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00249-1
44592046 178328 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 393 6 3 3 4.0 CC(C)C[C@H](NC(=O)N(C(=O)c1cc2ccccc2[nH]1)c1ccccc1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL469980 178328 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 393 6 3 3 4.0 CC(C)C[C@H](NC(=O)N(C(=O)c1cc2ccccc2[nH]1)c1ccccc1)C(=O)O 10.1016/j.bmc.2009.02.012
10347746 16622 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 558 6 3 3 6.2 CC1(NC(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(Cl)c3)C[C@H](c3ccccc3)c3ccccc32)CCCCC1 10.1021/jm00048a015
CHEMBL124611 16622 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 558 6 3 3 6.2 CC1(NC(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(Cl)c3)C[C@H](c3ccccc3)c3ccccc32)CCCCC1 10.1021/jm00048a015
44368633 46282 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 588 12 5 5 4.3 C[C@@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL153787 46282 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 588 12 5 5 4.3 C[C@@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00057a005
115208 3758 25 None -91 4 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 393 4 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm00163a069
1667 3758 25 None -91 4 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 393 4 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm00163a069
CHEMBL169703 3758 25 None -91 4 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 393 4 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm00163a069
10769565 17790 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 580 8 3 6 3.6 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1021/jm000959x
CHEMBL126160 17790 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 580 8 3 6 3.6 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1021/jm000959x
9982757 51196 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 483 5 2 5 4.3 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL158235 51196 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 483 5 2 5 4.3 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
44381562 168049 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 827 22 10 9 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NNC[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL436053 168049 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 827 22 10 9 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NNC[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
11505691 140394 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)[C@@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1021/jm049072h
CHEMBL382263 140394 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)[C@@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1021/jm049072h
9891461 164470 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 483 5 2 5 4.3 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL422604 164470 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 483 5 2 5 4.3 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
15104598 109295 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 481 13 2 2 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
CHEMBL323245 109295 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 481 13 2 2 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
14208258 102483 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(F)cc1 10.1021/jm00047a021
CHEMBL306394 102483 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(F)cc1 10.1021/jm00047a021
10769675 205470 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1cccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)c1 10.1021/jm970265x
CHEMBL92586 205470 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1cccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)c1 10.1021/jm970265x
14208200 203011 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 422 5 3 3 4.0 O=C(CCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL74181 203011 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 422 5 3 3 4.0 O=C(CCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
44341613 9522 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 516 13 2 3 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccc(F)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL112622 9522 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 516 13 2 3 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccc(F)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
52940616 17955 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269263 17955 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
10453063 106508 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 391 2 2 4 3.0 Cc1cccc(NC(=O)NC2N=C(N3CCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL315214 106508 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 391 2 2 4 3.0 Cc1cccc(NC(=O)NC2N=C(N3CCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
21842331 43292 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 522 7 2 4 5.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)CC3CCCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL150869 43292 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 522 7 2 4 5.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)CC3CCCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
73349791 204093 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 664 13 5 6 5.2 CCOP(=O)(O)CC(=O)N[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1021/jm00092a007
CHEMBL83244 204093 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 664 13 5 6 5.2 CCOP(=O)(O)CC(=O)N[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1021/jm00092a007
14208258 102483 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(F)cc1 10.1021/jm00120a002
CHEMBL306394 102483 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(F)cc1 10.1021/jm00120a002
44370461 119061 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL346070 119061 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
10453063 106508 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 391 2 2 4 3.0 Cc1cccc(NC(=O)NC2N=C(N3CCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL315214 106508 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 391 2 2 4 3.0 Cc1cccc(NC(=O)NC2N=C(N3CCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
14208200 203011 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 422 5 3 3 4.0 O=C(CCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL74181 203011 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 422 5 3 3 4.0 O=C(CCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
19766220 31718 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 395 4 2 4 3.8 CN1c2ccccc2C(c2ccccc2F)NCC1CNC(=O)c1ccsc1 10.1021/jm00163a069
CHEMBL140749 31718 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 395 4 2 4 3.8 CN1c2ccccc2C(c2ccccc2F)NCC1CNC(=O)c1ccsc1 10.1021/jm00163a069
10323073 25207 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 484 7 2 5 3.8 CCOC(=O)CN1C(=O)C(NC(=O)N[C@@H](C)c2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL134987 25207 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 484 7 2 5 3.8 CCOC(=O)CN1C(=O)C(NC(=O)N[C@@H](C)c2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44280252 99391 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 655 11 5 8 3.7 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL285746 99391 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 655 11 5 8 3.7 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
6604124 55311 3 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
CHEMBL1315743 55311 3 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
CHEMBL162111 55311 3 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
70682900 77496 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 385 3 2 3 4.6 O=C1Nc2ccccc2C(c2ccccc2F)=NC1C[C@@H]1CNc2ccccc21 10.1021/jm00390a019
CHEMBL2092991 77496 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 385 3 2 3 4.6 O=C1Nc2ccccc2C(c2ccccc2F)=NC1C[C@@H]1CNc2ccccc21 10.1021/jm00390a019
20063212 166588 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 395 3 0 3 4.5 CN1CC(CC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c2ccccc21 10.1021/jm00390a019
CHEMBL429063 166588 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 395 3 0 3 4.5 CN1CC(CC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c2ccccc21 10.1021/jm00390a019
44349353 116342 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 415 7 3 4 3.0 Cc1cc(C)cc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
CHEMBL338045 116342 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 415 7 3 4 3.0 Cc1cc(C)cc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
44381852 58734 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(=O)O 10.1016/S0960-894X(97)00107-8
CHEMBL169398 58734 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(=O)O 10.1016/S0960-894X(97)00107-8
44361604 31262 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 621 8 3 4 4.9 O=C(N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm991078x
CHEMBL140320 31262 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 621 8 3 4 4.9 O=C(N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm991078x
44381730 13851 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 450 8 2 4 2.5 CN1CCN(C(=O)CCC(NC(=O)c2cccc(Cl)c2)C(=O)NCCC(C)(C)C)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1196729 13851 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 450 8 2 4 2.5 CN1CCN(C(=O)CCC(NC(=O)c2cccc(Cl)c2)C(=O)NCCC(C)(C)C)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL557997 13851 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 450 8 2 4 2.5 CN1CCN(C(=O)CCC(NC(=O)c2cccc(Cl)c2)C(=O)NCCC(C)(C)C)CC1 10.1016/S0960-894X(00)80681-2
10320031 77472 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL2092868 77472 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
90663981 106328 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 891 21 8 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144550 106328 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 891 21 8 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
70689603 73247 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 588 8 1 6 5.5 COCCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017690 73247 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 588 8 1 6 5.5 COCCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
52946666 17952 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269260 17952 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
44300743 100492 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 572 6 4 6 4.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL294161 100492 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 572 6 4 6 4.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
11679146 134832 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1021/jm049072h
CHEMBL372773 134832 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1021/jm049072h
11741582 27753 6 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 4 2 3 3.3 CN1C(=O)C(NC(=O)NCc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137213 27753 6 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 4 2 3 3.3 CN1C(=O)C(NC(=O)NCc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10029145 97718 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 504 7 2 5 4.6 CCOC(=O)CCN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL273919 97718 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 504 7 2 5 4.6 CCOC(=O)CCN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10693825 205327 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 428 5 3 6 3.9 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N(C)C)c2)c1 10.1021/jm970373j
CHEMBL9171 205327 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 428 5 3 6 3.9 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N(C)C)c2)c1 10.1021/jm970373j
6604124 55311 3 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
CHEMBL1315743 55311 3 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
CHEMBL162111 55311 3 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
10528637 96855 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 477 6 3 7 4.4 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2)c1 10.1021/jm970373j
CHEMBL269123 96855 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 477 6 3 7 4.4 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2)c1 10.1021/jm970373j
14208229 102693 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 430 3 3 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00120a002
CHEMBL308111 102693 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 430 3 3 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00120a002
14208229 102693 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 430 3 3 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00047a021
CHEMBL308111 102693 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 430 3 3 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00047a021
44306823 201378 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 802 20 9 7 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(CCCCNC(=O)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL63707 201378 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 802 20 9 7 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(CCCCNC(=O)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
3081191 9457 9 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00124a003
CHEMBL112307 9457 9 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00124a003
3081191 9457 9 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL112307 9457 9 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
44293812 101245 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 645 5 2 4 5.9 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(Br)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL299523 101245 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 645 5 2 4 5.9 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(Br)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
11027990 67192 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptorInhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptor
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67192 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptorInhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptor
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
44330874 206621 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 974 28 10 11 2.1 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N/C(=C\c1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL99499 206621 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 974 28 10 11 2.1 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N/C(=C\c1ccccc1)C(N)=O 10.1021/jm00094a001
10056407 119643 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 854 20 7 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL351364 119643 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 854 20 7 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL318570 209469 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL438911 212058 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
24785180 180958 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 536 6 0 5 6.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476531 180958 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 536 6 0 5 6.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2008.06.057
11803697 106134 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc([N+](=O)[O-])c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
136898911 106134 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc([N+](=O)[O-])c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
CHEMBL3142912 106134 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc([N+](=O)[O-])c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
15667013 106922 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 920 26 10 11 0.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL318010 106922 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 920 26 10 11 0.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL319439 209472 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
3960 2313 20 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00079a003
891 2313 20 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00079a003
CHEMBL24938 2313 20 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00079a003
44349077 117338 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00079a003
CHEMBL340263 117338 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00079a003
10483574 6129 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 591 8 2 5 5.3 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL108130 6129 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 591 8 2 5 5.3 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
13605417 205834 3 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80681-2
CHEMBL9485 205834 3 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80681-2
10458620 114048 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 499 5 2 4 5.4 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1021/jm00048a015
CHEMBL333718 114048 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 499 5 2 4 5.4 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1021/jm00048a015
13605417 205834 3 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80687-3
CHEMBL9485 205834 3 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80687-3
14991580 100241 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 829 21 8 9 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1cccs1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL292490 100241 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 829 21 8 9 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1cccs1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
10507109 108740 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
CHEMBL321761 108740 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
10507109 108740 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm950626d
CHEMBL321761 108740 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm950626d
10507109 108740 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/S0960-894X(97)00062-0
CHEMBL321761 108740 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/S0960-894X(97)00062-0
44336539 5075 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
11039204 78180 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 588 7 3 6 4.2 CN(C)c1cccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)c1 10.1021/jm010813d
CHEMBL2112231 78180 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 588 7 3 6 4.2 CN(C)c1cccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)c1 10.1021/jm010813d
14208265 202804 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00120a002
CHEMBL72616 202804 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00120a002
14802530 21417 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 614 12 5 5 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CNC(=O)CC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL131754 21417 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 614 12 5 5 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CNC(=O)CC(=O)O)Cc1ccccc1 10.1021/jm00105a062
15104607 162861 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 497 13 2 2 6.9 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc2ccccc12 10.1021/jm00116a002
CHEMBL419585 162861 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 497 13 2 2 6.9 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc2ccccc12 10.1021/jm00116a002
44334305 109231 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 514 9 3 4 4.6 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL322913 109231 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 514 9 3 4 4.6 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
101918113 114915 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor by displacement of [125I]BH-CCK-8 from rat pancreatic aciniBinding affinity towards Cholecystokinin type A receptor by displacement of [125I]BH-CCK-8 from rat pancreatic acini
ChEMBL 650 14 6 7 0.7 CS[C@H]1C[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)N(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(C)=O)C1 10.1021/jm00001a019
CHEMBL3350334 114915 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor by displacement of [125I]BH-CCK-8 from rat pancreatic aciniBinding affinity towards Cholecystokinin type A receptor by displacement of [125I]BH-CCK-8 from rat pancreatic acini
ChEMBL 650 14 6 7 0.7 CS[C@H]1C[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)N(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(C)=O)C1 10.1021/jm00001a019
CHEMBL407736 210933 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
44211354 12755 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 536 6 1 4 4.2 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1188705 12755 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 536 6 1 4 4.2 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL537171 12755 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 536 6 1 4 4.2 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
44280740 99941 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 6.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL290122 99941 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 6.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL289310 209126 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
20063240 13539 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 480 6 2 4 4.7 CC(C)CC(N)C(=O)N1CC(CC2N=C(c3ccccc3)c3ccccc3NC2=O)c2ccccc21 10.1021/jm00390a019
CHEMBL1194526 13539 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 480 6 2 4 4.7 CC(C)CC(N)C(=O)N1CC(CC2N=C(c3ccccc3)c3ccccc3NC2=O)c2ccccc21 10.1021/jm00390a019
CHEMBL552817 13539 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 480 6 2 4 4.7 CC(C)CC(N)C(=O)N1CC(CC2N=C(c3ccccc3)c3ccccc3NC2=O)c2ccccc21 10.1021/jm00390a019
15614807 67385 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 365 3 2 2 4.6 O=C1Nc2ccccc2C(c2ccccc2)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
CHEMBL1907740 67385 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 365 3 2 2 4.6 O=C1Nc2ccccc2C(c2ccccc2)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
14208265 202804 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00047a021
CHEMBL72616 202804 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00047a021
887 4047 24 None - 4 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm960669+
9870520 4047 24 None - 4 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm960669+
CHEMBL324547 4047 24 None - 4 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm960669+
DB12355 4047 24 None - 4 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm960669+
10649606 49349 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL3142692 209386 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc(Cl)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
10070677 161175 13 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
CHEMBL41361 161175 13 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
10649606 49349 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
54580263 61528 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773878 61528 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.03.069
15104611 108770 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 514 13 3 4 6.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(O)c2ccccc2n1 10.1021/jm00116a002
CHEMBL321811 108770 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 514 13 3 4 6.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(O)c2ccccc2n1 10.1021/jm00116a002
15104601 169861 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
CHEMBL444847 169861 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
CHEMBL99786 214152 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
73355867 204537 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 680 12 5 6 6.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1ccccc1O)c1ccccc1 10.1021/jm00092a007
CHEMBL86879 204537 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 680 12 5 6 6.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1ccccc1O)c1ccccc1 10.1021/jm00092a007
10501974 96527 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 415 5 3 6 3.9 COc1cccc(-n2c(NNC(=O)Nc3cccc(C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL266376 96527 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 415 5 3 6 3.9 COc1cccc(-n2c(NNC(=O)Nc3cccc(C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL436451 211933 0 None - 0 Mouse 4.3 pIC50 = 4.3 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44368522 118976 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 574 11 5 5 4.4 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)NC[C@H](NC(=O)/C=C/C(=O)O)c1ccccc1 10.1021/jm00057a005
CHEMBL345303 118976 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 574 11 5 5 4.4 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)NC[C@H](NC(=O)/C=C/C(=O)O)c1ccccc1 10.1021/jm00057a005
CHEMBL382349 210555 0 None -3235 4 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
44336539 5075 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
44591825 183524 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 411 8 4 4 3.4 CSCCC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL482571 183524 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 411 8 4 4 3.4 CSCCC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
14991576 101744 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 866 21 9 9 3.4 COc1ccc2[nH]c(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cc2c1 10.1021/jm00089a010
CHEMBL302911 101744 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 866 21 9 9 3.4 COc1ccc2[nH]c(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cc2c1 10.1021/jm00089a010
51353551 17950 10 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269257 17950 10 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
10414170 170051 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1016/S0960-894X(00)80683-6
CHEMBL445095 170051 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1016/S0960-894X(00)80683-6
44300989 100511 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 625 7 4 6 4.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(C)(=O)=O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL294252 100511 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 625 7 4 6 4.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(C)(=O)=O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
44382624 119853 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 619 12 4 4 4.0 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)/C=C/c1ccccc1)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
CHEMBL353148 119853 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 619 12 4 4 4.0 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)/C=C/c1ccccc1)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
10414170 170051 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00121a004
CHEMBL445095 170051 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00121a004
15104602 9361 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
CHEMBL111808 9361 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
44366583 120782 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.1-6.4 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.1-6.4 uM
ChEMBL 420 4 1 5 4.9 CC(C)(C)OC(=O)n1cc(CC2CN(Cc3ccccc3)CCC2O)c2ccccc21 10.1016/0960-894X(94)80030-8
CHEMBL358016 120782 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.1-6.4 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.1-6.4 uM
ChEMBL 420 4 1 5 4.9 CC(C)(C)OC(=O)n1cc(CC2CN(Cc3ccccc3)CCC2O)c2ccccc21 10.1016/0960-894X(94)80030-8
73354294 106485 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 636 11 6 5 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CP(=O)(O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL315055 106485 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 636 11 6 5 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CP(=O)(O)O)c1ccccc1 10.1021/jm00092a007
15104610 9594 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 513 13 3 3 6.6 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2cc(O)ccc2c1 10.1021/jm00116a002
CHEMBL113041 9594 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 513 13 3 3 6.6 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2cc(O)ccc2c1 10.1021/jm00116a002
44280388 116369 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 759 15 4 8 5.0 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL33819 116369 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 759 15 4 8 5.0 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44334330 4960 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 435 7 2 3 4.7 Cc1cccc(NC(=O)N[C@@H](CC(C)C)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL105153 4960 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 435 7 2 3 4.7 Cc1cccc(NC(=O)N[C@@H](CC(C)C)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44381319 120213 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 495 11 4 5 3.6 N#C[C@H](N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
CHEMBL354817 120213 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 495 11 4 5 3.6 N#C[C@H](N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
10626596 112284 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 555 7 1 4 5.6 O=C1C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc2N1CC(=O)N(c1ccccc1)C1CC1 10.1021/jm970265x
CHEMBL330566 112284 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 555 7 1 4 5.6 O=C1C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc2N1CC(=O)N(c1ccccc1)C1CC1 10.1021/jm970265x
44327457 106854 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 571 11 3 4 5.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL317577 106854 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 571 11 3 4 5.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL262767 208803 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None Cc1ccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00113a023
CHEMBL262767 208803 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None Cc1ccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm960509y
CHEMBL262767 208803 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00173a006
44333311 4194 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 476 6 2 5 3.5 CCCc1cccc(NC(=O)NC2N=C(N3CCN(C)CC3)c3ccccc3N(CCC)C2=O)c1 10.1016/0960-894X(95)00530-0
CHEMBL100502 4194 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 476 6 2 5 3.5 CCCc1cccc(NC(=O)NC2N=C(N3CCN(C)CC3)c3ccccc3N(CCC)C2=O)c1 10.1016/0960-894X(95)00530-0
44303481 100232 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 524 9 3 6 4.3 CC(=O)Nc1nc(CC(C)(NC(=O)OC2C3CC4CC(C3)CC2C4)C(=O)NCCc2ccccc2)cs1 10.1016/S0960-894X(97)00356-9
CHEMBL292422 100232 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 524 9 3 6 4.3 CC(=O)Nc1nc(CC(C)(NC(=O)OC2C3CC4CC(C3)CC2C4)C(=O)NCCc2ccccc2)cs1 10.1016/S0960-894X(97)00356-9
10789887 205694 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 454 6 3 7 4.2 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9405 205694 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 454 6 3 7 4.2 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
45482492 196307 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 495 7 4 3 4.9 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cccc(C(F)(F)F)c2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL573560 196307 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 495 7 4 3 4.9 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cccc(C(F)(F)F)c2[nH]1 10.1016/j.bmc.2009.05.067
10370499 36721 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL145133 36721 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
10370499 36721 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 557 10 4 4 5.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
CHEMBL145133 36721 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 557 10 4 4 5.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
10370499 85563 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL2304064 85563 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1021/jm00057a005
10769315 16662 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 566 8 4 5 3.5 O=C(N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm000959x
CHEMBL124798 16662 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 566 8 4 5 3.5 O=C(N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm000959x
11621814 140708 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
CHEMBL382953 140708 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
10507109 108740 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
CHEMBL321761 108740 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
44370473 50589 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL157722 50589 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
44280213 101147 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 685 12 5 9 3.7 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL29888 101147 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 685 12 5 9 3.7 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
70697518 77453 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 367 3 2 3 4.4 O=C1Nc2ccccc2C(c2ccccc2)=NC1C[C@@H]1CNc2ccccc21 10.1021/jm00390a019
CHEMBL2092748 77453 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 367 3 2 3 4.4 O=C1Nc2ccccc2C(c2ccccc2)=NC1C[C@@H]1CNc2ccccc21 10.1021/jm00390a019
10649606 49349 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
44283087 120311 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 8 2 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)OCCc1ccccc1 10.1021/jm00086a017
CHEMBL35580 120311 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 8 2 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)OCCc1ccccc1 10.1021/jm00086a017
45482494 196308 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)N[C@H](Cc1ccccc1)C(=O)O)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL573561 196308 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)N[C@H](Cc1ccccc1)C(=O)O)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
54582288 61541 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2C)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773893 61541 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2C)cc1 10.1016/j.bmcl.2011.03.069
90663977 106317 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 823 21 8 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144539 106317 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 823 21 8 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44386117 130829 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 541 9 4 4 5.3 O=C(O)C[C@H](Cc1ccccc1)NC(=O)/C(=C/c1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
CHEMBL368803 130829 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 541 9 4 4 5.3 O=C(O)C[C@H](Cc1ccccc1)NC(=O)/C(=C/c1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
44458120 98504 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 377 5 3 3 2.0 O=C(N[C@@H]1C(=O)N(Cc2ccccc2)C[C@@H]1C(=O)O)c1cc2ccccc2[nH]1 10.1016/S0960-894X(00)80224-3
CHEMBL279730 98504 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 377 5 3 3 2.0 O=C(N[C@@H]1C(=O)N(Cc2ccccc2)C[C@@H]1C(=O)O)c1cc2ccccc2[nH]1 10.1016/S0960-894X(00)80224-3
44366587 43445 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.7-7.1 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.7-7.1 uM
ChEMBL 554 10 0 8 7.2 CCOP(=O)(OCC)OC1=CCN(Cc2ccccc2)CC1Cc1cn(C(=O)OC(C)(C)C)c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL151022 43445 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.7-7.1 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.7-7.1 uM
ChEMBL 554 10 0 8 7.2 CCOP(=O)(OCC)OC1=CCN(Cc2ccccc2)CC1Cc1cn(C(=O)OC(C)(C)C)c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL441840 212149 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
14208246 202976 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00120a002
CHEMBL73892 202976 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00120a002
15637194 25734 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 308 2 2 3 1.5 CN1C(=O)C(NC(N)=O)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135405 25734 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 308 2 2 3 1.5 CN1C(=O)C(NC(N)=O)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44592484 187529 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 337 5 4 3 2.2 O=C(O)CNC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL498273 187529 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 337 5 4 3 2.2 O=C(O)CNC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
10553207 206531 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 492 6 2 6 4.7 CC(C)Oc1cccc(-n2c(NNC(=O)c3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9888 206531 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 492 6 2 6 4.7 CC(C)Oc1cccc(-n2c(NNC(=O)c3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
23757281 9758 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 539 8 2 5 5.5 CCN(CC)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL114072 9758 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 539 8 2 5 5.5 CCN(CC)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
10389643 118516 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 462 5 3 4 3.8 O=C(O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL342614 118516 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 462 5 3 4 3.8 O=C(O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
9984739 114316 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 538 5 3 3 6.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2C1CCCCC1 10.1021/jm00048a015
CHEMBL334100 114316 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 538 5 3 3 6.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2C1CCCCC1 10.1021/jm00048a015
44280180 102160 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 655 11 5 8 3.6 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL30430 102160 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 655 11 5 8 3.6 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44329304 107632 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 526 7 3 3 5.5 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL319569 107632 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 526 7 3 3 5.5 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
44382749 59397 0 None - 0 Mouse 4.3 pIC50 = 4.3 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 532 11 4 4 3.0 CC(C)C[C@H](NC(=O)CCc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
CHEMBL172354 59397 0 None - 0 Mouse 4.3 pIC50 = 4.3 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 532 11 4 4 3.0 CC(C)C[C@H](NC(=O)CCc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
10673307 110147 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 511 7 3 5 4.2 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(NC=O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL325746 110147 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 511 7 3 5 4.2 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(NC=O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
14208246 202976 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00047a021
CHEMBL73892 202976 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00047a021
44327455 106861 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 585 12 3 4 6.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL317626 106861 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 585 12 3 4 6.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
15104603 9406 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 436 13 3 2 5.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc[nH]1 10.1021/jm00116a002
CHEMBL112054 9406 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 436 13 3 2 5.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc[nH]1 10.1021/jm00116a002
10412837 27416 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 479 5 3 5 4.0 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(Cc3n[nH]c(C)n3)C2=O)c1 10.1021/jm00078a018
CHEMBL136975 27416 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 479 5 3 5 4.0 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(Cc3n[nH]c(C)n3)C2=O)c1 10.1021/jm00078a018
CHEMBL345598 209963 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)N(C)C(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
44382562 58791 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 662 13 5 5 5.8 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc(O)cc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL169710 58791 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 662 13 5 5 5.8 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc(O)cc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
10408567 118774 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
CHEMBL343767 118774 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
90663991 106337 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 868 22 8 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144560 106337 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 868 22 8 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14991567 198118 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 847 20 8 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL59404 198118 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 847 20 8 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44280117 101581 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 672 12 3 6 5.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL30195 101581 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 672 12 3 6 5.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
14423345 202726 1 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 283 1 1 3 1.9 CN1C(=O)C(N)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL72151 202726 1 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 283 1 1 3 1.9 CN1C(=O)C(N)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10768084 9924 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 512 6 2 6 4.1 CN(C)c1cccc(NC(=O)N[C@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL114991 9924 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 512 6 2 6 4.1 CN(C)c1cccc(NC(=O)N[C@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
44408483 168363 0 None -165 4 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.7 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL438739 168363 0 None -165 4 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.7 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL262172 208783 0 None -26302 4 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
44376112 119688 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligandThe compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligand
ChEMBL 452 4 3 6 2.8 CN1C(=O)[C@@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL351854 119688 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligandThe compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligand
ChEMBL 452 4 3 6 2.8 CN1C(=O)[C@@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
14208221 79138 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 530 6 2 5 4.2 CN1C(=O)C(NC(=O)C(Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL2114102 79138 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 530 6 2 5 4.2 CN1C(=O)C(NC(=O)C(Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
44354128 20094 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 4.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL130578 20094 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 4.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
14802521 58775 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 628 13 5 5 4.7 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL169616 58775 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 628 13 5 5 4.7 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
10392523 206206 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL96970 206206 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
15104609 110050 0 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1nccc2ccccc12 10.1021/jm00116a002
CHEMBL325160 110050 0 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1nccc2ccccc12 10.1021/jm00116a002
19766222 116102 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 383 5 1 4 3.9 CC(C)COC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
CHEMBL336690 116102 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 383 5 1 4 3.9 CC(C)COC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
14208308 67401 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907845 67401 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
15167811 167328 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 417 3 0 3 4.3 CN1C(=O)C(N(C)C(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL431185 167328 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 417 3 0 3 4.3 CN1C(=O)C(N(C)C(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
11607292 165443 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
CHEMBL425392 165443 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
44303526 201454 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 708 14 4 6 6.3 O=C(CCC(=O)OCc1ccccc1)N[C@@H](CNC(=O)C(Cc1c[nH]c2ccc(F)cc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL64155 201454 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 708 14 4 6 6.3 O=C(CCC(=O)OCc1ccccc1)N[C@@H](CNC(=O)C(Cc1c[nH]c2ccc(F)cc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1016/S0960-894X(97)00356-9
54582313 61591 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc2ccccc2cc1N1CCN(C(=O)c2ncc(-c3ccc(OC)cc3)c(-c3ccc(C)cc3)n2)CC1 10.1016/j.bmcl.2011.03.069
CHEMBL1774039 61591 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc2ccccc2cc1N1CCN(C(=O)c2ncc(-c3ccc(OC)cc3)c(-c3ccc(C)cc3)n2)CC1 10.1016/j.bmcl.2011.03.069
10744359 10062 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 513 6 2 6 4.5 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc([N+](=O)[O-])c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL115833 10062 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 513 6 2 6 4.5 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc([N+](=O)[O-])c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
15689724 106116 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142696 106116 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44370497 164641 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 453 8 3 3 4.6 O=C(O)CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1 10.1021/jm00164a020
CHEMBL422873 164641 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 453 8 3 3 4.6 O=C(O)CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1 10.1021/jm00164a020
90663256 106148 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity against cholecystokinin type A receptor from rat pancreas binding assayInhibitory activity against cholecystokinin type A receptor from rat pancreas binding assay
ChEMBL 854 17 7 8 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CSC(C)(C)[C@H]1C(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00100a033
CHEMBL3143146 106148 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity against cholecystokinin type A receptor from rat pancreas binding assayInhibitory activity against cholecystokinin type A receptor from rat pancreas binding assay
ChEMBL 854 17 7 8 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CSC(C)(C)[C@H]1C(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00100a033
155521287 170011 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]CCK-8s from human CCKA incubated for 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human CCKA incubated for 60 mins by scintillation counting method
ChEMBL 478 7 0 6 4.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(F)c(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4450506 170011 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]CCK-8s from human CCKA incubated for 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human CCKA incubated for 60 mins by scintillation counting method
ChEMBL 478 7 0 6 4.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(F)c(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
44283081 99409 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 9 3 3 6.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(O)CCCc1ccccc1 10.1021/jm00086a017
CHEMBL2112071 99409 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 9 3 3 6.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(O)CCCc1ccccc1 10.1021/jm00086a017
CHEMBL285880 99409 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 9 3 3 6.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(O)CCCc1ccccc1 10.1021/jm00086a017
14208225 67412 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 3 3.9 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907855 67412 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 3 3.9 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208204 202760 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
CHEMBL72300 202760 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
14208204 202760 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00047a021
CHEMBL72300 202760 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00047a021
44376191 164773 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 452 4 3 6 2.8 CN1C(=O)[C@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL423472 164773 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 452 4 3 6 2.8 CN1C(=O)[C@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
10010890 108250 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 874 22 8 8 4.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL320858 108250 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 874 22 8 8 4.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
10409534 28028 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL137398 28028 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
10649606 49349 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
5311205 12983 1 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(N3CC4CCC(CC4)C3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL1190319 12983 1 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(N3CC4CCC(CC4)C3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL540596 12983 1 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(N3CC4CCC(CC4)C3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
54583260 61544 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773896 61544 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.03.069
11039097 79136 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 573 7 3 5 4.7 C[C@@H](c1ccccc1)N1C(=O)C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
CHEMBL2114084 79136 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 573 7 3 5 4.7 C[C@@H](c1ccccc1)N1C(=O)C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
24785177 189189 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1ccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL516113 189189 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1ccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL3142697 209387 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44373701 52211 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Compound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasCompound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 541 8 4 4 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N/C(=C\c1ccccc1)C(=O)O 10.1016/S0960-894X(01)81250-6
CHEMBL159138 52211 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Compound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasCompound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 541 8 4 4 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N/C(=C\c1ccccc1)C(=O)O 10.1016/S0960-894X(01)81250-6
9978327 78406 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 400 3 3 4 3.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2112753 78406 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 400 3 3 4 3.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
11765552 113131 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@@H](CNC(=O)CCC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm00017a022
CHEMBL332263 113131 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@@H](CNC(=O)CCC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm00017a022
44300888 100324 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 580 6 4 6 4.5 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(-c4nn[nH]n4)c3)C(=O)N(CC(=O)NC(C)(C)C)c3cc(C)ccc32)cc1 10.1016/0960-894X(95)00327-P
CHEMBL293107 100324 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 580 6 4 6 4.5 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(-c4nn[nH]n4)c3)C(=O)N(CC(=O)NC(C)(C)C)c3cc(C)ccc32)cc1 10.1016/0960-894X(95)00327-P
44348808 17753 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 451 7 3 4 3.9 O=C(O)CCC(NC(=O)c1ccc2ccccc2c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL125925 17753 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 451 7 3 4 3.9 O=C(O)CCC(NC(=O)c1ccc2ccccc2c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
71456207 78214 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 655 12 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1c[nH]nn1)c1ccccc1 10.1021/jm00092a007
CHEMBL2112331 78214 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 655 12 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1c[nH]nn1)c1ccccc1 10.1021/jm00092a007
9853654 22588 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00092a007
CHEMBL1328 22588 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00092a007
9853654 22588 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a062
CHEMBL1328 22588 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a062
15104627 109989 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 462 7 2 3 4.7 CN(Cc1ccccc1)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL324760 109989 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 462 7 2 3 4.7 CN(Cc1ccccc1)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
9853654 22588 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00057a005
CHEMBL1328 22588 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00057a005
44360121 116245 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 417 5 2 4 3.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(O)c1ccccc1 10.1021/jm00163a069
CHEMBL337530 116245 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 417 5 2 4 3.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(O)c1ccccc1 10.1021/jm00163a069
11742520 29413 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1ccccc1NC(=O)NC1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00078a018
CHEMBL138592 29413 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1ccccc1NC(=O)NC1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00078a018
10431936 92806 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL2448131 92806 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
14208198 103899 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 537 6 4 5 4.5 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL310246 103899 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 537 6 4 5 4.5 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
44349410 16598 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 394 7 3 3 3.5 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCCC1 10.1021/jm00079a003
CHEMBL124459 16598 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 394 7 3 3 3.5 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCCC1 10.1021/jm00079a003
15556550 67381 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 326 3 1 2 4.5 CC(C)C[C@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=O 10.1021/jm00390a019
CHEMBL1907736 67381 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 326 3 1 2 4.5 CC(C)C[C@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=O 10.1021/jm00390a019
11571172 140054 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm049072h
CHEMBL381347 140054 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm049072h
19018661 28271 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 442 5 3 4 3.3 CN1C(=O)C(NC(=O)Nc2cccc(CC(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137567 28271 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 442 5 3 4 3.3 CN1C(=O)C(NC(=O)Nc2cccc(CC(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10000984 116143 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3cnccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL336972 116143 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3cnccc3N(C)C2=O)c1 10.1021/jm00078a018
46235271 73301 2 None 2 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
10392523 206206 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL96970 206206 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
44280996 99283 0 None - 1 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 745 14 4 8 5.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL284976 99283 0 None - 1 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 745 14 4 8 5.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
15614737 75582 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 410 3 1 2 5.9 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=NC1Cc1ccc2ccccc2c1 10.1021/jm00390a019
CHEMBL20514 75582 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 410 3 1 2 5.9 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=NC1Cc1ccc2ccccc2c1 10.1021/jm00390a019
44303299 199566 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 598 11 4 6 5.5 CC(Cc1ccc(Oc2ccccc2)cc1)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)[C@H](O)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL60386 199566 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 598 11 4 6 5.5 CC(Cc1ccc(Oc2ccccc2)cc1)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)[C@H](O)c1ccccc1 10.1016/S0960-894X(97)00356-9
52949124 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
14208298 202927 1 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 465 3 1 3 4.2 CN1C(=O)C(NC(=O)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL73511 202927 1 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 465 3 1 3 4.2 CN1C(=O)C(NC(=O)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
44210425 164742 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 439 5 2 5 3.5 COc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL423278 164742 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 439 5 2 5 3.5 COc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1016/S0960-894X(00)80683-6
9960703 167475 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 621 6 3 7 4.0 O=C(Nc1cccc(-c2nn[nH]n2)c1)NC1N=C(c2ccccc2F)c2ccccc2N(CC(=O)N2CC3CCC(CC3)C2)C1=O 10.1016/s0960-894x(98)00237-6
CHEMBL432266 167475 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 621 6 3 7 4.0 O=C(Nc1cccc(-c2nn[nH]n2)c1)NC1N=C(c2ccccc2F)c2ccccc2N(CC(=O)N2CC3CCC(CC3)C2)C1=O 10.1016/s0960-894x(98)00237-6
44287087 99998 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 796 19 7 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL290719 99998 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 796 19 7 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44458113 167612 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 392 4 2 3 2.8 O=C(N[C@@H]1C(=O)N(c2ccccc2F)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL433222 167612 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 392 4 2 3 2.8 O=C(N[C@@H]1C(=O)N(c2ccccc2F)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
9872735 186444 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 567 5 2 4 5.1 Cc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3ccccc3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL49085 186444 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 567 5 2 4 5.1 Cc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3ccccc3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
44300852 101501 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 566 6 4 6 4.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL301418 101501 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 566 6 4 6 4.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
71458004 78218 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 670 12 5 8 4.7 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCn1nn[nH]c1=S)c1ccccc1 10.1021/jm00092a007
CHEMBL2112335 78218 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 670 12 5 8 4.7 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCn1nn[nH]c1=S)c1ccccc1 10.1021/jm00092a007
10323690 100032 0 None - 2 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
CHEMBL2114401 100032 0 None - 2 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
CHEMBL291033 100032 0 None - 2 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
14208299 67400 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 3 1 3 4.2 CN1C(=O)[C@@H](NC(=O)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907844 67400 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 3 1 3 4.2 CN1C(=O)[C@@H](NC(=O)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10416987 12103 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 539 5 2 4 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CC[N+](C)(C)CC3)C2=O)c1 10.1021/jm00078a018
CHEMBL1184312 12103 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 539 5 2 4 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CC[N+](C)(C)CC3)C2=O)c1 10.1021/jm00078a018
CHEMBL343949 12103 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 539 5 2 4 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CC[N+](C)(C)CC3)C2=O)c1 10.1021/jm00078a018
11607291 170451 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
CHEMBL445662 170451 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
44368594 120538 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 447 8 3 3 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1)C(=O)NCCc1ccccc1 10.1021/jm00057a005
CHEMBL356810 120538 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 447 8 3 3 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1)C(=O)NCCc1ccccc1 10.1021/jm00057a005
44349073 16380 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 395 7 3 4 2.5 CC1(C)CCN(NC(=O)C(CCC(=O)O)NC(=O)c2cccc(Cl)c2)CC1 10.1021/jm00079a003
CHEMBL123785 16380 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 395 7 3 4 2.5 CC1(C)CCN(NC(=O)C(CCC(=O)O)NC(=O)c2cccc(Cl)c2)CC1 10.1021/jm00079a003
11124446 78027 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@H]12 10.1021/jm010813d
CHEMBL2111552 78027 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@H]12 10.1021/jm010813d
14519981 9965 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00124a003
CHEMBL115269 9965 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00124a003
14519981 9965 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00116a002
CHEMBL115269 9965 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00116a002
44370694 47746 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL155017 47746 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
10348659 1774 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 604 8 2 5 5.4 O=C(NC1C(=O)N(c2ccccc2)c2c(N(C1=O)CC(=O)N(c1ccc(cc1)N(C)C)C(C)C)cccc2)Nc1ccccc1 10.1021/jm950626d
866 1774 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 604 8 2 5 5.4 O=C(NC1C(=O)N(c2ccccc2)c2c(N(C1=O)CC(=O)N(c1ccc(cc1)N(C)C)C(C)C)cccc2)Nc1ccccc1 10.1021/jm950626d
CHEMBL1184355 1774 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 604 8 2 5 5.4 O=C(NC1C(=O)N(c2ccccc2)c2c(N(C1=O)CC(=O)N(c1ccc(cc1)N(C)C)C(C)C)cccc2)Nc1ccccc1 10.1021/jm950626d
44306887 101591 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL302027 101591 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL355778 209993 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1C[C@H](CCc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
19910130 119286 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 439 14 3 3 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL348168 119286 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 439 14 3 3 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
44578398 181202 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc5ccccc45)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL477784 181202 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc5ccccc45)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL172177 207108 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1C[C@@H](Cc2ccccc2)NC(=O)[C@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44349064 16343 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 435 7 3 4 3.4 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL123684 16343 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 435 7 3 4 3.4 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
15167820 67372 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 393 3 0 3 4.6 CN1C(=O)[C@@H](Cc2cn(C)c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
CHEMBL1907724 67372 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 393 3 0 3 4.6 CN1C(=O)[C@@H](Cc2cn(C)c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
44327699 205749 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 641 15 2 5 7.2 COC(=O)CCCCCCN(CCc1ccccc1)C(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
CHEMBL94352 205749 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 641 15 2 5 7.2 COC(=O)CCCCCCN(CCc1ccccc1)C(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
52949124 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
44283086 118829 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 482 8 2 2 7.2 CC(/C=C/CCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL34422 118829 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 482 8 2 2 7.2 CC(/C=C/CCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10008405 118285 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL342110 118285 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL169174 207093 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
44333997 108272 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 588 10 3 5 5.3 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL320886 108272 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 588 10 3 5 5.3 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
10551234 96493 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 443 6 3 6 4.6 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
CHEMBL266120 96493 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 443 6 3 6 4.6 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
6956374 2373 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1021/jm000937a
902 2373 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1021/jm000937a
CHEMBL117281 2373 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1021/jm000937a
6956374 2373 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1016/S0960-894X(00)80684-8
902 2373 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1016/S0960-894X(00)80684-8
CHEMBL117281 2373 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1016/S0960-894X(00)80684-8
2118 201792 35 None - 2 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 308 1 0 4 3.6 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 10.1021/jm00396a028
CHEMBL661 201792 35 None - 2 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 308 1 0 4 3.6 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 10.1021/jm00396a028
CHEMBL2372078 208439 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@H]1CNC(=O)CNC(=O)[C@H](CCCNCc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2007.05.067
CHEMBL383458 210566 0 None -10 4 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
10409900 103381 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.
ChEMBL 420 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2C[C@@H](N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00234-K
CHEMBL30919 103381 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.
ChEMBL 420 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2C[C@@H](N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00234-K
44318205 204080 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 459 3 3 4 3.9 CN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)CCC3)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
CHEMBL83130 204080 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 459 3 3 4 3.9 CN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)CCC3)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
44303515 101623 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 571 9 2 5 5.3 CN(C)C(=O)c1oc2ccccc2c1CC(C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL302194 101623 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 571 9 2 5 5.3 CN(C)C(=O)c1oc2ccccc2c1CC(C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
10363545 204027 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL82685 204027 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
10363545 204027 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL82685 204027 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
90663984 106331 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 841 21 8 8 3.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144553 106331 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 841 21 8 8 3.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
118719193 114959 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 520 7 2 5 3.6 CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
CHEMBL3350871 114959 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 520 7 2 5 3.6 CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
CHEMBL3142685 209382 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None Cc1ccccc1NC(=O)NCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
10413618 201103 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/s0960-894x(00)00198-0
CHEMBL62205 201103 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/s0960-894x(00)00198-0
9983419 108899 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 499 8 3 3 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
CHEMBL321946 108899 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 499 8 3 3 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
10413618 201103 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL62205 201103 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
44280200 100357 0 None - 1 Mouse 6.2 pIC50 = 6.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 785 18 4 7 6.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL29331 100357 0 None - 1 Mouse 6.2 pIC50 = 6.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 785 18 4 7 6.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
10413618 201103 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1021/jm970065l
CHEMBL62205 201103 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1021/jm970065l
15719750 78074 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 446 9 3 3 4.0 O=C(O)CC[C@H](NC(=O)c1cccc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
CHEMBL2111825 78074 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 446 9 3 3 4.0 O=C(O)CC[C@H](NC(=O)c1cccc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
13605417 205834 3 None - 1 Guinea pig 7.2 pIC50 = 7.2 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
CHEMBL9485 205834 3 None - 1 Guinea pig 7.2 pIC50 = 7.2 Binding
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
54581301 61590 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 503 5 1 5 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5cc[nH]c5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774038 61590 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 503 5 1 5 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5cc[nH]c5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
15167812 101726 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 437 3 1 3 3.6 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)[N+]([O-])=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL302825 101726 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 437 3 1 3 3.6 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)[N+]([O-])=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
13605417 205834 3 None - 1 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00116a002
CHEMBL9485 205834 3 None - 1 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00116a002
44368382 45084 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 511 9 4 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL152682 45084 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 511 9 4 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
10480792 45543 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL153095 45543 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3350686 45543 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
136242438 78216 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 671 12 6 7 4.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1n[nH]c(=O)[nH]1)c1ccccc1 10.1021/jm00092a007
CHEMBL2112333 78216 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 671 12 6 7 4.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1n[nH]c(=O)[nH]1)c1ccccc1 10.1021/jm00092a007
10699165 110965 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 625 7 1 4 6.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(C(F)(F)F)cc1 10.1021/jm970265x
CHEMBL327552 110965 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 625 7 1 4 6.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(C(F)(F)F)cc1 10.1021/jm970265x
44211352 13872 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1196916 13872 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL558614 13872 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
11744065 78403 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 442 4 2 5 3.6 CC(=O)Oc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL2112750 78403 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 442 4 2 5 3.6 CC(=O)Oc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
15167809 67373 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 440 5 2 3 3.6 NC(=O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907725 67373 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 440 5 2 3 3.6 NC(=O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
135703408 142304 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assay
ChEMBL 511 4 2 6 6.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(O)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL389311 142304 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assay
ChEMBL 511 4 2 6 6.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(O)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
44349254 16654 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 354 10 3 3 2.6 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL124751 16654 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 354 10 3 3 2.6 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
23129945 9519 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 604 16 2 4 7.8 CCCCCN(CCCCC)C(=O)C(Cc1c[nH]c2ccc(OCc3ccccc3)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL112612 9519 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 604 16 2 4 7.8 CCCCCN(CCCCC)C(=O)C(Cc1c[nH]c2ccc(OCc3ccccc3)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
14888721 76884 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1055 30 11 14 -0.2 CSCC[C@H](NC(=O)[C@H](Cc1ccc(Cc2nnn[nH]2)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079551 76884 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1055 30 11 14 -0.2 CSCC[C@H](NC(=O)[C@H](Cc1ccc(Cc2nnn[nH]2)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL350222 209976 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)N(C)CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
22354599 193137 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 517 6 2 5 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccncc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL538912 193137 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 517 6 2 5 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccncc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
15104600 96639 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 515 13 2 2 7.0 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00116a002
CHEMBL267339 96639 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 515 13 2 2 7.0 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00116a002
10484212 99417 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL285921 99417 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
45482488 196628 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 441 7 4 3 4.2 Cc1cccc2cc(C(=O)Nc3ccccc3C(=O)NC(Cc3ccccc3)C(=O)O)[nH]c12 10.1016/j.bmc.2009.05.067
CHEMBL576021 196628 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 441 7 4 3 4.2 Cc1cccc2cc(C(=O)Nc3ccccc3C(=O)NC(Cc3ccccc3)C(=O)O)[nH]c12 10.1016/j.bmc.2009.05.067
44327458 206121 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 571 11 3 4 5.6 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL96469 206121 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 571 11 3 4 5.6 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
44379965 57533 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 496 6 2 5 5.5 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL167169 57533 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 496 6 2 5 5.5 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
44349335 116810 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 401 7 3 4 2.6 Cc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
CHEMBL339707 116810 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 401 7 3 4 2.6 Cc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
52949124 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10252366 25680 11 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 434 3 2 3 4.8 CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135364 25680 11 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 434 3 2 3 4.8 CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10649606 49349 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49349 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
70683295 73249 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 606 7 1 5 6.2 O=C(CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21)N1CCC(Cc2ccccc2)C1 10.1016/j.bmcl.2012.02.049
CHEMBL2017692 73249 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 606 7 1 5 6.2 O=C(CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21)N1CCC(Cc2ccccc2)C1 10.1016/j.bmcl.2012.02.049
73355866 204509 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for inhibition of CCK-A receptor by displacing [125I]-Bolton hunter CCK-8 radioligand in the rat pancreasCompound was evaluated for inhibition of CCK-A receptor by displacing [125I]-Bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 717 13 5 6 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNS(=O)(=O)C(F)(F)F)c1ccccc1 10.1021/jm00092a007
CHEMBL86702 204509 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for inhibition of CCK-A receptor by displacing [125I]-Bolton hunter CCK-8 radioligand in the rat pancreasCompound was evaluated for inhibition of CCK-A receptor by displacing [125I]-Bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 717 13 5 6 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNS(=O)(=O)C(F)(F)F)c1ccccc1 10.1021/jm00092a007
71454457 78213 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 655 12 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
CHEMBL2112330 78213 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 655 12 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
44370393 119139 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 492 14 2 3 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCCC1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL346784 119139 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 492 14 2 3 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCCC1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
15673149 85565 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 620 to 770The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 620 to 770
ChEMBL 717 13 5 6 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCNS(=O)(=O)C(F)(F)F)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304151 85565 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 620 to 770The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 620 to 770
ChEMBL 717 13 5 6 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCNS(=O)(=O)C(F)(F)F)c1ccccc1 10.1016/S0960-894X(00)80652-6
44349412 16686 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 396 12 3 3 3.6 CCCCC(CC)CNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL124917 16686 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 396 12 3 3 3.6 CCCCC(CC)CNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
10361419 26249 11 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 364 2 2 3 2.9 CN1C(=O)C(NC(=O)NC(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135988 26249 11 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 364 2 2 3 2.9 CN1C(=O)C(NC(=O)NC(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44303243 201236 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 545 9 5 5 4.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)[C@H](O)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL62832 201236 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 545 9 5 5 4.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)[C@H](O)c1ccccc1 10.1016/S0960-894X(97)00356-9
10507071 113111 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Inhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptorInhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptor
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL332261 113111 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Inhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptorInhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptor
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10553685 118646 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 508 8 3 5 4.2 COC[C@@H]1CCCN1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
CHEMBL342907 118646 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 508 8 3 5 4.2 COC[C@@H]1CCCN1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
9985100 114004 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2cccc(Cl)c2)c2ccccc21 10.1021/jm00048a015
CHEMBL333541 114004 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2cccc(Cl)c2)c2ccccc21 10.1021/jm00048a015
44368611 121480 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 541 10 4 3 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL359292 121480 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 541 10 4 3 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1021/jm00057a005
14208273 67396 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 457 7 1 3 5.1 CCCCCc1ccc(C(=O)N[C@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
CHEMBL1907840 67396 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 457 7 1 3 5.1 CCCCCc1ccc(C(=O)N[C@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
44334172 4501 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 556 10 3 5 4.9 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL102526 4501 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 556 10 3 5 4.9 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44379640 57282 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 522 6 2 5 5.8 CC(C)Oc1cccc(-n2c(C/N=C(\S)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL166737 57282 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 522 6 2 5 5.8 CC(C)Oc1cccc(-n2c(C/N=C(\S)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
44303470 201574 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 479 8 2 5 4.5 Cc1noc(C)c1CC(C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL64623 201574 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 479 8 2 5 4.5 Cc1noc(C)c1CC(C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL2372079 208440 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@H]1CNC(=O)CNC(=O)[C@H](CCNCc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2007.05.067
44286836 161176 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 810 19 6 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL41364 161176 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 810 19 6 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
15692562 109148 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 473 14 4 6 3.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc(O)c2cccc(O)c2n1 10.1021/jm00116a002
CHEMBL322284 109148 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 473 14 4 6 3.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc(O)c2cccc(O)c2n1 10.1021/jm00116a002
10700916 173864 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4553223 173864 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
46235271 73301 2 None 2 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2310858 207745 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None CCCC1CCN([C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(N)=O)[C@H]1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CCc1ccc(OS(=O)(=O)O)cc1 10.1021/jm00094a001
44293999 187841 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 597 6 2 5 5.1 COc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL50216 187841 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 597 6 2 5 5.1 COc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
9985667 162809 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1021/jm000959x
CHEMBL419237 162809 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1021/jm000959x
44293811 184536 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 601 5 2 4 5.8 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(Cl)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL48563 184536 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 601 5 2 4 5.8 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(Cl)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
9985667 162809 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL419237 162809 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
14590302 100968 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 444 4 1 4 4.3 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)c2ccc3ccccc3c2)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL297534 100968 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 444 4 1 4 4.3 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)c2ccc3ccccc3c2)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
367893 51344 1 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL158362 51344 1 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
10048986 27347 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 442 5 3 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)O)C2=O)c1 10.1021/jm00078a018
CHEMBL136919 27347 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 442 5 3 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)O)C2=O)c1 10.1021/jm00078a018
10816889 78430 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 570 8 3 6 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)[C@H](C#N)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
CHEMBL2112824 78430 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 570 8 3 6 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)[C@H](C#N)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
136046102 100210 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 864 20 9 10 3.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cnc2cccc(O)c2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL292298 100210 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 864 20 9 10 3.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cnc2cccc(O)c2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
11742839 12715 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)N[C@H]2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL1188361 12715 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)N[C@H]2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL536245 12715 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)N[C@H]2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
10074366 120087 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3349028 120087 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3545866 120087 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
15514020 78181 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 603 7 3 7 4.0 CC(=O)Oc1cccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)c1 10.1021/jm010813d
CHEMBL2112232 78181 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 603 7 3 7 4.0 CC(=O)Oc1cccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)c1 10.1021/jm010813d
14208234 202993 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 428 3 4 4 3.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(O)ccc2[nH]1 10.1021/jm00047a021
CHEMBL74066 202993 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 428 3 4 4 3.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(O)ccc2[nH]1 10.1021/jm00047a021
46235271 73301 2 None 2 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
14208270 67410 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 447 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907853 67410 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 447 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
13809511 101824 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 512 6 2 5 4.1 CN1C(=O)C(NC(=O)[C@@H](Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL303386 101824 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 512 6 2 5 4.1 CN1C(=O)C(NC(=O)[C@@H](Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
15060278 120285 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 633 12 3 5 6.5 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)OCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL355532 120285 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 633 12 3 5 6.5 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)OCc1ccccc1 10.1016/S0960-894X(00)80687-3
44329287 205901 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccc(F)cc3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL95209 205901 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccc(F)cc3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
10815039 112349 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 493 5 2 5 4.5 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL330917 112349 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 493 5 2 5 4.5 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
15614750 118818 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 426 4 3 3 3.9 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00163a069
CHEMBL344154 118818 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 426 4 3 3 3.9 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00163a069
10744557 32507 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 521 7 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1C(=O)O 10.1021/jm970065l
CHEMBL141370 32507 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 521 7 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1C(=O)O 10.1021/jm970065l
44372047 156588 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 854 20 7 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)N(C)C(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL407507 156588 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 854 20 7 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)N(C)C(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
16100410 141266 0 None -6309 4 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL386212 141266 0 None -6309 4 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
11803746 106131 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 870 21 9 10 3.0 COC(=O)c1ccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm960509y
CHEMBL3142904 106131 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 870 21 9 10 3.0 COC(=O)c1ccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm960509y
14208230 102734 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 446 3 3 3 4.5 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm00120a002
CHEMBL308414 102734 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 446 3 3 3 4.5 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm00120a002
14208234 202993 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 428 3 4 4 3.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(O)ccc2[nH]1 10.1021/jm00120a002
CHEMBL74066 202993 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 428 3 4 4 3.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(O)ccc2[nH]1 10.1021/jm00120a002
10053201 16415 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 546 6 3 3 5.9 CCc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL124004 16415 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 546 6 3 3 5.9 CCc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
90663986 106333 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 857 21 8 8 3.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144555 106333 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 857 21 8 8 3.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
90663994 106340 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 837 21 8 8 3.6 Cc1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
CHEMBL3144563 106340 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 837 21 8 8 3.6 Cc1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
44283030 99194 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 629 12 3 7 5.4 COC(=O)CCC(=O)N[C@H](COC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)c1ccccc1 10.1021/jm00086a017
CHEMBL284361 99194 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 629 12 3 7 5.4 COC(=O)CCC(=O)N[C@H](COC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)c1ccccc1 10.1021/jm00086a017
11607229 139907 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)[C@@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm049072h
CHEMBL380922 139907 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)[C@@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm049072h
44370451 50518 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL157658 50518 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
19754255 58798 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 340 2 2 3 4.4 Cn1c(C(=O)Nc2cc3c4ccccc4nc-3c[nH]2)cc2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL169767 58798 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 340 2 2 3 4.4 Cn1c(C(=O)Nc2cc3c4ccccc4nc-3c[nH]2)cc2ccccc21 10.1016/S0960-894X(00)80682-4
10094721 205167 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 439 5 3 7 3.5 CN(C)c1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9083 205167 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 439 5 3 7 3.5 CN(C)c1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
19754256 59294 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 287 2 2 2 3.9 O=C(Nc1cc2c3ccccc3nc-2c[nH]1)c1ccccc1 10.1016/S0960-894X(00)80682-4
CHEMBL171940 59294 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 287 2 2 2 3.9 O=C(Nc1cc2c3ccccc3nc-2c[nH]1)c1ccccc1 10.1016/S0960-894X(00)80682-4
10325557 46245 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 563 9 4 4 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@@H]3C[C@@H](C[C@@H](C3)C1)C2Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL153760 46245 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 563 9 4 4 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@@H]3C[C@@H](C[C@@H](C3)C1)C2Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
53465907 69070 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 441 8 4 3 4.7 O=C(Nc1ccccc1NC(=O)C(CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933109 69070 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 441 8 4 3 4.7 O=C(Nc1ccccc1NC(=O)C(CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
44381830 59024 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 610 15 6 7 2.5 N#C[C@H](N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
CHEMBL170664 59024 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 610 15 6 7 2.5 N#C[C@H](N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
10051647 116782 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2C(C)C 10.1021/jm00048a015
CHEMBL339547 116782 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2C(C)C 10.1021/jm00048a015
21842400 120461 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 496 7 2 4 5.3 CCC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccc2)c2ccccc21 10.1016/0960-894X(95)00556-9
CHEMBL356191 120461 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 496 7 2 4 5.3 CCC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccc2)c2ccccc21 10.1016/0960-894X(95)00556-9
10816869 51576 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Compound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasCompound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 569 8 3 5 5.2 COC(=O)[C@]1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
CHEMBL158547 51576 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Compound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasCompound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 569 8 3 5 5.2 COC(=O)[C@]1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
20063261 22923 12 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 412 3 2 3 4.3 Cc1cc(C)cc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL133087 22923 12 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 412 3 2 3 4.3 Cc1cc(C)cc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
44280713 99570 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 740 15 6 9 3.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL286907 99570 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 740 15 6 9 3.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
44382486 59108 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 518 11 4 4 2.8 CCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
CHEMBL171051 59108 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 518 11 4 4 2.8 CCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
CHEMBL2372081 208442 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@H]1CNC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2007.05.067
44303650 100312 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 548 6 2 3 6.4 O=C(NC1(C(=O)NCCc2ccccc2)CC2(Cc3cccc4cccc(c34)C2)C1)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(97)00356-9
CHEMBL292956 100312 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 548 6 2 3 6.4 O=C(NC1(C(=O)NCCc2ccccc2)CC2(Cc3cccc4cccc(c34)C2)C1)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(97)00356-9
44349354 118046 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 415 8 3 4 2.9 CCc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
CHEMBL341505 118046 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 415 8 3 4 2.9 CCc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
14208267 202821 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 380 3 2 4 3.1 N#Cc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL72710 202821 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 380 3 2 4 3.1 N#Cc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
10350069 9879 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@@H](CNC(=O)CCC(=O)O)NC(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm00017a022
CHEMBL114774 9879 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@@H](CNC(=O)CCC(=O)O)NC(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm00017a022
44348902 155221 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1000 24 11 11 2.3 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)ccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL405805 155221 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1000 24 11 11 2.3 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)ccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
44300862 157330 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 695 9 4 6 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)Cc3ccccc3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL408392 157330 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 695 9 4 6 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)Cc3ccccc3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
14208267 202821 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 380 3 2 4 3.1 N#Cc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL72710 202821 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 380 3 2 4 3.1 N#Cc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
10761732 75593 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 371 4 3 5 3.5 O=C(NNc1nc2ccccc2c(=O)n1-c1ccccc1)Nc1ccccc1 10.1021/jm970373j
CHEMBL2051984 75593 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 371 4 3 5 3.5 O=C(NNc1nc2ccccc2c(=O)n1-c1ccccc1)Nc1ccccc1 10.1021/jm970373j
44349314 16390 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 402 8 3 3 3.5 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00079a003
CHEMBL123852 16390 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 402 8 3 3 3.5 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00079a003
5311201 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL9387 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
5311201 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00530-0
CHEMBL9387 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00530-0
5311201 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
CHEMBL9387 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
5311201 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm9506736
CHEMBL9387 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm9506736
5311201 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL9387 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
44376130 56043 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 398 3 2 3 4.0 Cc1ccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00032a003
CHEMBL163049 56043 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 398 3 2 3 4.0 Cc1ccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00032a003
44280599 98705 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreas
ChEMBL 694 12 4 5 6.2 O=C(O)CC[C@H](NC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)C(=O)Nc1cccc2ccccc12 10.1021/jm950372w
CHEMBL281206 98705 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreas
ChEMBL 694 12 4 5 6.2 O=C(O)CC[C@H](NC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)C(=O)Nc1cccc2ccccc12 10.1021/jm950372w
5311201 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm970373j
CHEMBL9387 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm970373j
14802510 114619 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 629 13 4 6 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](COC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL334346 114619 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 629 13 4 6 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](COC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
44368298 120515 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 613 13 4 5 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](COC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL356599 120515 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 613 13 4 5 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](COC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
43811299 116160 11 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 452 3 2 3 4.7 CN1C(=O)C(NC(=O)Nc2cccc(C(F)(F)F)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL337055 116160 11 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 452 3 2 3 4.7 CN1C(=O)C(NC(=O)Nc2cccc(C(F)(F)F)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
5311201 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL9387 205663 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
44281205 114320 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 857 17 4 10 5.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL33412 114320 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 857 17 4 10 5.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
90663256 106148 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity against cholecystokinin type A receptor from bovine striatal binding assayInhibitory activity against cholecystokinin type A receptor from bovine striatal binding assay
ChEMBL 854 17 7 8 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CSC(C)(C)[C@H]1C(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00100a033
CHEMBL3143146 106148 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity against cholecystokinin type A receptor from bovine striatal binding assayInhibitory activity against cholecystokinin type A receptor from bovine striatal binding assay
ChEMBL 854 17 7 8 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CSC(C)(C)[C@H]1C(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00100a033
CHEMBL2372080 208441 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@H]1CNC(=O)CNC(=O)[C@H](CNCc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2007.05.067
10504136 204912 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 459 7 3 7 4.3 COc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
CHEMBL8922 204912 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 459 7 3 7 4.3 COc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
44286835 99821 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 796 20 8 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL289036 99821 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 796 20 8 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
9916170 76200 2 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 575 10 4 4 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccc(F)cc1 10.1016/s0960-894x(00)00198-0
CHEMBL2062146 76200 2 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 575 10 4 4 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccc(F)cc1 10.1016/s0960-894x(00)00198-0
10462874 98380 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 766 16 6 5 7.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCCNC(=O)Nc1ccccc1Cl 10.1016/S0960-894X(00)80687-3
CHEMBL278780 98380 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 766 16 6 5 7.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCCNC(=O)Nc1ccccc1Cl 10.1016/S0960-894X(00)80687-3
10074366 120087 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3349028 120087 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3545866 120087 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
10031013 204758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Cholecystokinin type A receptorBinding affinity against human Cholecystokinin type A receptor
ChEMBL 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
CHEMBL88239 204758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Cholecystokinin type A receptorBinding affinity against human Cholecystokinin type A receptor
ChEMBL 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
10031013 204758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
CHEMBL88239 204758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
10031013 204758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assayDisplacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assay
ChEMBL 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
CHEMBL88239 204758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assayDisplacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assay
ChEMBL 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
44286655 99394 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 808 16 6 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(=O)N(C(Cc2ccccc2)C(N)=O)CC1 10.1021/jm00037a005
CHEMBL285772 99394 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 808 16 6 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(=O)N(C(Cc2ccccc2)C(N)=O)CC1 10.1021/jm00037a005
44329384 206590 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 556 7 3 4 5.6 COc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
CHEMBL99289 206590 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 556 7 3 4 5.6 COc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
89913304 140240 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 249 2 1 2 2.0 O=C1C=C(Cl)C(O)(c2ccccc2)N1C1CC1 10.1039/C6MD00052E
CHEMBL3818437 140240 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 249 2 1 2 2.0 O=C1C=C(Cl)C(O)(c2ccccc2)N1C1CC1 10.1039/C6MD00052E
5279123 202836 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00120a002
CHEMBL72841 202836 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00120a002
15614763 67424 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to rat pancreas cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to rat pancreas cholecystokinin receptor
ChEMBL 401 3 3 2 5.1 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)N[C@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
CHEMBL1907932 67424 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to rat pancreas cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to rat pancreas cholecystokinin receptor
ChEMBL 401 3 3 2 5.1 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)N[C@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
5279123 202836 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00047a021
CHEMBL72841 202836 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00047a021
14991538 106343 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 921 24 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144566 106343 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 921 24 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
52949124 863 2 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counterDisplacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counterDisplacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counterDisplacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counterDisplacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10481933 13185 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 524 5 2 5 3.1 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1021/jm00078a018
CHEMBL1191818 13185 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 524 5 2 5 3.1 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1021/jm00078a018
CHEMBL542967 13185 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 524 5 2 5 3.1 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1021/jm00078a018
44279808 98684 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 712 13 6 9 2.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL281082 98684 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 712 13 6 9 2.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
10369804 16581 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1cccc2c1N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL124340 16581 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1cccc2c1N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
9984452 164751 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 529 9 4 4 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL423329 164751 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 529 9 4 4 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
44283055 116112 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 690-850Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 690-850
ChEMBL 515 9 4 4 4.4 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80156-0
CHEMBL336769 116112 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 690-850Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 690-850
ChEMBL 515 9 4 4 4.4 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80156-0
14208282 67344 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 363 5 1 3 3.4 CC(C)CCC(=O)N[C@H]1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00120a002
CHEMBL1907663 67344 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 363 5 1 3 3.4 CC(C)CCC(=O)N[C@H]1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00120a002
9984452 164751 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 529 9 4 4 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00105a062
CHEMBL423329 164751 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 529 9 4 4 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00105a062
15177358 52940604 16353 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 667 9 4 4 7.1 ClC(Cl)(Cl)Cl.O=C(NC(Cc1c[nH]c2ccccc12)NC(=O)C(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL1237153 16353 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 667 9 4 4 7.1 ClC(Cl)(Cl)Cl.O=C(NC(Cc1c[nH]c2ccccc12)NC(=O)C(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
44368624 120620 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 513 9 4 3 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL357564 120620 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 513 9 4 3 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
9984452 29501 0 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 529 9 4 4 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm970065l
CHEMBL138657 29501 0 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 529 9 4 4 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm970065l
44368329 120490 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 499 8 3 3 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3)C(=O)NCCc1ccccc1 10.1021/jm00057a005
CHEMBL356446 120490 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 499 8 3 3 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3)C(=O)NCCc1ccccc1 10.1021/jm00057a005
10483574 6129 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 591 8 2 5 5.3 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm950626d
CHEMBL108130 6129 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 591 8 2 5 5.3 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm950626d
73351320 105666 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 681 12 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNC(=O)C(F)(F)F)c1ccccc1 10.1021/jm00092a007
CHEMBL313559 105666 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 681 12 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNC(=O)C(F)(F)F)c1ccccc1 10.1021/jm00092a007
6439414 2976 11 None -2454 2 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 10.1021/jm00105a062
867 2976 11 None -2454 2 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 10.1021/jm00105a062
CHEMBL3351022 2976 11 None -2454 2 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 10.1021/jm00105a062
CHEMBL341460 2976 11 None -2454 2 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 10.1021/jm00105a062
44368728 119001 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 596 11 5 4 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)/C=C/C(=O)O)c1ccccc1 10.1021/jm00057a005
CHEMBL345512 119001 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 596 11 5 4 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)/C=C/C(=O)O)c1ccccc1 10.1021/jm00057a005
14208306 202486 1 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL70791 202486 1 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
44451577 95341 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity to mouse CCK1 receptorBinding affinity to mouse CCK1 receptor
ChEMBL 546 6 2 5 2.1 Cc1cccc(NC(=O)NC2C(=O)N(CC(=O)N3CCCC3)c3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
CHEMBL258630 95341 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity to mouse CCK1 receptorBinding affinity to mouse CCK1 receptor
ChEMBL 546 6 2 5 2.1 Cc1cccc(NC(=O)NC2C(=O)N(CC(=O)N3CCCC3)c3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
52949124 863 2 None -2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
46235271 73301 2 None 2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
15689723 106113 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C(F)(F)F)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142693 106113 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C(F)(F)F)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
89913313 140259 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 299 3 1 2 3.1 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
CHEMBL3818718 140259 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 299 3 1 2 3.1 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
443375 205872 40 None -3 5 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00163a069
CHEMBL9506 205872 40 None -3 5 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00163a069
44578305 180588 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 5 0 5 6.1 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc(Cl)c(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476095 180588 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 5 0 5 6.1 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc(Cl)c(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
14991571 201247 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 905 21 8 10 3.9 CC(=O)Oc1ccc2cc(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)ccc2c1 10.1021/jm00089a010
CHEMBL62887 201247 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 905 21 8 10 3.9 CC(=O)Oc1ccc2cc(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)ccc2c1 10.1021/jm00089a010
104929 2189 8 None - 3 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00121a004
3477 2189 8 None - 3 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00121a004
879 2189 8 None - 3 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00121a004
CHEMBL289498 2189 8 None - 3 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00121a004
10009894 25424 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 694 13 6 6 4.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@@H](NC(=O)OCc3ccccc3)C(=O)N21 10.1016/s0960-894x(01)00630-8
CHEMBL13517 25424 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 694 13 6 6 4.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@@H](NC(=O)OCc3ccccc3)C(=O)N21 10.1016/s0960-894x(01)00630-8
10070679 27560 11 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)C(NC(=O)Nc2cccc(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137066 27560 11 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)C(NC(=O)Nc2cccc(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL407530 210920 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
14208194 162884 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm000937a
CHEMBL419764 162884 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm000937a
14208243 202712 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL72073 202712 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14208194 162884 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL419764 162884 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
10452597 26720 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 384 3 2 3 3.6 CN1C(=O)C(NC(=O)Nc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136408 26720 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 384 3 2 3 3.6 CN1C(=O)C(NC(=O)Nc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14208243 202712 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL72073 202712 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
14208194 162884 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
CHEMBL419764 162884 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
14208243 202712 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL72073 202712 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
10817395 106658 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 600 8 1 4 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
CHEMBL316164 106658 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 600 8 1 4 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
10817395 106658 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 600 8 1 4 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL316164 106658 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 600 8 1 4 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
15689727 106111 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc(Cl)cc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142690 106111 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc(Cl)cc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44578455 181873 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL478630 181873 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
10480792 45543 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL153095 45543 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3350686 45543 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
14208210 202502 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 413 3 2 4 4.1 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2o1 10.1021/jm00047a021
CHEMBL70856 202502 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 413 3 2 4 4.1 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2o1 10.1021/jm00047a021
21842365 119249 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 495 6 2 5 4.5 Cc1cccc(NC(=O)NC2N=C(c3cccnc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL347843 119249 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 495 6 2 5 4.5 Cc1cccc(NC(=O)NC2N=C(c3cccnc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00557-A
11765257 108345 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL320980 108345 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
46234820 73292 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 572 6 1 5 6.1 CC(C)C1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017826 73292 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 572 6 1 5 6.1 CC(C)C1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL328422 209550 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None Cc1cccc(C)c1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
89913684 140238 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 299 3 1 2 3.0 O=C1C=C(Cl)C(O)(c2ccccc2)N1Cc1ccccc1 10.1039/C6MD00052E
CHEMBL3818410 140238 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 299 3 1 2 3.0 O=C1C=C(Cl)C(O)(c2ccccc2)N1Cc1ccccc1 10.1039/C6MD00052E
14208307 77471 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL2092867 77471 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208283 67343 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 375 3 1 3 3.5 CN1C(=O)[C@@H](NC(=O)C2CCCCC2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907662 67343 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 375 3 1 3 3.5 CN1C(=O)[C@@H](NC(=O)C2CCCCC2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
20190197 31304 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 421 4 1 3 4.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1ccc(Cl)cc1 10.1021/jm00163a069
CHEMBL140365 31304 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 421 4 1 3 4.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1ccc(Cl)cc1 10.1021/jm00163a069
10075052 189082 0 None - 2 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL515268 189082 0 None - 2 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL515288 189082 0 None - 2 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44334320 4954 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 531 9 2 4 4.6 Cc1cccc(NC(=O)N[C@H](C[S+]([O-])Cc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL105132 4954 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 531 9 2 4 4.6 Cc1cccc(NC(=O)N[C@H](C[S+]([O-])Cc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
15673150 85567 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 680 to 970The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 680 to 970
ChEMBL 681 12 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCNC(=O)C(F)(F)F)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304154 85567 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 680 to 970The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 680 to 970
ChEMBL 681 12 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCNC(=O)C(F)(F)F)c1ccccc1 10.1016/S0960-894X(00)80652-6
44349413 112608 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 410 12 3 3 4.0 CCC(CC)(CC)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL331413 112608 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 410 12 3 3 4.0 CCC(CC)(CC)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
44360216 32016 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 5 3 4 3.3 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)C(O)c1ccccc1 10.1021/jm00163a069
CHEMBL140974 32016 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 5 3 4 3.3 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)C(O)c1ccccc1 10.1021/jm00163a069
44349240 117614 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 368 11 3 3 3.0 CCCCCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL340755 117614 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 368 11 3 3 3.0 CCCCCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
9800177 67367 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 383 3 2 2 4.7 O=C1Nc2ccccc2C(c2ccccc2F)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
CHEMBL1907714 67367 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 383 3 2 2 4.7 O=C1Nc2ccccc2C(c2ccccc2F)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
15614841 67379 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 390 5 1 3 4.7 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1COCc1ccccc1 10.1021/jm00390a019
CHEMBL1907734 67379 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 390 5 1 3 4.7 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1COCc1ccccc1 10.1021/jm00390a019
CHEMBL286843 99560 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 541 8 3 4 7.2 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C1NC=C(CCc2ccccc2)S1 10.1021/jm00086a017
10480605 77957 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 487 5 4 7 3.7 Cc1ccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)cc1Nc1nn[nH]n1 10.1021/jm9506736
CHEMBL2110201 77957 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 487 5 4 7 3.7 Cc1ccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)cc1Nc1nn[nH]n1 10.1021/jm9506736
44349411 16664 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 380 7 3 3 3.1 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCC1 10.1021/jm00079a003
CHEMBL124802 16664 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 380 7 3 3 3.1 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCC1 10.1021/jm00079a003
44283159 99672 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 515 8 3 3 6.6 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)/C(S)=N/CCc1ccccc1 10.1021/jm00086a017
CHEMBL287682 99672 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 515 8 3 3 6.6 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)/C(S)=N/CCc1ccccc1 10.1021/jm00086a017
44331065 106742 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 974 25 8 11 1.3 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL316709 106742 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 974 25 8 11 1.3 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
15667015 161305 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 29 10 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL414793 161305 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 29 10 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
14208253 203003 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(Cl)c1 10.1021/jm00120a002
CHEMBL74125 203003 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(Cl)c1 10.1021/jm00120a002
14208253 203003 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(Cl)c1 10.1021/jm00047a021
CHEMBL74125 203003 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(Cl)c1 10.1021/jm00047a021
14802508 78381 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 615 12 4 6 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC(OC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL2112695 78381 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 615 12 4 6 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC(OC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
15104629 109630 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 462 7 3 3 4.9 C[C@@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
CHEMBL323627 109630 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 462 7 3 3 4.9 C[C@@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
14720386 48060 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 463 12 2 4 4.4 CCCN(CCC)C(=O)[C@H](CCC(=O)OCc1ccccc1)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL155406 48060 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 463 12 2 4 4.4 CCCN(CCC)C(=O)[C@H](CCC(=O)OCc1ccccc1)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
44329055 206225 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 554 7 3 3 6.1 CCc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
CHEMBL97133 206225 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 554 7 3 3 6.1 CCc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
44382706 58711 1 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 475 3 2 2 5.9 O=C1NN(C(=S)Nc2ccc(Cl)c(C(F)(F)F)c2)[C@@H](c2ccccc2)[C@@H]1c1ccccc1 10.1016/S0960-894X(00)80684-8
CHEMBL169274 58711 1 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 475 3 2 2 5.9 O=C1NN(C(=S)Nc2ccc(Cl)c(C(F)(F)F)c2)[C@@H](c2ccccc2)[C@@H]1c1ccccc1 10.1016/S0960-894X(00)80684-8
11667741 194907 0 None - 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCKalpha receptorInhibition of CCKalpha receptor
ChEMBL 366 4 1 5 2.5 Cc1c(CC(=O)O)c2cccnc2n1S(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.042
CHEMBL563949 194907 0 None - 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCKalpha receptorInhibition of CCKalpha receptor
ChEMBL 366 4 1 5 2.5 Cc1c(CC(=O)O)c2cccnc2n1S(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.042
10528465 96603 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 473 7 4 7 4.0 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(=O)O)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL267023 96603 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 473 7 4 7 4.0 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(=O)O)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL2369769 207940 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasConcentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL None None None C/C=C/CC[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/0960-894X(94)85022-4
11700447 72678 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
CHEMBL200953 72678 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
13953716 101126 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 442 3 2 5 4.9 Cc1nnc2n1-c1ccccc1C(c1ccccc1)=NC2NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00396a028
CHEMBL298705 101126 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 442 3 2 5 4.9 Cc1nnc2n1-c1ccccc1C(c1ccccc1)=NC2NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00396a028
44281292 114296 0 None - 1 Mouse 5.1 pIC50 = 5.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 816 17 5 9 5.0 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCNC(=O)CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL33398 114296 0 None - 1 Mouse 5.1 pIC50 = 5.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 816 17 5 9 5.0 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCNC(=O)CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44329456 110957 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 526 6 3 3 5.5 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL327526 110957 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 526 6 3 3 5.5 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
10995425 114958 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=S)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm010898i
CHEMBL3350859 114958 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=S)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm010898i
44592486 187244 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 393 7 4 3 3.6 CC(C)CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL496067 187244 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 393 7 4 3 3.6 CC(C)CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
155557285 173946 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1779 74 19 22 1.6 CCCC[C@H](NC(=O)[C@H](CNC(=O)CCCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4555341 173946 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1779 74 19 22 1.6 CCCC[C@H](NC(=O)[C@H](CNC(=O)CCCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44373702 119421 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Compound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasCompound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 555 8 4 4 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@]1(C(=O)O)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
CHEMBL349473 119421 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Compound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasCompound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 555 8 4 4 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@]1(C(=O)O)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
44286696 167422 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 796 18 6 7 4.4 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL431912 167422 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 796 18 6 7 4.4 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL170026 207097 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
10004579 78107 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 462 3 2 3 4.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(Br)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2111923 78107 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 462 3 2 3 4.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(Br)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
15281997 48238 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 486 5 2 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3nccn3C)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL155627 48238 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 486 5 2 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3nccn3C)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL2369762 207935 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasConcentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL None None None CCCCC[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/0960-894X(94)85022-4
44209152 58850 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 336 2 3 2 5.0 O=C(Nc1ccc(Cl)cc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
CHEMBL169953 58850 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 336 2 3 2 5.0 O=C(Nc1ccc(Cl)cc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
73349792 156872 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 669 13 5 7 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCSc1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
CHEMBL407857 156872 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 669 13 5 7 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCSc1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
44354100 116269 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL337661 116269 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
44354100 120298 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL355656 120298 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
101823779 1369 29 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
16162108 1369 29 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
8408 1369 29 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
CHEMBL4451154 1369 29 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
44408632 157692 0 None -3630 4 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL408832 157692 0 None -3630 4 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
44283055 99295 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 515 9 4 4 4.4 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL285049 99295 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 515 9 4 4 4.4 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
44591979 178482 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 426 7 4 3 3.2 NC(=O)C(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL471465 178482 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 426 7 4 3 3.2 NC(=O)C(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
54587151 61537 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 545 6 0 7 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1OC 10.1016/j.bmcl.2011.03.069
CHEMBL1773889 61537 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 545 6 0 7 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1OC 10.1016/j.bmcl.2011.03.069
5311201 205663 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00327-P
CHEMBL9387 205663 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00327-P
5311201 205663 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00048a015
CHEMBL9387 205663 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00048a015
5311201 205663 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL9387 205663 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL2111881 207476 0 None - 0 Guinea pig 5.1 pIC50 = 5.1 Binding
Binding affinity towards Cholecystokinin type A receptor was determined in guinea pig pancreatic membranes using [125I]-BH-CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor was determined in guinea pig pancreatic membranes using [125I]-BH-CCK-8 as radioligand
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)[C@H](C)c1c[nH]c2ccccc12 10.1021/jm960078j
CHEMBL2111882 207477 0 None - 0 Guinea pig 5.1 pIC50 = 5.1 Binding
Binding affinity towards Cholecystokinin type A receptor was determined in guinea pig pancreatic membranes using [125I]-BH-CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor was determined in guinea pig pancreatic membranes using [125I]-BH-CCK-8 as radioligand
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)[C@@H](C)c1c[nH]c2ccccc12 10.1021/jm960078j
44349278 16429 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 388 10 3 3 3.3 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00079a003
CHEMBL124090 16429 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 388 10 3 3 3.3 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00079a003
44283177 99840 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 655 16 2 5 7.6 CCOC(=O)CCCCCC(=O)N(CCc1ccccc1)CC(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL289239 99840 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 655 16 2 5 7.6 CCOC(=O)CCCCCC(=O)N(CCc1ccccc1)CC(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
44283085 99444 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 484 9 2 2 7.4 CC(CCCCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL286093 99444 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 484 9 2 2 7.4 CC(CCCCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
14208239 202793 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 398 4 3 3 4.2 O=C1Nc2ccccc2C(c2ccccc2F)=NC1NCc1cc2ccccc2[nH]1 10.1021/jm00120a002
CHEMBL72550 202793 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 398 4 3 3 4.2 O=C1Nc2ccccc2C(c2ccccc2F)=NC1NCc1cc2ccccc2[nH]1 10.1021/jm00120a002
10698051 204805 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 557 7 1 4 5.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
CHEMBL88545 204805 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 557 7 1 4 5.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
10698051 204805 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 557 7 1 4 5.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm970265x
CHEMBL88545 204805 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 557 7 1 4 5.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm970265x
70683305 73300 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 635 7 1 6 6.4 Cc1cccc(CC2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL2017834 73300 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 635 7 1 6 6.4 Cc1cccc(CC2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
14802543 169911 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 600 11 5 5 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@H](NC(=O)CC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL2112693 169911 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 600 11 5 5 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@H](NC(=O)CC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL444902 169911 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 600 11 5 5 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@H](NC(=O)CC(=O)O)c1ccccc1 10.1021/jm00105a062
44336539 5075 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]BDZ1 from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5075 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]BDZ1 from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
44349044 112808 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1021/jm000959x
CHEMBL331532 112808 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1021/jm000959x
44349044 112808 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL331532 112808 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
15104617 9908 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2ccccc2cn1 10.1021/jm00116a002
CHEMBL114916 9908 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2ccccc2cn1 10.1021/jm00116a002
14720390 49125 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL156415 49125 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
44349429 16658 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 406 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)C1CC2CCCCC2CN1 10.1021/jm00079a003
CHEMBL124780 16658 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 406 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)C1CC2CCCCC2CN1 10.1021/jm00079a003
23928173 113649 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 511 6 2 5 4.7 CN(C)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL332931 113649 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 511 6 2 5 4.7 CN(C)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
44381949 120212 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 474 3 3 4 4.6 CN1C(=O)[C@H](NC(=O)Nc2cc3c4ccccc4nc-3c[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL354802 120212 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 474 3 3 4 4.6 CN1C(=O)[C@H](NC(=O)Nc2cc3c4ccccc4nc-3c[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
14208209 163353 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 402 5 3 4 3.2 O=C(CNc1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL420722 163353 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 402 5 3 4 3.2 O=C(CNc1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00047a021
10841112 205367 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 588 8 0 6 6.1 COc1ccc(N(C(=O)CN2C(=O)C(Cc3noc4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL91986 205367 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 588 8 0 6 6.1 COc1ccc(N(C(=O)CN2C(=O)C(Cc3noc4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10048206 196978 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 428 7 3 4 4.1 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2o1 10.1016/j.bmc.2009.05.067
CHEMBL579245 196978 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 428 7 3 4 4.1 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2o1 10.1016/j.bmc.2009.05.067
10674604 167365 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 571 6 1 4 6.3 CC(C)(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm970265x
CHEMBL431451 167365 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 571 6 1 4 6.3 CC(C)(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm970265x
16100408 141259 0 None -1202 3 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL386186 141259 0 None -1202 3 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
14208210 202502 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 413 3 2 4 4.1 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2o1 10.1021/jm00120a002
CHEMBL70856 202502 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 413 3 2 4 4.1 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2o1 10.1021/jm00120a002
14208268 202779 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 418 3 2 4 3.5 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL72428 202779 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 418 3 2 4 3.5 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
10073533 22354 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 472 7 3 5 3.5 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCC(=O)O)C2=O)c1 10.1021/jm00078a018
CHEMBL132603 22354 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 472 7 3 5 3.5 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCC(=O)O)C2=O)c1 10.1021/jm00078a018
155543846 172641 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1838 72 19 24 2.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4522865 172641 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1838 72 19 24 2.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.8b01558
10484212 99417 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL285921 99417 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL3142923 209391 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None COc1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
53465844 69068 0 None - 2 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None - 2 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL208479 207455 0 None -3 4 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
46235272 73298 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 589 8 1 7 4.9 COCCC1CCCCN1C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017832 73298 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 589 8 1 7 4.9 COCCC1CCCCN1C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
54586175 61589 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 504 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccoc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774037 61589 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 504 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccoc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
15667018 157240 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 998 27 10 11 2.5 CCCC[C@H](NC(=O)c1ccc2cc(OS(=O)(=O)O)ccc2c1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL408286 157240 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 998 27 10 11 2.5 CCCC[C@H](NC(=O)c1ccc2cc(OS(=O)(=O)O)ccc2c1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
14208212 102478 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 396 3 3 4 3.0 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)C1Cc2ccccc2N1 10.1021/jm00120a002
CHEMBL306369 102478 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 396 3 3 4 3.0 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)C1Cc2ccccc2N1 10.1021/jm00120a002
44311593 102546 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 402 3 2 3 3.8 CN(C(=O)NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00120a002
CHEMBL306958 102546 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 402 3 2 3 3.8 CN(C(=O)NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00120a002
11114607 114953 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 591 7 3 5 5.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=S)N(Cc3ccccc3)C(=S)C[C@H]12 10.1021/jm010898i
CHEMBL3350852 114953 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 591 7 3 5 5.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=S)N(Cc3ccccc3)C(=S)C[C@H]12 10.1021/jm010898i
19018662 26307 11 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 424 3 2 3 4.1 CN1C(=O)C(NC(=O)Nc2ccc3c(c2)CCC3)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136038 26307 11 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 424 3 2 3 4.1 CN1C(=O)C(NC(=O)Nc2ccc3c(c2)CCC3)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10436569 77492 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
CHEMBL2092976 77492 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
44280224 104305 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 757 16 4 7 5.8 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL31090 104305 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 757 16 4 7 5.8 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
44334337 4607 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 541 10 2 5 5.1 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL103276 4607 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 541 10 2 5 5.1 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL34853 209968 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards Cholecystokinin type A receptor by displacement of [125I]BH-CCK-8 from rat pancreatic aciniBinding affinity towards Cholecystokinin type A receptor by displacement of [125I]BH-CCK-8 from rat pancreatic acini
ChEMBL None None None CCS[C@H]1CCN(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(C)=O)[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00001a019
14208300 77470 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 3 1 3 4.2 CN1C(=O)[C@H](NC(=O)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL2092866 77470 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 3 1 3 4.2 CN1C(=O)[C@H](NC(=O)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10474221 16670 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 368 8 3 3 2.9 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL124822 16670 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 368 8 3 3 2.9 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
14991565 198658 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 23 8 8 3.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL59759 198658 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 23 8 8 3.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL408083 210951 0 None -2 4 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
11812882 78184 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 483 5 3 5 2.5 CN1C(=O)C[C@@H]2[C@@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
CHEMBL2112236 78184 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 483 5 3 5 2.5 CN1C(=O)C[C@@H]2[C@@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
44591826 191934 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 425 8 3 5 3.4 CSCCC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2n1C)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL520997 191934 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 425 8 3 5 3.4 CSCCC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2n1C)C(=O)O 10.1016/j.bmc.2009.02.012
44279862 98673 0 None - 1 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 702 13 3 7 5.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL281017 98673 0 None - 1 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 702 13 3 7 5.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44286976 141413 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 768 18 8 7 3.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL38716 141413 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 768 18 8 7 3.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
15670985 205362 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 490 9 3 5 3.2 COc1cccc(N(CC(=O)N(C)c2ccccc2)C(=O)CNC(=O)Nc2cccc(C(=O)O)c2)c1 10.1021/jm970373j
CHEMBL9195 205362 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 490 9 3 5 3.2 COc1cccc(N(CC(=O)N(C)c2ccccc2)C(=O)CNC(=O)Nc2cccc(C(=O)O)c2)c1 10.1021/jm970373j
CHEMBL3142681 209380 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None Cc1ccccc1NC(=O)NCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
70681224 73295 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
CHEMBL2017829 73295 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
52949124 863 2 None -2 2 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL328422 209550 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1cccc(C)c1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
44381829 167963 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 840 23 10 10 2.9 CC(C)(C)OC(=O)N[C@H](CNN[C@@H](CCCCNC(=O)/C=C/c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)Cc1c[nH]c2ccccc12 10.1016/S0960-894X(00)80680-0
CHEMBL435465 167963 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 840 23 10 10 2.9 CC(C)(C)OC(=O)N[C@H](CNN[C@@H](CCCCNC(=O)/C=C/c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)Cc1c[nH]c2ccccc12 10.1016/S0960-894X(00)80680-0
10392523 206206 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL96970 206206 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
44370406 49617 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 529 16 2 4 6.6 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCc1ccccc1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL156814 49617 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 529 16 2 4 6.6 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCc1ccccc1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
70684970 77495 0 None - 0 Guinea pig 4.0 pIC50 = 4.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 395 3 0 3 4.5 CN1C[C@@H](CC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c2ccccc21 10.1021/jm00390a019
CHEMBL2092990 77495 0 None - 0 Guinea pig 4.0 pIC50 = 4.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 395 3 0 3 4.5 CN1C[C@@H](CC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c2ccccc21 10.1021/jm00390a019
44283515 99712 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 516 8 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)SCCc1ccccc1 10.1021/jm00086a017
CHEMBL288038 99712 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 516 8 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)SCCc1ccccc1 10.1021/jm00086a017
155540415 172370 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1862 71 17 23 3.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4516868 172370 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1862 71 17 23 3.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44349348 16754 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 412 7 3 5 2.2 N#Cc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
CHEMBL125316 16754 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 412 7 3 5 2.2 N#Cc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
45482490 196463 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2c(F)cccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL574715 196463 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2c(F)cccc2[nH]1 10.1016/j.bmc.2009.05.067
19766168 59245 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 367 4 3 3 2.5 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)O)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL171722 59245 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 367 4 3 3 2.5 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)O)C2=O)c1 10.1016/S0960-894X(00)80683-6
71452691 78219 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 671 12 5 7 3.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)C[S+]([O-])c1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
CHEMBL2112336 78219 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 671 12 5 7 3.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)C[S+]([O-])c1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
CHEMBL172635 207111 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1C[C@H](c2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44280372 98928 0 None - 1 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 5.8 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL282645 98928 0 None - 1 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 5.8 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
136060577 87248 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assay
ChEMBL 495 4 1 5 6.3 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccccc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL233647 87248 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assay
ChEMBL 495 4 1 5 6.3 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccccc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
22883501 10322 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 552 6 2 6 5.0 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCCC3)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
CHEMBL116300 10322 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 552 6 2 6 5.0 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCCC3)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
54583297 61592 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774040 61592 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
14208254 202801 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 4 2 4 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL72599 202801 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 4 2 4 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
14802520 115793 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL335914 115793 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
14802520 119854 1 None - 1 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL353157 119854 1 None - 1 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
44368612 121482 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 612 13 5 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL359361 121482 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 612 13 5 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
23815458 167232 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 483 5 3 5 4.2 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL430516 167232 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 483 5 3 5 4.2 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
46235271 73301 2 None 2 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
14208254 202801 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 4 2 4 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL72599 202801 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 4 2 4 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
44210427 120255 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 459 4 2 4 4.7 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL355319 120255 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 459 4 2 4 4.7 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL382051 210546 0 None -489 4 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
10555245 96043 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@H](Cc1ccccc1)NC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@@H](NC(=O)OCc3ccccc3)C(=O)N21 10.1021/jm000959x
CHEMBL262463 96043 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@H](Cc1ccccc1)NC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@@H](NC(=O)OCc3ccccc3)C(=O)N21 10.1021/jm000959x
44210426 58806 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 449 4 2 4 2.2 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL169807 58806 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 449 4 2 4 2.2 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
44300863 196672 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 619 7 4 6 3.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(C)(=O)=O)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL57642 196672 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 619 7 4 6 3.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(C)(=O)=O)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
73349793 204730 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 638 12 5 7 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCc1nnn[nH]1)c1ccccc1 10.1021/jm00092a007
CHEMBL88090 204730 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 638 12 5 7 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCc1nnn[nH]1)c1ccccc1 10.1021/jm00092a007
44329442 205938 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1ccc([C@H]2C[C@@H](c3ccccc3)C[C@@H](NC(=O)Nc3cccc(C)c3)C(=O)N2CC(=O)NC(C)(C)C)cc1 10.1016/S0960-894X(01)80832-5
CHEMBL95369 205938 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1ccc([C@H]2C[C@@H](c3ccccc3)C[C@@H](NC(=O)Nc3cccc(C)c3)C(=O)N2CC(=O)NC(C)(C)C)cc1 10.1016/S0960-894X(01)80832-5
44334237 107546 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 556 10 3 5 4.4 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(NC(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL319466 107546 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 556 10 3 5 4.4 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(NC(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44370473 50589 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL157722 50589 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
10673193 97692 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 506 6 2 5 5.3 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL273693 97692 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 506 6 2 5 5.3 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
10006792 44671 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 517 6 2 5 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL152306 44671 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 517 6 2 5 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
44387108 167691 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 650 9 3 5 4.7 COC(=O)[C@@]1(Cc2ccccc2)C[C@H]2[C@H](NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)C34CC5CC(CC(C5)C3)C4)CCCN2C1=O 10.1016/0960-894X(96)00160-6
CHEMBL433770 167691 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 650 9 3 5 4.7 COC(=O)[C@@]1(Cc2ccccc2)C[C@H]2[C@H](NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)C34CC5CC(CC(C5)C3)C4)CCCN2C1=O 10.1016/0960-894X(96)00160-6
136055865 119691 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 468 4 3 7 3.4 CN1C(=O)[C@@H](NC(=O)Nc2ccc(-c3noc(O)n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL351891 119691 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 468 4 3 7 3.4 CN1C(=O)[C@@H](NC(=O)Nc2ccc(-c3noc(O)n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
10673193 97692 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 506 6 2 5 5.3 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL273693 97692 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 506 6 2 5 5.3 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
44572200 178763 0 None -14 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assayBinding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assay
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL473612 178763 0 None -14 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assayBinding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assay
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL475226 178763 0 None -14 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assayBinding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assay
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
90663557 106215 0 None 6165 2 Rat 10.7 pKi = 10.7 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1152 31 11 13 2.0 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NC(=O)c1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL3143672 106215 0 None 6165 2 Rat 10.7 pKi = 10.7 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1152 31 11 13 2.0 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NC(=O)c1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
443375 205872 40 None -2 5 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm051219x
CHEMBL9506 205872 40 None -2 5 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm051219x
10819755 164890 0 None 52480 2 Rat 10.5 pKi = 10.5 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL423907 164890 0 None 52480 2 Rat 10.5 pKi = 10.5 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
9919500 203217 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL1161142 203217 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL76248 203217 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
9919500 203217 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL1161142 203217 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL76248 203217 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
90662930 106089 0 None 3981 2 Rat 10.3 pKi = 10.3 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1073 29 11 11 2.6 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NC(=O)c1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL3142366 106089 0 None 3981 2 Rat 10.3 pKi = 10.3 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1073 29 11 11 2.6 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NC(=O)c1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
44357046 27850 1 None 18 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 1012 28 9 13 0.7 CSCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL137280 27850 1 None 18 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 1012 28 9 13 0.7 CSCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
4627 809 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL None None None None 10.1021/jm970477u
864 809 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL None None None None 10.1021/jm970477u
9833444 809 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL None None None None 10.1021/jm970477u
CHEMBL1121 809 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL None None None None 10.1021/jm970477u
DB09142 809 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL None None None None 10.1021/jm970477u
4627 809 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
864 809 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
9833444 809 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
CHEMBL1121 809 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
DB09142 809 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
108187 913 30 None 4 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm990967h
873 913 30 None 4 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm990967h
CHEMBL2062154 913 30 None 4 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm990967h
CHEMBL287735 913 30 None 4 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm990967h
5311201 205663 30 None 26 6 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm990967h
CHEMBL9387 205663 30 None 26 6 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm990967h
443375 205872 40 None -3 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL9506 205872 40 None -3 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm990967h
11804040 118943 0 None 2137 2 Rat 9.7 pKi = 9.7 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL345049 118943 0 None 2137 2 Rat 9.7 pKi = 9.7 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL384035 210569 1 None -8 4 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL428666 210569 1 None -8 4 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
10581797 62914 0 None 9120 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 26 9 11 1.3 CC[C@H](C)[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/jm970477u
CHEMBL1791002 62914 0 None 9120 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 26 9 11 1.3 CC[C@H](C)[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/jm970477u
4627 809 44 None -2 5 Human 9.6 pKi = 9.6 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
864 809 44 None -2 5 Human 9.6 pKi = 9.6 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
9833444 809 44 None -2 5 Human 9.6 pKi = 9.6 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
CHEMBL1121 809 44 None -2 5 Human 9.6 pKi = 9.6 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
DB09142 809 44 None -2 5 Human 9.6 pKi = 9.6 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
4627 809 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm9603072
864 809 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm9603072
9833444 809 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm9603072
CHEMBL1121 809 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm9603072
DB09142 809 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm9603072
4627 809 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain
ChEMBL None None None None 10.1021/jm00122a026
864 809 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain
ChEMBL None None None None 10.1021/jm00122a026
9833444 809 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain
ChEMBL None None None None 10.1021/jm00122a026
CHEMBL1121 809 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain
ChEMBL None None None None 10.1021/jm00122a026
DB09142 809 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain
ChEMBL None None None None 10.1021/jm00122a026
121964 205 28 None 831 2 Rat 9.5 pKi = 9.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
858 205 28 None 831 2 Rat 9.5 pKi = 9.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
CHEMBL323521 205 28 None 831 2 Rat 9.5 pKi = 9.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
14208194 162884 2 None 1122 2 Rat 9.5 pKi = 9.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9703247
CHEMBL419764 162884 2 None 1122 2 Rat 9.5 pKi = 9.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9703247
CHEMBL384035 210569 1 None -8 4 Guinea pig 9.5 pKi = 9.5 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2003.11.001
CHEMBL428666 210569 1 None -8 4 Guinea pig 9.5 pKi = 9.5 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2003.11.001
53465844 69068 0 None 131 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-BH-JMV-179 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [125I]-BH-JMV-179 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-BH-JMV-179 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [125I]-BH-JMV-179 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
4627 809 44 None -1 5 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm9703247
864 809 44 None -1 5 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm9703247
9833444 809 44 None -1 5 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm9703247
CHEMBL1121 809 44 None -1 5 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm9703247
DB09142 809 44 None -1 5 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm9703247
10701167 62915 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 990 27 8 11 1.8 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/jm970477u
CHEMBL1791005 62915 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 990 27 8 11 1.8 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/jm970477u
CHEMBL2115177 207516 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
4627 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
864 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
9833444 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
CHEMBL1121 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
DB09142 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
10507071 113111 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm9703247
CHEMBL332261 113111 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm9703247
4627 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm00126a007
864 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm00126a007
9833444 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm00126a007
CHEMBL1121 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm00126a007
DB09142 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm00126a007
4627 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None None 10.1016/S0960-894X(00)80678-2
864 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None None 10.1016/S0960-894X(00)80678-2
9833444 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None None 10.1016/S0960-894X(00)80678-2
CHEMBL1121 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None None 10.1016/S0960-894X(00)80678-2
DB09142 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None None 10.1016/S0960-894X(00)80678-2
4627 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00122a026
864 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00122a026
9833444 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00122a026
CHEMBL1121 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00122a026
DB09142 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00122a026
4627 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranesCompound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm0000416
864 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranesCompound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm0000416
9833444 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranesCompound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm0000416
CHEMBL1121 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranesCompound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm0000416
DB09142 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranesCompound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm0000416
4627 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00053a022
864 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00053a022
9833444 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00053a022
CHEMBL1121 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00053a022
DB09142 809 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00053a022
443375 205872 40 None -3 5 Rat 9.2 pKi = 9.2 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00084a009
CHEMBL9506 205872 40 None -3 5 Rat 9.2 pKi = 9.2 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00084a009
5311400 3241 1 None -2 3 Guinea pig 9.1 pKi = 9.1 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
900 3241 1 None -2 3 Guinea pig 9.1 pKi = 9.1 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
CHEMBL262197 3241 1 None -2 3 Guinea pig 9.1 pKi = 9.1 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
CHEMBL384035 210569 1 None -8 4 Guinea pig 9.0 pKi = 9.0 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL428666 210569 1 None -8 4 Guinea pig 9.0 pKi = 9.0 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL384035 210569 1 None -8 4 Guinea pig 9.0 pKi = 9.0 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL428666 210569 1 None -8 4 Guinea pig 9.0 pKi = 9.0 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
44357045 26370 0 None 85 2 Rat 9.0 pKi = 9.0 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 1012 28 9 13 0.7 CSCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL136096 26370 0 None 85 2 Rat 9.0 pKi = 9.0 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 1012 28 9 13 0.7 CSCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL2369815 207948 0 None 85 2 Rat 9.0 pKi = 9.0 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None CSCC[C@@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
10557073 16196 0 None 3467 2 Guinea pig 8.9 pKi = 8.9 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 763 20 7 8 2.3 CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C 10.1021/jm0000416
CHEMBL122934 16196 0 None 3467 2 Guinea pig 8.9 pKi = 8.9 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 763 20 7 8 2.3 CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C 10.1021/jm0000416
10004216 4675 0 None -11 2 Rat 8.8 pKi = 8.8 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1016/0960-894X(95)00528-2
CHEMBL103750 4675 0 None -11 2 Rat 8.8 pKi = 8.8 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1016/0960-894X(95)00528-2
CHEMBL1172429 206845 0 None 26 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
44359425 14575 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL1206331 14575 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL262687 14575 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
443375 205872 40 None -2 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/j.bmcl.2007.09.093
CHEMBL9506 205872 40 None -2 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/j.bmcl.2007.09.093
44328894 108137 0 None -25 2 Human 8.0 pKi = 8 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 587 5 2 4 4.8 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CC(=O)N2CC3CCC(CC3)C2)c2ccccc2N(c2ccccc2F)C1=O 10.1016/S0960-894X(96)00613-0
CHEMBL320624 108137 0 None -25 2 Human 8.0 pKi = 8 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 587 5 2 4 4.8 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CC(=O)N2CC3CCC(CC3)C2)c2ccccc2N(c2ccccc2F)C1=O 10.1016/S0960-894X(96)00613-0
3476 1373 8 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm200438b
59751 1373 8 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm200438b
878 1373 8 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm200438b
CHEMBL39263 1373 8 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm200438b
10840582 167416 0 None 257 2 Rat 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm9703247
CHEMBL431858 167416 0 None 257 2 Rat 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm9703247
45486933 195261 0 None 3 2 Human 7.0 pKi = 7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 520 7 2 6 5.3 CC(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.09.064
CHEMBL566360 195261 0 None 3 2 Human 7.0 pKi = 7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 520 7 2 6 5.3 CC(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.09.064
45487006 197234 0 None -10 2 Human 7.0 pKi = 7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 666 8 3 6 5.0 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
CHEMBL584525 197234 0 None -10 2 Human 7.0 pKi = 7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 666 8 3 6 5.0 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
10767708 14377 0 None -138 2 Rat 7.0 pKi = 7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 500 6 2 3 5.6 O=C(Nc1ccccc1)NC1C(=O)N(CCC2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1021/jm990967h
CHEMBL120296 14377 0 None -138 2 Rat 7.0 pKi = 7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 500 6 2 3 5.6 O=C(Nc1ccccc1)NC1C(=O)N(CCC2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1021/jm990967h
45486994 196047 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 506 7 2 6 4.8 O=C(NCCc1ccc(Cl)cc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL571457 196047 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 506 7 2 6 4.8 O=C(NCCc1ccc(Cl)cc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
44408411 160763 0 None -2089 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1242 31 11 15 4.4 CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL412331 160763 0 None -2089 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1242 31 11 15 4.4 CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
118719285 114984 0 None -25 3 Guinea pig 6.0 pKi = 6 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 733 15 5 7 4.7 CN(C)[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C)c1ccccc1 10.1021/jm00053a022
CHEMBL3351057 114984 0 None -25 3 Guinea pig 6.0 pKi = 6 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 733 15 5 7 4.7 CN(C)[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C)c1ccccc1 10.1021/jm00053a022
44265924 205649 0 None - 1 Rat 6.0 pKi = 6 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 363 5 1 1 5.7 O=C(NCC=C(c1ccccc1)c1ccccc1)c1cccc2ccccc12 10.1021/jm00084a009
CHEMBL9379 205649 0 None - 1 Rat 6.0 pKi = 6 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 363 5 1 1 5.7 O=C(NCC=C(c1ccccc1)c1ccccc1)c1cccc2ccccc12 10.1021/jm00084a009
10440219 168133 0 None -25 2 Guinea pig 6.0 pKi = 6 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL 776 15 6 7 4.4 CN(C)C(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)c1ccccc1 10.1016/S0960-894X(00)80678-2
CHEMBL436722 168133 0 None -25 2 Guinea pig 6.0 pKi = 6 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL 776 15 6 7 4.4 CN(C)C(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)c1ccccc1 10.1016/S0960-894X(00)80678-2
11527738 75636 0 None -10964 4 Human 5.0 pKi = 5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 518 7 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL205455 75636 0 None -10964 4 Human 5.0 pKi = 5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 518 7 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL411201 211125 0 None -4786 4 Human 5.0 pKi = 5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm0303103
44408484 136983 0 None -19498 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1033 30 13 12 1.4 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL375412 136983 0 None -19498 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1033 30 13 12 1.4 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm050851n
44418924 156340 0 None -19952 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL407198 156340 0 None -19952 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
9844256 11692 0 None -3 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 406 7 3 2 4.6 O=C(O)CCNC(=O)c1cc(-c2ccccc2)[nH]c1CC12CC3CC(CC(C3)C1)C2 10.1021/jm049069y
CHEMBL1181869 11692 0 None -3 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 406 7 3 2 4.6 O=C(O)CCNC(=O)c1cc(-c2ccccc2)[nH]c1CC12CC3CC(CC(C3)C1)C2 10.1021/jm049069y
CHEMBL2067947 11692 0 None -3 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 406 7 3 2 4.6 O=C(O)CCNC(=O)c1cc(-c2ccccc2)[nH]c1CC12CC3CC(CC(C3)C1)C2 10.1021/jm049069y
44403980 11700 0 None -398 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(C(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1181938 11700 0 None -398 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(C(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067951 11700 0 None -398 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(C(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
10771043 25948 0 None -61 2 Guinea pig 6.0 pKi = 6.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1cccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm00021a019
CHEMBL135658 25948 0 None -61 2 Guinea pig 6.0 pKi = 6.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1cccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm00021a019
44212464 63807 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 527 8 2 5 3.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808399 63807 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 527 8 2 5 3.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
56673524 63824 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808418 63824 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
10438352 9706 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 588 8 3 6 3.9 COC(=O)[C@@]1(Cc2ccccc2)C[C@@H]2[C@@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm9703247
CHEMBL113699 9706 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 588 8 3 6 3.9 COC(=O)[C@@]1(Cc2ccccc2)C[C@@H]2[C@@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm9703247
10054705 107941 0 None -28 2 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 625 10 3 4 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
CHEMBL319880 107941 0 None -28 2 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 625 10 3 4 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
44357069 155152 0 None -147 2 Guinea pig 5.0 pKi = 5.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 675 9 5 5 5.4 C[C@@H](NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL405062 155152 0 None -147 2 Guinea pig 5.0 pKi = 5.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 675 9 5 5 5.4 C[C@@H](NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm00021a019
10077166 99472 0 None -75 2 Guinea pig 6.0 pKi = 6.0 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1016/s0960-894x(98)00231-5
CHEMBL286247 99472 0 None -75 2 Guinea pig 6.0 pKi = 6.0 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1016/s0960-894x(98)00231-5
44280157 155188 0 None -75 2 Guinea pig 6.0 pKi = 6.0 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 667 8 3 5 6.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1CC[C@H](Oc2ccc(Cl)cc2Cl)C[C@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
CHEMBL405468 155188 0 None -75 2 Guinea pig 6.0 pKi = 6.0 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 667 8 3 5 6.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1CC[C@H](Oc2ccc(Cl)cc2Cl)C[C@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
10257865 206696 3 None -173 5 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99939 206696 3 None -173 5 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
56683505 63810 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 8 2 5 3.7 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(Br)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808402 63810 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 8 2 5 3.7 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(Br)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL430298 211870 0 None -2137 4 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm0303103
44331483 107012 0 None -25 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 541 5 1 4 6.1 O=C(NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O)Oc1ccccc1 10.1016/S0960-894X(96)00544-6
CHEMBL318569 107012 0 None -25 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 541 5 1 4 6.1 O=C(NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O)Oc1ccccc1 10.1016/S0960-894X(96)00544-6
10840039 113294 0 None -16 2 Rat 7.9 pKi = 7.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 6 2 4 6.2 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL332403 113294 0 None -16 2 Rat 7.9 pKi = 7.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 6 2 4 6.2 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL218327 207649 0 None -2630 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
CHEMBL1207511 206867 0 None -2398 2 Guinea pig 6.0 pKi = 6.0 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80678-2
CHEMBL412917 206867 0 None -2398 2 Guinea pig 6.0 pKi = 6.0 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80678-2
CHEMBL353862 209981 0 None -77 3 Guinea pig 6.0 pKi = 6.0 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O)c1ccccc1 10.1016/S0960-894X(00)80678-2
CHEMBL3350335 209728 0 None -245 2 Guinea pig 5.0 pKi = 5.0 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
10626579 15336 0 None -38 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 554 6 2 4 6.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(OC(F)(F)F)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL121703 15336 0 None -38 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 554 6 2 4 6.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(OC(F)(F)F)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
10552321 163358 0 None -165 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 5 2 3 5.3 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL420728 163358 0 None -165 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 5 2 3 5.3 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
11698512 167692 0 None -21 3 Guinea pig 6.0 pKi = 6.0 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 435 8 3 3 5.5 CCCc1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL433776 167692 0 None -21 3 Guinea pig 6.0 pKi = 6.0 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 435 8 3 3 5.5 CCCc1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
3503 1862 8 None -1174 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 534 5 2 3 6.1 O=C(N[C@H]1C(=O)N(c2ccccc2)c2c(N(C1=O)CC13CC4CC(C3)CC(C1)C4)cccc2)Nc1ccccc1 10.1016/S0960-894X(96)00544-6
5311147 1862 8 None -1174 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 534 5 2 3 6.1 O=C(N[C@H]1C(=O)N(c2ccccc2)c2c(N(C1=O)CC13CC4CC(C3)CC(C1)C4)cccc2)Nc1ccccc1 10.1016/S0960-894X(96)00544-6
CHEMBL329305 1862 8 None -1174 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 534 5 2 3 6.1 O=C(N[C@H]1C(=O)N(c2ccccc2)c2c(N(C1=O)CC13CC4CC(C3)CC(C1)C4)cccc2)Nc1ccccc1 10.1016/S0960-894X(96)00544-6
44346296 113999 0 None -1174 2 Rat 6.0 pKi = 6.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 562 6 2 4 5.9 O=Cc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL333517 113999 0 None -1174 2 Rat 6.0 pKi = 6.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 562 6 2 4 5.9 O=Cc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
11527738 75636 0 None -10964 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 518 7 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
CHEMBL205455 75636 0 None -10964 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 518 7 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
10257865 206696 3 None -173 5 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99939 206696 3 None -173 5 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
10576324 113465 0 None -54 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 6 2 3 5.3 CC(C)CC(C)N1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL332595 113465 0 None -54 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 6 2 3 5.3 CC(C)CC(C)N1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
135529065 156473 0 None -275 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 588 7 2 7 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL407340 156473 0 None -275 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 588 7 2 7 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
11511721 75749 0 None -194 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 502 7 2 5 5.5 CNc1cccc(NC(=O)C[C@@H]2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
CHEMBL205751 75749 0 None -194 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 502 7 2 5 5.5 CNc1cccc(NC(=O)C[C@@H]2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
10618720 192896 0 None -4 2 Guinea pig 4.9 pKi = 4.9 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 363 4 2 2 4.5 O=C(O)c1cc2ccccc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm9508907
CHEMBL52740 192896 0 None -4 2 Guinea pig 4.9 pKi = 4.9 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 363 4 2 2 4.5 O=C(O)c1cc2ccccc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm9508907
CHEMBL64605 214079 6 None -1288 3 Guinea pig 4.9 pKi = 4.9 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0000416
11635377 197131 0 None 39 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 554 7 2 6 6.0 CC(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.09.064
CHEMBL583457 197131 0 None 39 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 554 7 2 6 6.0 CC(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.09.064
44346047 112903 0 None -537 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 568 7 2 7 6.4 O=C(Nc1cccc(C2N=NN=N2)c1)NC1C(=O)N(CCC2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1021/jm990967h
CHEMBL331872 112903 0 None -537 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 568 7 2 7 6.4 O=C(Nc1cccc(C2N=NN=N2)c1)NC1C(=O)N(CCC2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1021/jm990967h
CHEMBL3351051 209789 0 None -17 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cccc2ccccc12)NC)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
CHEMBL3351053 209791 0 None -426 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
44356886 28215 0 None -42 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 757 11 5 5 7.3 O=C(O)c1cc(NC(=O)[C@@H](CC2CCCCC2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL137525 28215 0 None -42 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 757 11 5 5 7.3 O=C(O)c1cc(NC(=O)[C@@H](CC2CCCCC2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
10747345 116477 0 None -6 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1ccccc1NC(=O)[C@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
CHEMBL338728 116477 0 None -6 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1ccccc1NC(=O)[C@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
44329798 107063 0 None -100 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 610 10 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(C(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
CHEMBL318852 107063 0 None -100 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 610 10 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(C(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
11497371 70286 0 None -40 3 Guinea pig 6.9 pKi = 6.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 525 7 3 3 7.4 Cc1cc(C)c(-c2nc(C(=O)Nc3ccc(C)c(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
CHEMBL195007 70286 0 None -40 3 Guinea pig 6.9 pKi = 6.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 525 7 3 3 7.4 Cc1cc(C)c(-c2nc(C(=O)Nc3ccc(C)c(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
10552320 116956 0 None -109 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 6 2 3 5.2 CC(C)C(C)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL339879 116956 0 None -109 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 6 2 3 5.2 CC(C)C(C)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
10257865 206696 3 None -204 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99939 206696 3 None -204 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
9960432 39187 6 None -12 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
CHEMBL147186 39187 6 None -12 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
11571140 71357 0 None -23 3 Guinea pig 6.9 pKi = 6.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 489 7 3 3 6.9 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL196517 71357 0 None -23 3 Guinea pig 6.9 pKi = 6.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 489 7 3 3 6.9 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
45487002 195912 0 None -10 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 672 8 3 7 5.1 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL570520 195912 0 None -10 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 672 8 3 7 5.1 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
9958214 114295 0 None -269 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
CHEMBL333979 114295 0 None -269 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
44272156 141010 0 None -45 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL384731 141010 0 None -45 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
44444933 94230 0 None - 1 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 455 6 3 3 5.8 O=C(O)c1cccc(NC(=O)c2nc(-c3ccccc3)[nH]c2CC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm070880t
CHEMBL252559 94230 0 None - 1 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 455 6 3 3 5.8 O=C(O)c1cccc(NC(=O)c2nc(-c3ccccc3)[nH]c2CC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm070880t
9853208 101254 0 None -1071 2 Guinea pig 5.9 pKi = 5.9 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 710 11 6 9 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2[nH]ccc2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
CHEMBL299540 101254 0 None -1071 2 Guinea pig 5.9 pKi = 5.9 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 710 11 6 9 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2[nH]ccc2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
44346825 114275 0 None -77 2 Guinea pig 4.9 pKi = 4.9 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
CHEMBL333920 114275 0 None -77 2 Guinea pig 4.9 pKi = 4.9 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
3960 2313 20 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm950423p
891 2313 20 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm950423p
CHEMBL24938 2313 20 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm950423p
16100406 82811 0 None -33 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL218600 82811 0 None -33 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
11612498 133039 0 None -5 3 Guinea pig 5.9 pKi = 5.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 469 7 3 3 6.2 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccccc3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL371068 133039 0 None -5 3 Guinea pig 5.9 pKi = 5.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 469 7 3 3 6.2 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccccc3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
9808153 112177 0 None -36 2 Guinea pig 5.9 pKi = 5.9 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 571 11 3 4 5.6 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1021/jm00072a005
CHEMBL330390 112177 0 None -36 2 Guinea pig 5.9 pKi = 5.9 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 571 11 3 4 5.6 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1021/jm00072a005
10676550 118857 0 None -12 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm00021a019
CHEMBL344396 118857 0 None -12 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm00021a019
10257865 206696 3 None -204 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99939 206696 3 None -204 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
44271859 140993 0 None -4 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1292 39 14 16 2.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL384618 140993 0 None -4 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1292 39 14 16 2.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL1172251 206841 0 None -229 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
CHEMBL3351058 209794 0 None -83 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)C1CCCCC1 10.1021/jm00053a022
44265978 205767 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 365 6 2 2 5.3 O=C(NCCN(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
CHEMBL9444 205767 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 365 6 2 2 5.3 O=C(NCCN(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
CHEMBL2370437 208105 0 None -10 2 Guinea pig 4.9 pKi = 4.9 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
10745516 14242 0 None -60 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 563 5 2 4 5.8 CN(C)c1cccc(NC(=O)NC2C(=O)N(c3ccccc3)c3ccccc3N(C3[C@H]4C[C@@H]5C[C@@H](C[C@H]3C5)C4)C2=O)c1 10.1021/jm990967h
CHEMBL120015 14242 0 None -60 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 563 5 2 4 5.8 CN(C)c1cccc(NC(=O)NC2C(=O)N(c3ccccc3)c3ccccc3N(C3[C@H]4C[C@@H]5C[C@@H](C[C@H]3C5)C4)C2=O)c1 10.1021/jm990967h
56673524 63824 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808418 63824 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
44331467 106967 0 None -41 2 Rat 5.9 pKi = 5.9 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 529 7 1 4 5.8 CC(C)CCN1C(=O)C(NC(=O)Oc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL318291 106967 0 None -41 2 Rat 5.9 pKi = 5.9 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 529 7 1 4 5.8 CC(C)CCN1C(=O)C(NC(=O)Oc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
44357057 118715 0 None -446 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccccc2F)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL343367 118715 0 None -446 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccccc2F)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
10794262 168063 0 None -6 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 645 10 4 4 4.8 O=C(O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
CHEMBL436175 168063 0 None -6 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 645 10 4 4 4.8 O=C(O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
11539356 71336 0 None -69 3 Guinea pig 5.8 pKi = 5.8 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 435 7 3 3 5.6 CC(C)c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL196441 71336 0 None -69 3 Guinea pig 5.8 pKi = 5.8 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 435 7 3 3 5.6 CC(C)c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
56683506 63811 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 511 8 2 5 3.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(F)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808403 63811 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 511 8 2 5 3.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(F)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
19700629 63809 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 561 8 2 5 4.0 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(C(F)(F)F)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808401 63809 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 561 8 2 5 4.0 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(C(F)(F)F)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
10770670 92061 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL2067959 92061 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL24313 92061 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
9850043 112375 1 None -446 3 Rat 5.8 pKi = 5.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL330977 112375 1 None -446 3 Rat 5.8 pKi = 5.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44346826 113315 0 None -69 2 Guinea pig 4.8 pKi = 4.8 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 595 7 3 4 3.9 O=C(O)CNC(=O)[C@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL332510 113315 0 None -69 2 Guinea pig 4.8 pKi = 4.8 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 595 7 3 4 3.9 O=C(O)CNC(=O)[C@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL334114 209648 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N 10.1021/jm0000416
CHEMBL2372623 208532 0 None -16 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
CHEMBL2370598 208133 0 None -12 2 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of 0.1 nM [3H]Boc[Nle28,31]-CCK27-33 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]Boc[Nle28,31]-CCK27-33 from guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)C[C@@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
44385472 81714 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL 1246 26 13 15 2.2 CCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCCCNC(=O)CC(NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](CN)Cc1ccccc1 10.1021/jm00389a002
CHEMBL216677 81714 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL 1246 26 13 15 2.2 CCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCCCNC(=O)CC(NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](CN)Cc1ccccc1 10.1021/jm00389a002
19700643 63688 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1807152 63688 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
11712880 138394 0 None -114 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell line
ChEMBL 490 6 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
CHEMBL378388 138394 0 None -114 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell line
ChEMBL 490 6 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
10769748 112508 0 None -1148 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 591 6 3 4 6.1 CC(=O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL331119 112508 0 None -1148 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 591 6 3 4 6.1 CC(=O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
10482868 106920 0 None -107 5 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 557 10 3 4 5.2 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL317999 106920 0 None -107 5 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 557 10 3 4 5.2 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
10460621 106694 0 None -8 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 567 8 3 3 6.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)c(Cl)c1 10.1021/jm00072a005
CHEMBL316462 106694 0 None -8 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 567 8 3 3 6.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)c(Cl)c1 10.1021/jm00072a005
44451877 95535 0 None -162 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 587 7 1 6 6.9 Cc1nc(-c2cccc(NC(=O)CN3C(=O)N(CC(=O)C(C)(C)C)c4ccccc4N(C4CCCCC4)C3=O)c2)cs1 10.1016/j.bmc.2007.12.047
CHEMBL259557 95535 0 None -162 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 587 7 1 6 6.9 Cc1nc(-c2cccc(NC(=O)CN3C(=O)N(CC(=O)C(C)(C)C)c4ccccc4N(C4CCCCC4)C3=O)c2)cs1 10.1016/j.bmc.2007.12.047
10722460 15023 0 None -309 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1cccc(Br)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL121028 15023 0 None -309 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1cccc(Br)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL440259 212114 0 None -4 2 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
44318341 204281 0 None -501 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 698 10 5 5 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)c(I)c1 10.1016/0960-894X(95)00435-V
CHEMBL1628582 204281 0 None -501 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 698 10 5 5 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)c(I)c1 10.1016/0960-894X(95)00435-V
CHEMBL84864 204281 0 None -501 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 698 10 5 5 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)c(I)c1 10.1016/0960-894X(95)00435-V
10698109 106812 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
CHEMBL317181 106812 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
45486967 195747 0 None 39 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 472 7 2 6 4.1 O=C(NCCc1ccccc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL569616 195747 0 None 39 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 472 7 2 6 4.1 O=C(NCCc1ccccc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45102806 195088 0 None -15 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 646 8 3 7 5.1 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL565324 195088 0 None -15 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 646 8 3 7 5.1 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
45486936 195296 0 None -25 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 640 8 3 6 5.1 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
CHEMBL566574 195296 0 None -25 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 640 8 3 6 5.1 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
11700410 197077 0 None -31 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 704 8 3 7 4.4 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(I)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL583035 197077 0 None -31 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 704 8 3 7 4.4 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(I)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
9872866 63822 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 7 2 5 4.1 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808416 63822 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 7 2 5 4.1 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
44212230 4195 0 None -208 2 Rat 5.8 pKi = 5.8 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 572 8 1 5 5.9 CC(C)CCN1C(=O)C(NC(=O)Oc2cccc(N(C)C)c2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL100509 4195 0 None -208 2 Rat 5.8 pKi = 5.8 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 572 8 1 5 5.9 CC(C)CCN1C(=O)C(NC(=O)Oc2cccc(N(C)C)c2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
10792765 112581 0 None -2754 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 550 5 3 4 5.8 O=C(Nc1cccc(O)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL331244 112581 0 None -2754 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 550 5 3 4 5.8 O=C(Nc1cccc(O)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
10770670 92061 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067959 92061 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL24313 92061 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
44359447 14534 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL1206132 14534 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL217767 14534 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL216831 207598 0 None -29 2 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCC)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
10482233 167639 0 None -41 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 533 8 3 3 6.0 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)cc1 10.1021/jm00072a005
CHEMBL433407 167639 0 None -41 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 533 8 3 3 6.0 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)cc1 10.1021/jm00072a005
10795116 27707 0 None -602 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 743 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCc2ccc3ccccc3c2)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL137180 27707 0 None -602 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 743 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCc2ccc3ccccc3c2)cc(C(=O)O)c1 10.1021/jm00021a019
9850043 112375 1 None -446 3 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL330977 112375 1 None -446 3 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
52949124 863 2 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
44356826 118801 0 None -19 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 781 12 5 6 6.6 COc1ccc(C[C@@H](NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)C(=O)Nc2cc(C(=O)O)cc(C(=O)O)c2)cc1 10.1021/jm00021a019
CHEMBL344014 118801 0 None -19 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 781 12 5 6 6.6 COc1ccc(C[C@@H](NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)C(=O)Nc2cc(C(=O)O)cc(C(=O)O)c2)cc1 10.1021/jm00021a019
56666598 63828 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 575 9 2 4 5.3 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccc(F)cc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808422 63828 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 575 9 2 4 5.3 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccc(F)cc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
16733645 13070 0 None -416 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 598 9 2 7 5.4 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3cn(CC(=O)O)cn3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL1190962 13070 0 None -416 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 598 9 2 7 5.4 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3cn(CC(=O)O)cn3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL541903 13070 0 None -416 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 598 9 2 7 5.4 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3cn(CC(=O)O)cn3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44280114 5041 0 None 1 2 Guinea pig 5.8 pKi = 5.8 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 567 7 2 4 6.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/s0960-894x(98)00231-5
CHEMBL105618 5041 0 None 1 2 Guinea pig 5.8 pKi = 5.8 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 567 7 2 4 6.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/s0960-894x(98)00231-5
44572200 178763 0 None -14 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL473612 178763 0 None -14 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL475226 178763 0 None -14 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
56659685 63821 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 533 7 2 5 3.8 Cc1cccc(NC(=O)NC2C(=O)N(CCN3CCOCC3)c3ccccc3N(CC3CCCCC3)C2=O)c1 10.1016/j.bmc.2011.05.057
CHEMBL1808415 63821 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 533 7 2 5 3.8 Cc1cccc(NC(=O)NC2C(=O)N(CCN3CCOCC3)c3ccccc3N(CC3CCCCC3)C2=O)c1 10.1016/j.bmc.2011.05.057
5311201 205663 30 None -1174 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm051219x
CHEMBL9387 205663 30 None -1174 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm051219x
16732019 85009 0 None -1737 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 542 7 2 7 4.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL226533 85009 0 None -1737 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 542 7 2 7 4.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
54045469 63818 0 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 481 9 2 5 3.2 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN(C)C)C2=O)cc1 10.1016/j.bmc.2011.05.057
CHEMBL1808412 63818 0 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 481 9 2 5 3.2 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN(C)C)C2=O)cc1 10.1016/j.bmc.2011.05.057
10258121 98121 0 None 11 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 606 11 4 2 7.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)NC(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL276676 98121 0 None 11 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 606 11 4 2 7.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)NC(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL59865 214039 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN 10.1021/jm0000416
CHEMBL1172253 206843 0 None -138 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
44265911 205404 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 276 4 2 1 3.6 O=C(NC/C=C/c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
CHEMBL9220 205404 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 276 4 2 1 3.6 O=C(NC/C=C/c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
10004216 4675 0 None -11 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL103750 4675 0 None -11 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
44356887 31102 0 None -776 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 757 11 5 6 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccsc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL140179 31102 0 None -776 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 757 11 5 6 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccsc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
10323690 100032 0 None -21 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL2114401 100032 0 None -21 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL291033 100032 0 None -21 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00072a005
44272076 168244 0 None -407 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)[C@H](NC(=O)OC(C)(C)C)CCC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL437661 168244 0 None -407 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)[C@H](NC(=O)OC(C)(C)C)CCC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
10819816 118236 0 None 7 2 Rat 7.7 pKi = 7.7 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 998 28 10 13 0.4 CSCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL341762 118236 0 None 7 2 Rat 7.7 pKi = 7.7 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 998 28 10 13 0.4 CSCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
73354497 88955 0 None 7 2 Rat 7.7 pKi = 7.7 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 998 28 10 13 0.4 CSCC[C@@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL2369817 88955 0 None 7 2 Rat 7.7 pKi = 7.7 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 998 28 10 13 0.4 CSCC[C@@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
44359447 14534 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL1206132 14534 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL217767 14534 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
10768579 113367 0 None -32 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 531 6 2 4 5.5 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL332568 113367 0 None -32 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 531 6 2 4 5.5 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
53465844 69068 0 None 131 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-SR-27897 from human CCK1 R197A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 R197A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-SR-27897 from human CCK1 R197A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 R197A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10722460 15023 0 None -309 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1cccc(Br)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL121028 15023 0 None -309 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1cccc(Br)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44408526 136422 0 None -2344 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL374325 136422 0 None -2344 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
16100409 82821 0 None -870 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL218651 82821 0 None -870 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
16732916 136430 0 None -338 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 596 8 2 5 6.3 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C23CC4CC(CC(C4)C2)C3)C1=O)Nc1cccc(C(=O)O)c1 10.1021/jm070139l
CHEMBL374388 136430 0 None -338 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 596 8 2 5 6.3 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C23CC4CC(CC(C4)C2)C3)C1=O)Nc1cccc(C(=O)O)c1 10.1021/jm070139l
10695854 113504 0 None -25 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
CHEMBL332646 113504 0 None -25 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
45486955 195722 0 None -5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 628 8 3 7 5.0 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL569470 195722 0 None -5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 628 8 3 7 5.0 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486969 195794 0 None 7 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 598 8 3 7 5.4 C[C@H](c1ccc(Cl)c(Cl)c1)[C@@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
CHEMBL569849 195794 0 None 7 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 598 8 3 7 5.4 C[C@H](c1ccc(Cl)c(Cl)c1)[C@@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
45486947 195227 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 654 8 2 7 5.2 COC(=O)[C@H](Cc1ccc(F)c(Br)c1)NC(=O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
CHEMBL566177 195227 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 654 8 2 7 5.2 COC(=O)[C@H](Cc1ccc(F)c(Br)c1)NC(=O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
11693225 197123 0 None -7 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 676 8 3 7 4.8 O=C(N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(I)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL583344 197123 0 None -7 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 676 8 3 7 4.8 O=C(N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(I)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
16090700 82051 0 None 10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 541 8 4 4 4.2 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cc2ccccc2[nH]1 10.1021/jm060590x
CHEMBL217595 82051 0 None 10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 541 8 4 4 4.2 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cc2ccccc2[nH]1 10.1021/jm060590x
9958214 114295 0 None -269 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
CHEMBL333979 114295 0 None -269 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
45486995 196124 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 486 8 2 6 4.5 O=C(NCCCc1ccccc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL572046 196124 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 486 8 2 6 4.5 O=C(NCCCc1ccccc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486940 197207 0 None -31 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 550 8 3 7 4.2 O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL584259 197207 0 None -31 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 550 8 3 7 4.2 O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
44444929 94442 0 None - 1 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 788 11 6 5 6.1 O=C(O)c1cc(NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL254020 94442 0 None - 1 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 788 11 6 5 6.1 O=C(O)c1cc(NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
10795162 118533 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL2067970 118533 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL342616 118533 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
16090702 165645 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 461 4 2 3 4.4 O=C(c1ccc(Br)cc1NS(=O)(=O)c1cc2ccccc2[nH]1)N1CCCCC1 10.1021/jm060590x
CHEMBL426524 165645 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 461 4 2 3 4.4 O=C(c1ccc(Br)cc1NS(=O)(=O)c1cc2ccccc2[nH]1)N1CCCCC1 10.1021/jm060590x
44331343 4345 0 None -57 2 Rat 5.7 pKi = 5.7 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 606 6 2 3 7.0 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/S0960-894X(96)00544-6
CHEMBL101456 4345 0 None -57 2 Rat 5.7 pKi = 5.7 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 606 6 2 3 7.0 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/S0960-894X(96)00544-6
44403984 12205 0 None -125 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(CC12CC3CC(CC(C3)C1)C2)C(=O)c1cc2[nH]cnc2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1185003 12205 0 None -125 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(CC12CC3CC(CC(C3)C1)C2)C(=O)c1cc2[nH]cnc2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067967 12205 0 None -125 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(CC12CC3CC(CC(C3)C1)C2)C(=O)c1cc2[nH]cnc2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
10795162 118533 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067970 118533 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL342616 118533 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
6956374 2373 4 None - 1 Guinea pig 4.7 pKi = 4.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1021/jm070880t
902 2373 4 None - 1 Guinea pig 4.7 pKi = 4.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1021/jm070880t
CHEMBL117281 2373 4 None - 1 Guinea pig 4.7 pKi = 4.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1021/jm070880t
9939183 113629 0 None -6606 2 Rat 4.7 pKi = 4.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 633 7 2 5 5.9 O=C(Nc1cccc(CN2CCOCC2)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL332850 113629 0 None -6606 2 Rat 4.7 pKi = 4.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 633 7 2 5 5.9 O=C(Nc1cccc(CN2CCOCC2)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44347144 112567 0 None -12 2 Guinea pig 4.7 pKi = 4.7 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 512 6 2 4 4.0 COC(=O)CNC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL331177 112567 0 None -12 2 Guinea pig 4.7 pKi = 4.7 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 512 6 2 4 4.0 COC(=O)CNC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL386304 210633 0 None -6 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
44272056 97712 0 None -42 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL273880 97712 0 None -42 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
10794634 112603 0 None 11220 2 Guinea pig 8.7 pKi = 8.7 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 677 19 7 7 0.3 CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(N)=O 10.1021/jm0000416
CHEMBL331394 112603 0 None 11220 2 Guinea pig 8.7 pKi = 8.7 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 677 19 7 7 0.3 CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(N)=O 10.1021/jm0000416
53465844 69068 0 None 131 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL333477 209646 0 None -3 3 Guinea pig 8.6 pKi = 8.6 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/j.bmcl.2003.11.001
CHEMBL333762 209647 0 None - 1 Guinea pig 8.6 pKi = 8.6 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1021/jm0000416
11216391 162941 0 None 1348 2 Guinea pig 8.6 pKi = 8.6 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 747 23 7 7 2.1 CCCCCNC(=O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2003.11.001
CHEMBL420161 162941 0 None 1348 2 Guinea pig 8.6 pKi = 8.6 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 747 23 7 7 2.1 CCCCCNC(=O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2003.11.001
CHEMBL119992 206856 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N 10.1021/jm0000416
CHEMBL3350278 209720 0 None 20 2 Guinea pig 6.7 pKi = 6.7 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00174a016
44265932 96554 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 420 5 2 1 6.3 O=C(NCC=C(c1ccc(Cl)cc1)c1ccc(Cl)cc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
CHEMBL266596 96554 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 420 5 2 1 6.3 O=C(NCC=C(c1ccc(Cl)cc1)c1ccc(Cl)cc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
44265967 164321 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 350 11 2 1 6.5 CCCCCC(=CCNC(=O)Nc1ccc(Cl)cc1)CCCCC 10.1021/jm00084a009
CHEMBL422036 164321 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 350 11 2 1 6.5 CCCCCC(=CCNC(=O)Nc1ccc(Cl)cc1)CCCCC 10.1021/jm00084a009
CHEMBL379405 210518 0 None -11 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
10099504 206472 0 None -14 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 568 10 2 4 5.8 CC(Cc1cccc2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL98516 206472 0 None -14 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 568 10 2 4 5.8 CC(Cc1cccc2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
10628607 116274 0 None -467 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 713 11 5 5 6.4 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL337673 116274 0 None -467 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 713 11 5 5 6.4 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm00021a019
19700636 63816 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 491 8 2 4 4.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808410 63816 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 491 8 2 4 4.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
9872866 63822 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 7 2 5 4.1 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808416 63822 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 7 2 5 4.1 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
19700617 63827 0 None - 1 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 543 8 2 4 4.7 CN(C)CCCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808421 63827 0 None - 1 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 543 8 2 4 4.7 CN(C)CCCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
10370321 12873 0 None -30902 2 Rat 4.7 pKi = 4.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 550 5 3 4 5.8 O=C(Nc1ccc(O)cc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL118954 12873 0 None -30902 2 Rat 4.7 pKi = 4.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 550 5 3 4 5.8 O=C(Nc1ccc(O)cc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44346909 114085 0 None -10 2 Guinea pig 4.7 pKi = 4.7 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 498 6 3 3 3.9 O=C(O)CNC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL333758 114085 0 None -10 2 Guinea pig 4.7 pKi = 4.7 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 498 6 3 3 3.9 O=C(O)CNC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
44356888 118364 0 None -35 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 765 12 5 5 7.0 O=C(O)c1cc(NC(=O)[C@@H](CCc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL342205 118364 0 None -35 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 765 12 5 5 7.0 O=C(O)c1cc(NC(=O)[C@@H](CCc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
10795162 118533 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL2067970 118533 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL342616 118533 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
11561828 140096 0 None -4 2 Guinea pig 5.7 pKi = 5.7 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 468 7 3 2 6.8 O=C(O)c1cccc(NC(=O)c2cc(-c3ccccc3)[nH]c2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL381426 140096 0 None -4 2 Guinea pig 5.7 pKi = 5.7 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 468 7 3 2 6.8 O=C(O)c1cccc(NC(=O)c2cc(-c3ccccc3)[nH]c2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
44451547 96264 0 None -489 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 587 8 2 8 4.7 CN(c1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCC3)C2=O)c1)c1nn[nH]n1 10.1016/j.bmc.2007.12.047
CHEMBL264150 96264 0 None -489 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 587 8 2 8 4.7 CN(c1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCC3)C2=O)c1)c1nn[nH]n1 10.1016/j.bmc.2007.12.047
16733469 85093 0 None -6309 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 576 10 2 6 5.8 O=C(O)CSc1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1021/jm070139l
CHEMBL227333 85093 0 None -6309 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 576 10 2 6 5.8 O=C(O)CSc1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1021/jm070139l
44296914 100779 0 None -1318 2 Guinea pig 5.7 pKi = 5.7 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 765 12 5 5 7.0 O=C(CC1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL296167 100779 0 None -1318 2 Guinea pig 5.7 pKi = 5.7 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 765 12 5 5 7.0 O=C(CC1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL3351052 209790 0 None -14 2 Guinea pig 5.7 pKi = 5.7 Binding
Affinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membraneAffinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membrane
ChEMBL None None None CN(C(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)C1CCCCC1)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
46235271 73301 2 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
44357058 164306 0 None -173 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 785 11 5 5 7.3 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL421921 164306 0 None -173 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 785 11 5 5 7.3 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
10794888 164700 0 None -15 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1 10.1021/jm00021a019
CHEMBL422981 164700 0 None -15 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1 10.1021/jm00021a019
16732444 142774 0 None -2570 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3cnn(CC(=O)O)c3c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL389713 142774 0 None -2570 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3cnn(CC(=O)O)c3c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44346225 161360 0 None -12022 2 Rat 5.7 pKi = 5.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 564 6 3 4 5.6 O=C(Nc1cccc(CO)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL415240 161360 0 None -12022 2 Rat 5.7 pKi = 5.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 564 6 3 4 5.6 O=C(Nc1cccc(CO)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
9985629 167496 0 None -41 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 577 8 3 3 6.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Br)cc1 10.1021/jm00072a005
CHEMBL432389 167496 0 None -41 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 577 8 3 3 6.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Br)cc1 10.1021/jm00072a005
10768308 14726 0 None -19 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 520 4 2 3 5.7 O=C(Nc1ccccc1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)C1=O 10.1021/jm990967h
CHEMBL120793 14726 0 None -19 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 520 4 2 3 5.7 O=C(Nc1ccccc1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)C1=O 10.1021/jm990967h
10506830 113468 0 None -6 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 548 6 2 3 6.5 O=C(Nc1ccccc1)NC1C(=O)N(CCC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL332601 113468 0 None -6 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 548 6 2 3 6.5 O=C(Nc1ccccc1)NC1C(=O)N(CCC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
11664728 133898 0 None -10 2 Guinea pig 5.7 pKi = 5.7 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 482 7 3 2 7.1 Cc1ccccc1-c1cc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL371750 133898 0 None -10 2 Guinea pig 5.7 pKi = 5.7 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 482 7 3 2 7.1 Cc1ccccc1-c1cc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
10554602 15123 0 None -29 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 546 7 2 4 6.3 CSc1cccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL121331 15123 0 None -29 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 546 7 2 4 6.3 CSc1cccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
10505959 112992 0 None -74 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 513 6 2 4 5.4 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL331975 112992 0 None -74 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 513 6 2 4 5.4 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
44345980 113635 0 None -79 2 Rat 7.6 pKi = 7.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 538 6 2 7 6.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(C3N=NN=N3)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL332902 113635 0 None -79 2 Rat 7.6 pKi = 7.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 538 6 2 7 6.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(C3N=NN=N3)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
44387568 61878 0 None -144 3 Guinea pig 5.7 pKi = 5.7 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 660 11 7 6 2.0 C[C@@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm0000416
CHEMBL177799 61878 0 None -144 3 Guinea pig 5.7 pKi = 5.7 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 660 11 7 6 2.0 C[C@@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm0000416
10327028 89025 0 None -144 3 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 660 11 7 6 2.0 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL2371222 89025 0 None -144 3 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 660 11 7 6 2.0 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
19700615 63823 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808417 63823 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
10652142 101099 0 None -1819 2 Guinea pig 5.7 pKi = 5.7 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 679 11 5 6 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccsc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL298521 101099 0 None -1819 2 Guinea pig 5.7 pKi = 5.7 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 679 11 5 6 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccsc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
138106885 166358 71 None -1 4 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
36314 166358 71 None -1 4 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
CHEMBL428647 166358 71 None -1 4 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
44331524 163114 0 None -13 2 Rat 6.6 pKi = 6.6 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 530 8 2 3 6.5 CC(CC1CCCC1)N1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(C(C)CC2CCCC2)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL420459 163114 0 None -13 2 Rat 6.6 pKi = 6.6 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 530 8 2 3 6.5 CC(CC1CCCC1)N1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(C(C)CC2CCCC2)c2ccccc21 10.1016/S0960-894X(96)00544-6
10101023 89027 0 None -57 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 675 11 8 7 -0.1 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CC(=O)NCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL2371224 89027 0 None -57 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 675 11 8 7 -0.1 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CC(=O)NCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL3350720 209742 0 None -4 2 Guinea pig 6.6 pKi = 6.6 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00174a016
11541870 71107 0 None -33 3 Guinea pig 5.6 pKi = 5.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 433 7 3 3 5.4 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL196141 71107 0 None -33 3 Guinea pig 5.6 pKi = 5.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 433 7 3 3 5.4 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
44451622 95470 0 None -371 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 562 9 2 5 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CCC(=O)O)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL259276 95470 0 None -371 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 562 9 2 5 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CCC(=O)O)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
44451920 95680 0 None -245 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 519 7 2 5 5.5 CNc1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
CHEMBL260394 95680 0 None -245 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 519 7 2 5 5.5 CNc1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
10325110 111495 0 None -29 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 544 9 3 5 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc([N+](=O)[O-])cc1 10.1021/jm00072a005
CHEMBL328852 111495 0 None -29 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 544 9 3 5 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc([N+](=O)[O-])cc1 10.1021/jm00072a005
10006936 205991 0 None -5 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 521 6 3 3 6.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)Nc1ccc2ccccc2c1 10.1021/jm00072a005
CHEMBL95689 205991 0 None -5 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 521 6 3 3 6.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)Nc1ccc2ccccc2c1 10.1021/jm00072a005
9985004 205884 0 None -26 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 549 8 3 3 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1cccc2ccccc12 10.1021/jm00072a005
CHEMBL95115 205884 0 None -26 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 549 8 3 3 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1cccc2ccccc12 10.1021/jm00072a005
44331506 106801 0 None -22 2 Rat 6.6 pKi = 6.6 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 574 5 2 3 6.8 O=C(Nc1cccc(Cl)c1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00544-6
CHEMBL317108 106801 0 None -22 2 Rat 6.6 pKi = 6.6 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 574 5 2 3 6.8 O=C(Nc1cccc(Cl)c1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00544-6
44346825 114275 0 None -77 2 Guinea pig 4.6 pKi = 4.6 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
CHEMBL333920 114275 0 None -77 2 Guinea pig 4.6 pKi = 4.6 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
52949124 863 2 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL3351050 209788 0 None -33 2 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12 10.1021/jm00053a022
CHEMBL171594 207105 0 None -33 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1016/S0960-894X(00)80678-2
73347063 89024 0 None -162 3 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 674 11 7 6 2.4 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL2371221 89024 0 None -162 3 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 674 11 7 6 2.4 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
22171089 93549 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(OC)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248552 93549 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(OC)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
15002730 93590 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(C(Cc2cc(-c3ccc(Cl)cc3)n(-c3ccc(OC)cc3)n2)C(=O)O)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248752 93590 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(C(Cc2cc(-c3ccc(Cl)cc3)n(-c3ccc(OC)cc3)n2)C(=O)O)cc1 10.1016/j.bmcl.2007.09.093
22171039 93591 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(C)cc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248754 93591 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(C)cc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
44444767 93624 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 432 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248948 93624 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 432 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
10343558 93625 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(Cl)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248949 93625 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(Cl)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
15002734 93626 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3OC)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248950 93626 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3OC)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
10388627 93668 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(OC)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL249151 93668 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(OC)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
10366068 93669 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(C(Cc2cc(-c3ccc(C)cc3)n(-c3ccc(OC)cc3)n2)C(=O)O)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL249153 93669 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(C(Cc2cc(-c3ccc(C)cc3)n(-c3ccc(OC)cc3)n2)C(=O)O)cc1 10.1016/j.bmcl.2007.09.093
22171037 93709 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 426 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(C)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL249361 93709 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 426 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(C)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
10320262 93736 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 426 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(C)cc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL249560 93736 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 426 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(C)cc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
44444777 93765 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 412 7 1 4 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL249763 93765 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 412 7 1 4 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
11754311 93887 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 466 7 1 4 6.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(Cl)cc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL250576 93887 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 466 7 1 4 6.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(Cl)cc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
22171092 153962 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(C)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL399055 153962 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(C)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
10433726 153963 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(Cl)cc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL399056 153963 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(Cl)cc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
22171012 154196 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 466 7 1 4 6.3 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(Cl)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL399915 154196 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 466 7 1 4 6.3 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(Cl)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
44444763 154330 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3OC)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL400670 154330 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3OC)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
45486974 196013 0 None 50 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 580 7 3 7 4.8 C[C@@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)[C@@H](O)c1cccc(Br)c1 10.1016/j.bmcl.2009.09.064
CHEMBL571206 196013 0 None 50 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 580 7 3 7 4.8 C[C@@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)[C@@H](O)c1cccc(Br)c1 10.1016/j.bmcl.2009.09.064
44271963 96277 0 None -4466 2 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)[C@H](NC(=O)OC(C)(C)C)CCC(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL264273 96277 0 None -4466 2 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)[C@H](NC(=O)OC(C)(C)C)CCC(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
11555184 165479 0 None -281 3 Guinea pig 6.6 pKi = 6.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 503 7 3 3 7.0 Cc1ccc(NC(=O)c2[nH]c(C3(C)CCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm0490686
CHEMBL425574 165479 0 None -281 3 Guinea pig 6.6 pKi = 6.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 503 7 3 3 7.0 Cc1ccc(NC(=O)c2[nH]c(C3(C)CCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm0490686
45255234 197358 0 None -15 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 584 8 3 7 4.9 O=C(N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL585914 197358 0 None -15 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 584 8 3 7 4.9 O=C(N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486935 195084 0 None -25 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 612 8 3 7 4.5 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL565298 195084 0 None -25 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 612 8 3 7 4.5 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
45486976 197294 0 None -39 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 656 8 3 7 4.6 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL585157 197294 0 None -39 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 656 8 3 7 4.6 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
10792724 14295 0 None -162 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 548 5 2 3 6.4 Cc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL120031 14295 0 None -162 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 548 5 2 3 6.4 Cc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
10793611 15325 0 None -4 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 594 7 2 4 7.2 CSc1cccc(NC(=O)NC2C(=O)N(CCC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL121624 15325 0 None -4 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 594 7 2 4 7.2 CSc1cccc(NC(=O)NC2C(=O)N(CCC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
19043400 98288 0 None -162 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 480 4 2 3 5.1 O=C(Nc1ccccc1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2CC3CCC2C3)C1=O 10.1021/jm990967h
CHEMBL278018 98288 0 None -162 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 480 4 2 3 5.1 O=C(Nc1ccccc1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2CC3CCC2C3)C1=O 10.1021/jm990967h
9869202 71732 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm0490686
CHEMBL197716 71732 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm0490686
CHEMBL2067960 71732 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm0490686
44444930 154383 0 None - 1 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 688 11 6 6 5.7 Nc1cccc2cc(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)c(C(=O)NCC34CC5CC(CC(C5)C3)C4)cc12 10.1021/jm070880t
CHEMBL400974 154383 0 None - 1 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 688 11 6 6 5.7 Nc1cccc2cc(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)c(C(=O)NCC34CC5CC(CC(C5)C3)C4)cc12 10.1021/jm070880t
44444931 154406 0 None - 1 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 688 11 6 6 5.7 Nc1cccc2cc(C(=O)NCC34CC5CC(CC(C5)C3)C4)c(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)cc12 10.1021/jm070880t
CHEMBL401097 154406 0 None - 1 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 688 11 6 6 5.7 Nc1cccc2cc(C(=O)NCC34CC5CC(CC(C5)C3)C4)c(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)cc12 10.1021/jm070880t
16090789 82837 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 521 6 2 7 4.4 O=C(Nc1ccc(C(=O)N2CCCCC2)c(NS(=O)(=O)c2cccc3nsnc23)c1)c1ccccc1 10.1021/jm060590x
CHEMBL218729 82837 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 521 6 2 7 4.4 O=C(Nc1ccc(C(=O)N2CCCCC2)c(NS(=O)(=O)c2cccc3nsnc23)c1)c1ccccc1 10.1021/jm060590x
16733466 85092 0 None -7413 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 558 10 2 5 5.6 O=C(O)CCc1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1021/jm070139l
CHEMBL227330 85092 0 None -7413 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 558 10 2 5 5.6 O=C(O)CCc1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1021/jm070139l
16732165 168382 0 None -3235 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 571 8 2 6 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3c(ccn3CC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL438843 168382 0 None -3235 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 571 8 2 6 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3c(ccn3CC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
9936141 12156 0 None -12 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 510 7 4 3 7.0 O=C(O)c1cc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184700 12156 0 None -12 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 510 7 4 3 7.0 O=C(O)c1cc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067956 12156 0 None -12 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 510 7 4 3 7.0 O=C(O)c1cc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
9869202 71732 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm049069y
CHEMBL197716 71732 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm049069y
CHEMBL2067960 71732 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm049069y
44444932 154312 0 None - 1 Guinea pig 4.6 pKi = 4.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 623 8 3 4 4.8 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)C(=O)O 10.1021/jm070880t
CHEMBL400548 154312 0 None - 1 Guinea pig 4.6 pKi = 4.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 623 8 3 4 4.8 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)C(=O)O 10.1021/jm070880t
44357208 118478 0 None -4 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 737 10 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)c2ccccc2)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL342465 118478 0 None -4 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 737 10 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)c2ccccc2)cc(C(=O)O)c1 10.1021/jm00021a019
56673524 63824 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808418 63824 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
10842269 101103 0 None -575 2 Guinea pig 5.6 pKi = 5.6 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 681 11 6 6 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL298551 101103 0 None -575 2 Guinea pig 5.6 pKi = 5.6 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 681 11 6 6 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
10698746 116285 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 595 7 3 4 4.0 O=C(O)CNC(=O)[C@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3 10.1021/jm00021a019
CHEMBL337743 116285 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 595 7 3 4 4.0 O=C(O)CNC(=O)[C@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3 10.1021/jm00021a019
19700615 63823 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808417 63823 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
11799257 112968 0 None -32 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 490 6 2 3 5.1 O=C(Nc1ccccc1)NC1C(=O)N(CCc2ccccc2)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL331929 112968 0 None -32 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 490 6 2 3 5.1 O=C(Nc1ccccc1)NC1C(=O)N(CCc2ccccc2)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
10795162 118533 0 None -630 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL2067970 118533 0 None -630 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL342616 118533 0 None -630 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
19700643 63688 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1807152 63688 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
10439779 106204 0 None -5 3 Guinea pig 6.6 pKi = 6.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 710 11 7 8 2.2 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCSSCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL3143501 106204 0 None -5 3 Guinea pig 6.6 pKi = 6.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 710 11 7 8 2.2 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCSSCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
52949124 863 2 None -2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
56663144 63808 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 507 8 2 5 3.2 Cc1cccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)c1 10.1016/j.bmc.2011.05.057
CHEMBL1808400 63808 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 507 8 2 5 3.2 Cc1cccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)c1 10.1016/j.bmc.2011.05.057
46235271 73301 2 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
887 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm070139l
9870520 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm070139l
CHEMBL324547 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm070139l
DB12355 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm070139l
44451581 95381 0 None -316 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 594 9 2 6 6.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCC(=O)O)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL258863 95381 0 None -316 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 594 9 2 6 6.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCC(=O)O)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
10652140 101374 0 None -177 2 Guinea pig 5.6 pKi = 5.6 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 679 11 7 7 4.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL300456 101374 0 None -177 2 Guinea pig 5.6 pKi = 5.6 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 679 11 7 7 4.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
44329398 205954 0 None -12 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 543 10 3 4 4.8 O=C(O)CN(CCc1ccccc1)C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00072a005
CHEMBL95461 205954 0 None -12 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 543 10 3 4 4.8 O=C(O)CN(CCc1ccccc1)C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00072a005
10098459 4201 0 None -208 2 Rat 6.5 pKi = 6.5 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 528 7 2 3 5.8 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL100548 4201 0 None -208 2 Rat 6.5 pKi = 6.5 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 528 7 2 3 5.8 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
73354642 89028 0 None -46 3 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 646 11 7 6 1.6 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL2371225 89028 0 None -46 3 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 646 11 7 6 1.6 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
11568611 71635 0 None -263 3 Guinea pig 5.5 pKi = 5.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 449 6 3 3 5.8 CC(C)(C)c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL197370 71635 0 None -263 3 Guinea pig 5.5 pKi = 5.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 449 6 3 3 5.8 CC(C)(C)c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
5311188 9712 2 None -1 2 Rat 5.5 pKi = 5.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm9703247
CHEMBL113718 9712 2 None -1 2 Rat 5.5 pKi = 5.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm9703247
44265912 204681 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 354 6 2 1 5.1 O=C(NCCC(c1ccccc1)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
CHEMBL8779 204681 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 354 6 2 1 5.1 O=C(NCCC(c1ccccc1)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
44346355 157325 0 None -446 3 Guinea pig 5.5 pKi = 5.5 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 1260 26 13 15 1.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0000416
CHEMBL408389 157325 0 None -446 3 Guinea pig 5.5 pKi = 5.5 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 1260 26 13 15 1.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0000416
CHEMBL2370588 208127 0 None -446 2 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL3350335 209728 0 None -245 2 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
CHEMBL3142843 209390 0 None -6 2 Guinea pig 4.5 pKi = 4.5 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CC(C)(C)OC(=O)NCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00174a016
11495719 70030 0 None -14 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 431 7 3 3 5.8 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC2CCCCC2)[nH]1 10.1021/jm0490686
CHEMBL194514 70030 0 None -14 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 431 7 3 3 5.8 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC2CCCCC2)[nH]1 10.1021/jm0490686
10817243 113018 0 None -22 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 591 7 2 4 6.6 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL332128 113018 0 None -22 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 591 7 2 4 6.6 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
16733051 136433 0 None -758 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 595 8 2 7 4.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)NS(C)(=O)=O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL374390 136433 0 None -758 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 595 8 2 7 4.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)NS(C)(=O)=O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
11800981 10114 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm9703247
CHEMBL116001 10114 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm9703247
44379428 57866 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibitory activity against CCK-A receptorInhibitory activity against CCK-A receptor
ChEMBL 557 9 3 6 4.9 C[C@@](N)(Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80669-1
CHEMBL168182 57866 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibitory activity against CCK-A receptorInhibitory activity against CCK-A receptor
ChEMBL 557 9 3 6 4.9 C[C@@](N)(Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80669-1
CHEMBL1206136 206862 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL218455 206862 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
10372489 4198 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 692 20 7 7 1.3 CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)O 10.1021/jm0000416
CHEMBL100538 4198 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 692 20 7 7 1.3 CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)O 10.1021/jm0000416
44359425 14575 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL1206331 14575 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL262687 14575 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
90662935 106093 0 None 10 2 Rat 8.5 pKi = 8.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1057 30 11 11 2.6 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL3142373 106093 0 None 10 2 Rat 8.5 pKi = 8.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1057 30 11 11 2.6 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
53465844 69068 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 W39A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 W39A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 W39A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 W39A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10075052 189082 0 None 10 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL515268 189082 0 None 10 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL515288 189082 0 None 10 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
53465844 69068 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 F107A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 F107A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 F107A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 F107A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
44215880 69065 0 None 3890 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)NC(CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933100 69065 0 None 3890 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)NC(CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
887 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm051219x
9870520 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm051219x
CHEMBL324547 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm051219x
DB12355 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm051219x
10460632 206589 0 None -43 2 Human 5.5 pKi = 5.5 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 568 10 2 4 5.8 CC(Cc1ccc2ccccc2c1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99252 206589 0 None -43 2 Human 5.5 pKi = 5.5 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 568 10 2 4 5.8 CC(Cc1ccc2ccccc2c1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
9890720 167905 0 None -2 2 Guinea pig 5.5 pKi = 5.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm0490686
CHEMBL2067971 167905 0 None -2 2 Guinea pig 5.5 pKi = 5.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm0490686
CHEMBL435127 167905 0 None -2 2 Guinea pig 5.5 pKi = 5.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm0490686
44356448 167676 0 None -75 2 Guinea pig 6.5 pKi = 6.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2cccc(F)c2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL433656 167676 0 None -75 2 Guinea pig 6.5 pKi = 6.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2cccc(F)c2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
44356666 168064 0 None -16 2 Guinea pig 6.5 pKi = 6.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 799 11 3 11 5.2 O=C(NCC12CC3CC(CC(C3)C1)C2)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-n2cnnn2)cc(-n2cnnn2)c1 10.1021/jm00021a019
CHEMBL436187 168064 0 None -16 2 Guinea pig 6.5 pKi = 6.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 799 11 3 11 5.2 O=C(NCC12CC3CC(CC(C3)C1)C2)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-n2cnnn2)cc(-n2cnnn2)c1 10.1021/jm00021a019
11643045 71794 0 None -43 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 511 9 3 3 6.8 Cc1ccccc1-c1nc(C(=O)Nc2cccc(CCC(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL197873 71794 0 None -43 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 511 9 3 3 6.8 Cc1ccccc1-c1nc(C(=O)Nc2cccc(CCC(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
10793342 112606 0 None -158 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 579 6 2 5 6.0 O=C(Nc1cccc([N+](=O)[O-])c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL331405 112606 0 None -158 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 579 6 2 5 6.0 O=C(Nc1cccc([N+](=O)[O-])c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44329798 107063 0 None -245 5 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 610 10 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(C(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
CHEMBL318852 107063 0 None -245 5 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 610 10 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(C(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
19700615 63823 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808417 63823 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
887 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1016/j.bmc.2007.12.047
9870520 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1016/j.bmc.2007.12.047
CHEMBL324547 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1016/j.bmc.2007.12.047
DB12355 4047 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1016/j.bmc.2007.12.047
11534594 197122 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 616 8 2 6 7.0 O=C(NCC(c1ccc(Cl)cc1)c1ccc(Cl)cc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL583343 197122 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 616 8 2 6 7.0 O=C(NCC(c1ccc(Cl)cc1)c1ccc(Cl)cc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
10071178 74146 1 None 501 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm060590x
CHEMBL202861 74146 1 None 501 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm060590x
CHEMBL3350665 209736 0 None -3 2 Guinea pig 6.5 pKi = 6.5 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
44272041 96636 0 None -338 2 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL267329 96636 0 None -338 2 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
10459641 111746 0 None -26 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 529 9 3 4 5.4 COc1ccc(CCNC(=O)C(C)(Cc2c[nH]c3ccccc23)NC(=O)OC2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)cc1 10.1021/jm00072a005
CHEMBL329088 111746 0 None -26 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 529 9 3 4 5.4 COc1ccc(CCNC(=O)C(C)(Cc2c[nH]c3ccccc23)NC(=O)OC2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)cc1 10.1021/jm00072a005
45486968 195793 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 550 8 3 7 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL569848 195793 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 550 8 3 7 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486985 196076 0 None -63 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 650 8 3 6 4.5 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
CHEMBL571650 196076 0 None -63 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 650 8 3 6 4.5 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
10411553 153361 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 452 4 3 6 2.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(-c3nnn[nH]3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm070880t
CHEMBL398312 153361 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 452 4 3 6 2.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(-c3nnn[nH]3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm070880t
5311201 205663 30 None -2570 6 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm070880t
CHEMBL9387 205663 30 None -2570 6 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm070880t
136036823 155137 0 None -263 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 574 7 2 7 4.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL404967 155137 0 None -263 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 574 7 2 7 4.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
10099495 107247 0 None -117 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 567 8 3 3 6.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)cc1Cl 10.1021/jm00072a005
CHEMBL319120 107247 0 None -117 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 567 8 3 3 6.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)cc1Cl 10.1021/jm00072a005
45486958 195911 0 None -19 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 8 3 7 3.6 O=C(N[C@H](Cc1ccccc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL570518 195911 0 None -19 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 8 3 7 3.6 O=C(N[C@H](Cc1ccccc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
44444928 154079 0 None - 1 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 610 10 6 5 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL399252 154079 0 None - 1 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 610 10 6 5 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm070880t
16090699 141384 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 463 8 4 4 3.4 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccccc1NS(=O)(=O)c1cc2ccccc2[nH]1 10.1021/jm060590x
CHEMBL386985 141384 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 463 8 4 4 3.4 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccccc1NS(=O)(=O)c1cc2ccccc2[nH]1 10.1021/jm060590x
10603971 101144 0 None -208 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 624 11 6 5 5.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL298861 101144 0 None -208 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 624 11 6 5 5.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm9508907
9958028 11699 0 None -12 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 511 7 4 4 6.4 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1181937 11699 0 None -12 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 511 7 4 4 6.4 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067950 11699 0 None -12 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 511 7 4 4 6.4 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
9956948 11823 0 None 1 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 483 7 4 4 6.0 O=C(Nc1cc(CO)cc(CO)c1)c1[nH]c(-c2ccc3ccccc3c2)nc1CC1CCCCCC1 10.1021/jm049069y
CHEMBL1182723 11823 0 None 1 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 483 7 4 4 6.0 O=C(Nc1cc(CO)cc(CO)c1)c1[nH]c(-c2ccc3ccccc3c2)nc1CC1CCCCCC1 10.1021/jm049069y
CHEMBL2067953 11823 0 None 1 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 483 7 4 4 6.0 O=C(Nc1cc(CO)cc(CO)c1)c1[nH]c(-c2ccc3ccccc3c2)nc1CC1CCCCCC1 10.1021/jm049069y
11576933 12162 0 None -19 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 499 7 4 4 5.5 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184725 12162 0 None -19 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 499 7 4 4 5.5 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067957 12162 0 None -19 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 499 7 4 4 5.5 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
44404005 12179 0 None -100 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 623 11 5 5 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184845 12179 0 None -100 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 623 11 5 5 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067963 12179 0 None -100 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 623 11 5 5 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL206974 207438 0 None -72 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm0303103
CHEMBL1172249 206840 0 None -5 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
CHEMBL206974 207438 0 None -72 5 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
CHEMBL3351048 209786 0 None -5 2 Guinea pig 5.5 pKi = 5.5 Binding
Affinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membraneAffinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membrane
ChEMBL None None None CN(C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
CHEMBL407057 210888 0 None -1513 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O 10.1021/jm050921q
11513177 72184 0 None -131 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 501 7 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(C34CCC(CC3)CC4)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL199091 72184 0 None -131 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 501 7 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(C34CCC(CC3)CC4)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
10004216 4675 0 None -11 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL103750 4675 0 None -11 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
18472063 63826 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 529 7 2 4 4.3 CN(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808420 63826 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 529 7 2 4 4.3 CN(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1206136 206862 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
CHEMBL218455 206862 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00122a026
54554106 63817 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 451 8 2 4 3.2 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN(C)C)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808411 63817 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 451 8 2 4 3.2 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN(C)C)c2ccccc21 10.1016/j.bmc.2011.05.057
10723216 161446 0 None -4466 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 680 11 6 5 5.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL415936 161446 0 None -4466 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 680 11 6 5 5.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL265595 208910 0 None -1584 4 Human 5.5 pKi = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O 10.1021/jm0303103
10604664 154696 0 None -602 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 691 9 2 7 5.6 O=C(Nc1cccc(C(=O)OCCN2CCOCC2)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL402702 154696 0 None -602 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 691 9 2 7 5.6 O=C(Nc1cccc(C(=O)OCCN2CCOCC2)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
10580234 98577 0 None -251 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]ccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL280248 98577 0 None -251 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]ccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL3350331 209727 0 None 1 2 Guinea pig 6.5 pKi = 6.5 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
CHEMBL3350665 209736 0 None -3 2 Guinea pig 6.5 pKi = 6.5 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
44265916 205861 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 352 5 2 1 5.0 O=C(NCC=C(c1ccccc1)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
CHEMBL9500 205861 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 352 5 2 1 5.0 O=C(NCC=C(c1ccccc1)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
CHEMBL2371662 208361 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00389a002
10031454 108101 0 None -67 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 596 10 2 4 5.5 CC(Cc1ccc(Br)cc1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL320399 108101 0 None -67 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 596 10 2 4 5.5 CC(Cc1ccc(Br)cc1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
56659684 63820 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 519 7 2 5 3.5 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC2CCCCC2)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808414 63820 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 519 7 2 5 3.5 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC2CCCCC2)C1=O 10.1016/j.bmc.2011.05.057
10508004 11694 0 None -2454 2 Rat 5.5 pKi = 5.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1ccc(Br)cc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL118189 11694 0 None -2454 2 Rat 5.5 pKi = 5.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1ccc(Br)cc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44382456 119955 0 None -3162 3 Rat 6.5 pKi = 6.5 Binding
The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 572 10 5 5 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)cc1 10.1016/S0960-894X(00)80686-1
CHEMBL354049 119955 0 None -3162 3 Rat 6.5 pKi = 6.5 Binding
The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 572 10 5 5 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)cc1 10.1016/S0960-894X(00)80686-1
CHEMBL83942 119955 0 None -3162 3 Rat 6.5 pKi = 6.5 Binding
The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 572 10 5 5 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)cc1 10.1016/S0960-894X(00)80686-1
CHEMBL3351061 209796 0 None -4 2 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CN(C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
9867157 99778 4 None 194 2 Guinea pig 6.5 pKi = 6.5 Binding
In vitro affinity against Cholecystokinin type A receptor in guinea pig pancreatic cellIn vitro affinity against Cholecystokinin type A receptor in guinea pig pancreatic cell
ChEMBL 426 9 3 4 2.3 O=C(O)C[C@H](NS(=O)(=O)c1ccc2ccccc2c1)C(=O)NCCc1ccccc1 10.1016/S0960-894X(00)80008-6
CHEMBL288641 99778 4 None 194 2 Guinea pig 6.5 pKi = 6.5 Binding
In vitro affinity against Cholecystokinin type A receptor in guinea pig pancreatic cellIn vitro affinity against Cholecystokinin type A receptor in guinea pig pancreatic cell
ChEMBL 426 9 3 4 2.3 O=C(O)C[C@H](NS(=O)(=O)c1ccc2ccccc2c1)C(=O)NCCc1ccccc1 10.1016/S0960-894X(00)80008-6
44356825 168068 0 None -1621 2 Guinea pig 5.5 pKi = 5.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 767 11 6 6 6.3 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL436209 168068 0 None -1621 2 Guinea pig 5.5 pKi = 5.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 767 11 6 6 6.3 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
11798204 192995 0 None -10 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 460 5 2 3 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2ccccc2cc1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm9508907
CHEMBL53129 192995 0 None -10 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 460 5 2 3 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2ccccc2cc1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm9508907
10815832 15013 0 None -109 2 Rat 7.4 pKi = 7.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 520 7 2 4 5.8 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL121021 15013 0 None -109 2 Rat 7.4 pKi = 7.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 520 7 2 4 5.8 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL218763 207654 0 None -3630 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
CHEMBL120632 206863 30 None -2187 3 Guinea pig 4.4 pKi = 4.4 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0000416
CHEMBL120632 206863 30 None -2187 3 Guinea pig 4.4 pKi = 4.4 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm9603072
9939572 37258 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL14557 37258 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL2067949 37258 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
16731711 85094 0 None -15 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 570 7 2 5 5.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1021/jm070139l
CHEMBL227369 85094 0 None -15 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 570 7 2 5 5.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1021/jm070139l
10676212 115509 0 None -489 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 701 8 4 5 5.9 O=C(O)c1cc(NC(=O)[C@H]2CCCN2C(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL335587 115509 0 None -489 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 701 8 4 5 5.9 O=C(O)c1cc(NC(=O)[C@H]2CCCN2C(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
44280162 98997 0 None -21 2 Guinea pig 5.4 pKi = 5.4 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 667 8 3 5 6.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1CC[C@H](Oc2ccc(Cl)cc2Cl)C[C@@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
CHEMBL283040 98997 0 None -21 2 Guinea pig 5.4 pKi = 5.4 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 667 8 3 5 6.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1CC[C@H](Oc2ccc(Cl)cc2Cl)C[C@@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
10324322 107219 0 None -43 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 518 10 2 4 4.7 CC(Cc1ccccc1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL319085 107219 0 None -43 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 518 10 2 4 4.7 CC(Cc1ccccc1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
10484529 100963 0 None -707 2 Guinea pig 5.4 pKi = 5.4 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 663 11 5 6 5.8 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccoc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL297480 100963 0 None -707 2 Guinea pig 5.4 pKi = 5.4 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 663 11 5 6 5.8 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccoc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
44272042 96599 0 None -131 2 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL266990 96599 0 None -131 2 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
16732021 167911 0 None -549 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 588 9 2 8 5.3 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL435143 167911 0 None -549 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 588 9 2 8 5.3 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44451843 158892 0 None -1230 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 562 8 2 5 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CC(=O)O)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL410114 158892 0 None -1230 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 562 8 2 5 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CC(=O)O)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
53465844 69068 0 None 131 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 I352A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 I352A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 I352A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 I352A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL132314 206960 0 None -6456 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0303103
44461961 105130 0 None -446 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 724 11 4 5 6.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N=[N+]=[N-])c(I)c1 10.1016/0960-894X(95)00435-V
CHEMBL2079605 105130 0 None -446 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 724 11 4 5 6.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N=[N+]=[N-])c(I)c1 10.1016/0960-894X(95)00435-V
CHEMBL312252 105130 0 None -446 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 724 11 4 5 6.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N=[N+]=[N-])c(I)c1 10.1016/0960-894X(95)00435-V
11547802 135480 0 None -177 2 Guinea pig 6.4 pKi = 6.4 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 8 3 3 6.4 Cc1ccccc1-c1nc(C(=O)Nc2cccc(CC(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL373168 135480 0 None -177 2 Guinea pig 6.4 pKi = 6.4 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 8 3 3 6.4 Cc1ccccc1-c1nc(C(=O)Nc2cccc(CC(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
45486941 195089 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 7 2 6 4.2 O=C(NCCc1ccccc1)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL565325 195089 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 7 2 6 4.2 O=C(NCCc1ccccc1)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486964 195718 0 None -39 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 606 8 3 6 4.4 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
CHEMBL569391 195718 0 None -39 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 606 8 3 6 4.4 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
887 4047 24 None -5011 4 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm070880t
9870520 4047 24 None -5011 4 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm070880t
CHEMBL324547 4047 24 None -5011 4 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm070880t
DB12355 4047 24 None -5011 4 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 10.1021/jm070880t
45486949 195270 0 None -50 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 8 3 7 3.6 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL566390 195270 0 None -50 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 8 3 7 3.6 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486970 195952 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 578 8 3 7 5.0 CC(C)(c1ccc(Cl)cc1)[C@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
CHEMBL570761 195952 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 578 8 3 7 5.0 CC(C)(c1ccc(Cl)cc1)[C@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
45486997 196106 0 None -12 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 486 7 1 6 4.5 CN(CCc1ccccc1)C(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL571832 196106 0 None -12 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 486 7 1 6 4.5 CN(CCc1ccccc1)C(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
9939572 37258 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL14557 37258 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL2067949 37258 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
10327180 37401 0 None - 1 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 676 11 5 6 5.5 Cn1ccc2cc(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)c(C(=O)NCC34CC5CC(CC(C5)C3)C4)cc21 10.1021/jm070880t
CHEMBL14571 37401 0 None - 1 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 676 11 5 6 5.5 Cn1ccc2cc(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)c(C(=O)NCC34CC5CC(CC(C5)C3)C4)cc21 10.1021/jm070880t
44425006 141548 0 None -3311 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 544 8 2 5 5.6 CC1CCCC1C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL388068 141548 0 None -3311 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 544 8 2 5 5.6 CC1CCCC1C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44404001 11828 0 None -6 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 635 11 6 6 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(CO)cc(CO)c1 10.1021/jm049069y
CHEMBL1182744 11828 0 None -6 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 635 11 6 6 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(CO)cc(CO)c1 10.1021/jm049069y
CHEMBL2067969 11828 0 None -6 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 635 11 6 6 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(CO)cc(CO)c1 10.1021/jm049069y
44403982 12172 0 None -7 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 4.9 CN(C(=O)[C@H](Cc1ccccc1)NC(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)c1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184798 12172 0 None -7 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 4.9 CN(C(=O)[C@H](Cc1ccccc1)NC(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)c1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067958 12172 0 None -7 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 4.9 CN(C(=O)[C@H](Cc1ccccc1)NC(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)c1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
9939572 37258 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL14557 37258 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067949 37258 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
9890720 167905 0 None -2 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm049069y
CHEMBL2067971 167905 0 None -2 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm049069y
CHEMBL435127 167905 0 None -2 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm049069y
10509945 88954 0 None 229 2 Rat 8.4 pKi = 8.4 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL2369816 88954 0 None 229 2 Rat 8.4 pKi = 8.4 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL384035 210569 1 None -22 4 Rat 8.4 pKi = 8.4 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00389a002
CHEMBL428666 210569 1 None -22 4 Rat 8.4 pKi = 8.4 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00389a002
10508430 16163 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 648 18 6 6 1.8 CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC 10.1021/jm0000416
CHEMBL122872 16163 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 648 18 6 6 1.8 CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC 10.1021/jm0000416
44332766 107850 0 None 48 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(F)ccc21 10.1016/0960-894X(95)00528-2
CHEMBL319795 107850 0 None 48 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(F)ccc21 10.1016/0960-894X(95)00528-2
19043395 4705 0 None 194 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 490 6 2 3 5.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(Cl)ccc21 10.1016/0960-894X(95)00528-2
CHEMBL103968 4705 0 None 194 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 490 6 2 3 5.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(Cl)ccc21 10.1016/0960-894X(95)00528-2
53465844 69068 0 None 131 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-SR-27897 from human CCK1 F330A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 F330A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-SR-27897 from human CCK1 F330A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 F330A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
44265985 205939 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 376 6 2 1 6.0 O=C(NCCC=C(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
CHEMBL9538 205939 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 376 6 2 1 6.0 O=C(NCCC=C(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
44265913 204867 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 381 5 1 1 5.9 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1021/jm00084a009
CHEMBL8893 204867 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 381 5 1 1 5.9 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1021/jm00084a009
10604230 114713 0 None -5 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 645 10 4 4 4.8 O=C(O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
CHEMBL334523 114713 0 None -5 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 645 10 4 4 4.8 O=C(O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
10676196 118735 0 None -234 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 699 11 5 5 6.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC2CCCCC2)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL343515 118735 0 None -234 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 699 11 5 5 6.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC2CCCCC2)cc(C(=O)O)c1 10.1021/jm00021a019
56673523 63819 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 479 10 2 4 3.9 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808413 63819 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 479 10 2 4 3.9 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/j.bmc.2011.05.057
16732018 85043 0 None -741 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 548 9 2 6 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(OCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL226729 85043 0 None -741 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 548 9 2 6 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(OCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
10769001 112682 0 None -13803 2 Rat 5.4 pKi = 5.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 549 5 3 4 5.7 Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL331468 112682 0 None -13803 2 Rat 5.4 pKi = 5.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 549 5 3 4 5.7 Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
10390666 206564 0 None -17 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 485 7 3 3 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCc1ccccc1 10.1021/jm00072a005
CHEMBL99076 206564 0 None -17 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 485 7 3 3 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCc1ccccc1 10.1021/jm00072a005
19043358 4295 0 None 22 2 Rat 7.4 pKi = 7.4 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 490 6 2 3 5.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccc(Cl)cc21 10.1016/0960-894X(95)00528-2
CHEMBL101125 4295 0 None 22 2 Rat 7.4 pKi = 7.4 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 490 6 2 3 5.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccc(Cl)cc21 10.1016/0960-894X(95)00528-2
44408524 155164 0 None -169 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL405192 155164 0 None -169 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
11605694 168088 0 None -70 3 Guinea pig 6.4 pKi = 6.4 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 7 3 3 6.8 Cc1ccc(NC(=O)c2[nH]c(-c3ccccc3C)nc2CCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm0490686
CHEMBL436314 168088 0 None -70 3 Guinea pig 6.4 pKi = 6.4 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 7 3 3 6.8 Cc1ccc(NC(=O)c2[nH]c(-c3ccccc3C)nc2CCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm0490686
10818497 25648 0 None -58 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 701 8 4 5 5.9 O=C(O)c1cc(NC(=O)[C@@H]2CCCN2C(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL135344 25648 0 None -58 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 701 8 4 5 5.9 O=C(O)c1cc(NC(=O)[C@@H]2CCCN2C(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL3351054 209792 0 None -812 2 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
9983949 206007 0 None -23 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 513 9 3 3 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCCc1ccccc1 10.1021/jm00072a005
CHEMBL95793 206007 0 None -23 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 513 9 3 3 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCCc1ccccc1 10.1021/jm00072a005
52949124 863 2 None -2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 863 2 None -2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 863 2 None -2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 863 2 None -2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10531553 116130 0 None -31 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 595 7 3 4 4.0 O=C(O)CNC(=O)[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3 10.1021/jm00021a019
CHEMBL336896 116130 0 None -31 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 595 7 3 4 4.0 O=C(O)CNC(=O)[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3 10.1021/jm00021a019
44346345 112585 0 None -43 2 Rat 7.4 pKi = 7.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 523 5 2 4 5.1 CN(C)c1cccc(NC(=O)NC2C(=O)N(c3ccccc3)c3ccccc3N(C3CC4CCC3C4)C2=O)c1 10.1021/jm990967h
CHEMBL331262 112585 0 None -43 2 Rat 7.4 pKi = 7.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 523 5 2 4 5.1 CN(C)c1cccc(NC(=O)NC2C(=O)N(c3ccccc3)c3ccccc3N(C3CC4CCC3C4)C2=O)c1 10.1021/jm990967h
10747623 168914 0 None -29 2 Guinea pig 6.4 pKi = 6.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 746 12 6 5 6.1 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCCc2c[nH]c3ccccc23)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL443028 168914 0 None -29 2 Guinea pig 6.4 pKi = 6.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 746 12 6 5 6.1 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCCc2c[nH]c3ccccc23)cc(C(=O)O)c1 10.1021/jm00021a019
44451519 95313 0 None -58 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 518 6 1 4 6.1 Cc1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
CHEMBL258486 95313 0 None -58 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 518 6 1 4 6.1 Cc1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
10579091 14257 0 None -398 2 Rat 6.4 pKi = 6.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 577 6 2 4 6.2 CN(C)c1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL120021 14257 0 None -398 2 Rat 6.4 pKi = 6.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 577 6 2 4 6.2 CN(C)c1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
44265914 204952 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 363 5 1 1 5.7 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc2ccccc2c1 10.1021/jm00084a009
CHEMBL8949 204952 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 363 5 1 1 5.7 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc2ccccc2c1 10.1021/jm00084a009
16732162 141561 0 None -1862 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 584 8 2 6 6.4 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3ccc(C(=O)O)o3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL388144 141561 0 None -1862 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 584 8 2 6 6.4 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3ccc(C(=O)O)o3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
10004216 4675 0 None -11 2 Rat 5.3 pKi = 5.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL103750 4675 0 None -11 2 Rat 5.3 pKi = 5.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
44346255 116381 0 None -30 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 564 6 2 7 6.7 CC(C)(C1CCCC1)N1C(=O)C(NC(=O)Nc2cccc(C3N=NN=N3)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL338278 116381 0 None -30 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 564 6 2 7 6.7 CC(C)(C1CCCC1)N1C(=O)C(NC(=O)Nc2cccc(C3N=NN=N3)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
19700643 63688 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1807152 63688 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
135423404 85087 0 None -4365 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 570 8 2 7 5.0 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C2CCCC2)C1=O)Nc1cccc(-c2noc(=O)[nH]2)c1 10.1021/jm070139l
CHEMBL227276 85087 0 None -4365 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 570 8 2 7 5.0 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C2CCCC2)C1=O)Nc1cccc(-c2noc(=O)[nH]2)c1 10.1021/jm070139l
5311201 205663 30 None -2570 6 Guinea pig 6.3 pKi = 6.3 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00048a001
CHEMBL9387 205663 30 None -2570 6 Guinea pig 6.3 pKi = 6.3 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00048a001
115208 3758 25 None -91 4 Rat 7.3 pKi = 7.3 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.
ChEMBL 393 4 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm950423p
1667 3758 25 None -91 4 Rat 7.3 pKi = 7.3 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.
ChEMBL 393 4 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm950423p
CHEMBL169703 3758 25 None -91 4 Rat 7.3 pKi = 7.3 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.
ChEMBL 393 4 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm950423p
44346126 15097 0 None -27 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 514 4 2 3 5.7 O=C(Nc1cccc(Cl)c1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2CC3CCC2C3)C1=O 10.1021/jm990967h
CHEMBL121267 15097 0 None -27 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 514 4 2 3 5.7 O=C(Nc1cccc(Cl)c1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2CC3CCC2C3)C1=O 10.1021/jm990967h
10792618 163801 0 None -70 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 543 7 2 4 5.7 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL421271 163801 0 None -70 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 543 7 2 4 5.7 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
44265917 205880 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 364 5 1 2 5.1 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc2ccccc2n1 10.1021/jm00084a009
CHEMBL9510 205880 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 364 5 1 2 5.1 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc2ccccc2n1 10.1021/jm00084a009
9850043 112375 1 None -446 3 Rat 6.3 pKi = 6.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL330977 112375 1 None -446 3 Rat 6.3 pKi = 6.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
10603576 14346 0 None -19 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 594 8 2 7 5.6 CC(C)Cn1nnc(-c2cccc(NC(=O)NC3C(=O)N(CCC(C)(C)C)c4ccccc4N(c4ccccc4)C3=O)c2)n1 10.1021/jm990967h
CHEMBL120168 14346 0 None -19 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 594 8 2 7 5.6 CC(C)Cn1nnc(-c2cccc(NC(=O)NC3C(=O)N(CCC(C)(C)C)c4ccccc4N(c4ccccc4)C3=O)c2)n1 10.1021/jm990967h
10747599 25656 0 None -46 2 Guinea pig 6.3 pKi = 6.3 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 743 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCc2cccc3ccccc23)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL135350 25656 0 None -46 2 Guinea pig 6.3 pKi = 6.3 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 743 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCc2cccc3ccccc23)cc(C(=O)O)c1 10.1021/jm00021a019
13605417 205834 3 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00084a009
CHEMBL9485 205834 3 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00084a009
53465844 69068 0 None 131 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-BH-JMV-179 from human CCK1 receptor N333A mutant expressed in COS7 cells after 60 mins by gamma countingDisplacement of [125I]-BH-JMV-179 from human CCK1 receptor N333A mutant expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-BH-JMV-179 from human CCK1 receptor N333A mutant expressed in COS7 cells after 60 mins by gamma countingDisplacement of [125I]-BH-JMV-179 from human CCK1 receptor N333A mutant expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
53465844 69068 0 None 131 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-SR-27897 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-SR-27897 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10507109 108740 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
CHEMBL321761 108740 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
11512151 195111 0 None 158 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 534 7 2 6 5.5 CC(C)(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.09.064
CHEMBL565511 195111 0 None 158 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 534 7 2 6 5.5 CC(C)(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.09.064
44328951 164045 0 None -3 2 Human 7.3 pKi = 7.3 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line (n=1)
ChEMBL 533 5 2 4 3.8 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1016/S0960-894X(96)00613-0
CHEMBL421575 164045 0 None -3 2 Human 7.3 pKi = 7.3 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line (n=1)
ChEMBL 533 5 2 4 3.8 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1016/S0960-894X(96)00613-0
11556194 195882 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 598 8 3 7 5.4 C[C@H](c1ccc(Cl)c(Cl)c1)[C@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
CHEMBL570297 195882 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 598 8 3 7 5.4 C[C@H](c1ccc(Cl)c(Cl)c1)[C@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
9832467 143761 0 None -602 5 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 477 7 3 4 5.9 O=C(O)c1cccc(NC(=O)c2nc(C3CCCCC3)[nH]c2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm070880t
CHEMBL390519 143761 0 None -602 5 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 477 7 3 4 5.9 O=C(O)c1cccc(NC(=O)c2nc(C3CCCCC3)[nH]c2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm070880t
11555110 11861 0 None -5 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 500 7 5 4 5.7 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4[nH]ccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1182962 11861 0 None -5 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 500 7 5 4 5.7 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4[nH]ccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067954 11861 0 None -5 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 500 7 5 4 5.7 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4[nH]ccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
44403999 12178 0 None -12 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 619 10 5 5 5.2 O=C(O)c1cccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm049069y
CHEMBL1184841 12178 0 None -12 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 619 10 5 5 5.2 O=C(O)c1cccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm049069y
CHEMBL2067962 12178 0 None -12 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 619 10 5 5 5.2 O=C(O)c1cccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm049069y
11605951 12180 0 None -25 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 512 8 4 3 6.5 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184851 12180 0 None -25 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 512 8 4 3 6.5 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067961 12180 0 None -25 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 512 8 4 3 6.5 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
73356071 88956 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL2369818 88956 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL382349 210555 0 None -3235 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
56663145 63813 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 541 8 2 5 3.9 Cc1cccc(Cl)c1NC(=O)NC1C(=O)N(CCC(C)C)c2ccccc2N(CCN2CCOCC2)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808407 63813 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 541 8 2 5 3.9 Cc1cccc(Cl)c1NC(=O)NC1C(=O)N(CCC(C)C)c2ccccc2N(CCN2CCOCC2)C1=O 10.1016/j.bmc.2011.05.057
19700618 63814 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 523 9 2 6 2.9 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)cc1 10.1016/j.bmc.2011.05.057
CHEMBL1808408 63814 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 523 9 2 6 2.9 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)cc1 10.1016/j.bmc.2011.05.057
118719287 114985 0 None -6 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 727 17 4 7 4.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cccc2ccccc12)N(C)C)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
CHEMBL3351059 114985 0 None -6 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 727 17 4 7 4.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cccc2ccccc12)N(C)C)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
CHEMBL3142842 209389 0 None -2 2 Guinea pig 5.3 pKi = 5.3 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CC(C)(C)OC(=O)NCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
53465844 69068 0 None 131 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SR-27897 from human CCK1 R336A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 R336A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SR-27897 from human CCK1 R336A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 R336A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
11518283 165607 0 None -74 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 461 7 3 3 6.2 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL426290 165607 0 None -74 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 461 7 3 3 6.2 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
10482868 106920 0 None -37 5 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 557 10 3 4 5.2 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL317999 106920 0 None -37 5 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 557 10 3 4 5.2 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
11613212 71757 0 None -39 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 513 7 3 4 6.4 Cc1cc(C)c(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(COC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
CHEMBL197780 71757 0 None -39 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 513 7 3 4 6.4 Cc1cc(C)c(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(COC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
56666597 63812 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 585 8 2 5 4.0 Cc1cc(Br)ccc1NC(=O)NC1C(=O)N(CCC(C)C)c2ccccc2N(CCN2CCOCC2)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808405 63812 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 585 8 2 5 4.0 Cc1cc(Br)ccc1NC(=O)NC1C(=O)N(CCC(C)C)c2ccccc2N(CCN2CCOCC2)C1=O 10.1016/j.bmc.2011.05.057
118719284 114983 0 None -72 2 Guinea pig 5.3 pKi = 5.3 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 739 15 5 7 4.9 CN(C)[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C)C1CCCCC1 10.1021/jm00053a022
CHEMBL3351056 114983 0 None -72 2 Guinea pig 5.3 pKi = 5.3 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 739 15 5 7 4.9 CN(C)[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C)C1CCCCC1 10.1021/jm00053a022
16733185 141560 0 None -346 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 594 8 2 5 6.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3cccc(C(=O)O)c3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL388143 141560 0 None -346 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 594 8 2 5 6.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3cccc(C(=O)O)c3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
16732164 142771 0 None -1862 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 571 8 2 6 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3ccn(CC(=O)O)c3c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL389711 142771 0 None -1862 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 571 8 2 6 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3ccn(CC(=O)O)c3c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
10623068 112343 0 None -89 2 Rat 6.3 pKi = 6.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 442 6 2 3 4.7 CCCCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL330854 112343 0 None -89 2 Rat 6.3 pKi = 6.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 442 6 2 3 4.7 CCCCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL1172246 206839 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc2ccccc2)C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC1=O 10.1016/j.bmcl.2010.05.078
44408483 168363 0 None -165 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.7 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL438739 168363 0 None -165 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.7 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
11511706 71917 0 None -12 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 501 7 3 3 6.6 Cc1ccccc1-c1nc(C(=O)Nc2ccc(F)c(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL198225 71917 0 None -12 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 501 7 3 3 6.6 Cc1ccccc1-c1nc(C(=O)Nc2ccc(F)c(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
11571142 135283 0 None -346 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 489 7 3 3 6.7 CC1(c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)CCCCC1 10.1021/jm0490686
CHEMBL373050 135283 0 None -346 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 489 7 3 3 6.7 CC1(c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)CCCCC1 10.1021/jm0490686
9832467 143761 0 None -602 5 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 477 7 3 4 5.9 O=C(O)c1cccc(NC(=O)c2nc(C3CCCCC3)[nH]c2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL390519 143761 0 None -602 5 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 477 7 3 4 5.9 O=C(O)c1cccc(NC(=O)c2nc(C3CCCCC3)[nH]c2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
10256780 112182 0 None -234 2 Rat 6.3 pKi = 6.3 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 540 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00544-6
CHEMBL330409 112182 0 None -234 2 Rat 6.3 pKi = 6.3 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 540 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00544-6
CHEMBL262172 208783 0 None -26302 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
10626665 10164 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm9703247
CHEMBL116127 10164 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm9703247
11540160 71104 0 None -117 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 475 7 3 3 6.6 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL196133 71104 0 None -117 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 475 7 3 3 6.6 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
16732443 85072 0 None -1202 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 532 7 2 5 5.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL227147 85072 0 None -1202 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 532 7 2 5 5.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCCC2)c2ccccc21 10.1021/jm070139l
135610887 85017 0 None -2951 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 558 7 2 7 4.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL226583 85017 0 None -2951 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 558 7 2 7 4.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
11656338 75592 0 None -389 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 504 7 2 5 5.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CO)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
CHEMBL205198 75592 0 None -389 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 504 7 2 5 5.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CO)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
10071178 74146 1 None 501 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL202861 74146 1 None 501 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10367509 106956 0 None -14 2 Guinea pig 5.2 pKi = 5.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 471 6 3 3 5.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)Nc1ccccc1 10.1021/jm00072a005
CHEMBL318238 106956 0 None -14 2 Guinea pig 5.2 pKi = 5.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 471 6 3 3 5.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)Nc1ccccc1 10.1021/jm00072a005
44331505 4287 0 None -25 2 Rat 7.2 pKi = 7.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 450 8 2 3 4.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL101063 4287 0 None -25 2 Rat 7.2 pKi = 7.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 450 8 2 3 4.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
10794691 116561 0 None 1 2 Guinea pig 6.2 pKi = 6.2 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 684 10 5 4 5.3 O=C(O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
CHEMBL339177 116561 0 None 1 2 Guinea pig 6.2 pKi = 6.2 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 684 10 5 4 5.3 O=C(O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
11679213 133020 0 None -61 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 7 3 3 6.8 Cc1ccc(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
CHEMBL370882 133020 0 None -61 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 7 3 3 6.8 Cc1ccc(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
44451522 157769 0 None -26 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 531 6 1 4 5.1 Cc1cccc(NC(=O)CN2C(=O)N(CC(=O)N3CCCC3)c3ccccc3N(C3CCCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
CHEMBL408915 157769 0 None -26 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 531 6 1 4 5.1 Cc1cccc(NC(=O)CN2C(=O)N(CC(=O)N3CCCC3)c3ccccc3N(C3CCCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
CHEMBL1206334 206864 0 None -1023 2 Guinea pig 7.2 pKi = 7.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80678-2
CHEMBL262894 206864 0 None -1023 2 Guinea pig 7.2 pKi = 7.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80678-2
11541048 195300 0 None 7 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 C[C@H](CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
CHEMBL566604 195300 0 None 7 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 C[C@H](CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
44444934 154407 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 749 16 6 7 4.8 COc1ccc(CCNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)cc1 10.1021/jm070880t
CHEMBL401098 154407 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 749 16 6 7 4.8 COc1ccc(CCNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)cc1 10.1021/jm070880t
11801315 114276 0 None -50 2 Rat 7.2 pKi = 7.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 577 6 2 4 6.0 CN(C)c1cccc(NC(=O)NC2C(=O)N(CC3[C@H]4C[C@@H]5C[C@@H](C[C@H]3C5)C4)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL333930 114276 0 None -50 2 Rat 7.2 pKi = 7.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 577 6 2 4 6.0 CN(C)c1cccc(NC(=O)NC2C(=O)N(CC3[C@H]4C[C@@H]5C[C@@H](C[C@H]3C5)C4)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
108187 913 30 None -4265 5 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm070880t
873 913 30 None -4265 5 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm070880t
CHEMBL2062154 913 30 None -4265 5 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm070880t
CHEMBL287735 913 30 None -4265 5 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm070880t
10698427 14385 0 None -645 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 578 6 3 4 5.8 O=C(Nc1cccc(C(=O)O)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL120363 14385 0 None -645 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 578 6 3 4 5.8 O=C(Nc1cccc(C(=O)O)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
10555899 112874 0 None -2344 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 623 8 5 6 5.2 CC(O)C(O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL331763 112874 0 None -2344 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 623 8 5 6 5.2 CC(O)C(O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL3351062 209797 0 None -173 2 Guinea pig 5.2 pKi = 5.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
11535277 12173 0 None -10 2 Guinea pig 5.2 pKi = 5.2 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 513 8 4 4 5.9 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184817 12173 0 None -10 2 Guinea pig 5.2 pKi = 5.2 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 513 8 4 4 5.9 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067964 12173 0 None -10 2 Guinea pig 5.2 pKi = 5.2 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 513 8 4 4 5.9 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
10457639 107226 0 None - 1 Guinea pig 5.2 pKi = 5.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 474 8 4 2 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc(Cl)cc1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL319096 107226 0 None - 1 Guinea pig 5.2 pKi = 5.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 474 8 4 2 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc(Cl)cc1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
16732911 142684 0 None -999 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 564 9 2 6 5.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL389639 142684 0 None -999 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 564 9 2 6 5.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
16732017 85042 0 None -6025 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 561 9 2 6 5.0 CN(CC(=O)O)c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm070139l
CHEMBL226726 85042 0 None -6025 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 561 9 2 6 5.0 CN(CC(=O)O)c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm070139l
16732020 85085 0 None -3311 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 571 8 2 8 4.7 CN(c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1)c1nn[nH]n1 10.1021/jm070139l
CHEMBL227254 85085 0 None -3311 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 571 8 2 8 4.7 CN(c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1)c1nn[nH]n1 10.1021/jm070139l
CHEMBL383458 210566 0 None -10 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
44331468 4222 0 None -16 2 Rat 7.2 pKi = 7.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 470 7 2 3 4.8 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(Cc2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL100685 4222 0 None -16 2 Rat 7.2 pKi = 7.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 470 7 2 3 4.8 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(Cc2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL2370441 208106 0 None -2 2 Guinea pig 6.2 pKi = 6.2 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
11542079 71378 0 None -11 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 483 7 3 3 6.5 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL196580 71378 0 None -11 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 483 7 3 3 6.5 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
11685703 71576 0 None -25 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 391 7 3 3 4.9 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC(C)C)[nH]1 10.1021/jm0490686
CHEMBL197205 71576 0 None -25 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 391 7 3 3 4.9 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC(C)C)[nH]1 10.1021/jm0490686
16733307 168257 0 None -1819 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 585 8 2 7 5.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(C(=O)O)co3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL437736 168257 0 None -1819 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 585 8 2 7 5.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(C(=O)O)co3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
10697783 117130 0 None -141 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 543 7 2 4 5.7 CN(C)c1ccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)cc1 10.1021/jm990967h
CHEMBL340107 117130 0 None -141 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 543 7 2 4 5.7 CN(C)c1ccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)cc1 10.1021/jm990967h
56673429 63600 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 537 9 2 6 3.3 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)c(C)c1 10.1016/j.bmc.2011.05.057
CHEMBL1806517 63600 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 537 9 2 6 3.3 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)c(C)c1 10.1016/j.bmc.2011.05.057
19700612 63806 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 493 8 2 5 2.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808398 63806 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 493 8 2 5 2.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
16732594 14252 0 None -2511 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc3c2cnn3CC(=O)O)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL1161950 14252 0 None -2511 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc3c2cnn3CC(=O)O)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL1200187 14252 0 None -2511 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc3c2cnn3CC(=O)O)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44303372 200990 0 None - 1 Mouse 8.2 pKi = 8.2 Binding
Binding affinity in Cholecystokinin type A receptor binding assay (iv) in miceBinding affinity in Cholecystokinin type A receptor binding assay (iv) in mice
ChEMBL 317 7 2 3 2.0 CCCCNC(=O)[C@@H]1Cc2ccccc2N1C(=O)CC(N)CC 10.1021/jm980521l
CHEMBL61498 200990 0 None - 1 Mouse 8.2 pKi = 8.2 Binding
Binding affinity in Cholecystokinin type A receptor binding assay (iv) in miceBinding affinity in Cholecystokinin type A receptor binding assay (iv) in mice
ChEMBL 317 7 2 3 2.0 CCCCNC(=O)[C@@H]1Cc2ccccc2N1C(=O)CC(N)CC 10.1021/jm980521l
10768190 112333 0 None -15 2 Rat 8.1 pKi = 8.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 516 6 2 4 6.0 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL330773 112333 0 None -15 2 Rat 8.1 pKi = 8.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 516 6 2 4 6.0 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
53465844 69068 0 None 131 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SR-27897 from human CCK1 M195A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 M195A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69068 0 None 131 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SR-27897 from human CCK1 M195A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 M195A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10460632 206589 0 None 43 2 Guinea pig 7.2 pKi = 7.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 568 10 2 4 5.8 CC(Cc1ccc2ccccc2c1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99252 206589 0 None 43 2 Guinea pig 7.2 pKi = 7.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 568 10 2 4 5.8 CC(Cc1ccc2ccccc2c1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
10696354 112991 0 None -74 2 Rat 7.2 pKi = 7.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 488 5 2 3 5.5 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
CHEMBL331971 112991 0 None -74 2 Rat 7.2 pKi = 7.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 488 5 2 3 5.5 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
16100410 141266 0 None -6309 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL386212 141266 0 None -6309 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
9850043 112064 1 None -309 2 Rat 6.2 pKi = 6.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O 10.1016/S0960-894X(96)00544-6
CHEMBL329984 112064 1 None -309 2 Rat 6.2 pKi = 6.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O 10.1016/S0960-894X(96)00544-6
9850043 112375 1 None -446 3 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL330977 112375 1 None -446 3 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44425005 141922 0 None -79 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 478 7 2 5 4.2 CC(C)C1=NN(CC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(CC(=O)C(C)(C)C)c2ccccc21 10.1021/jm070139l
CHEMBL389019 141922 0 None -79 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 478 7 2 5 4.2 CC(C)C1=NN(CC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(CC(=O)C(C)(C)C)c2ccccc21 10.1021/jm070139l
136036821 95364 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 602 9 2 7 5.6 CC(C)(C)C(=O)CN1C(=O)N(CCCC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL258782 95364 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 602 9 2 7 5.6 CC(C)(C)C(=O)CN1C(=O)N(CCCC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
9958214 114295 0 None -269 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
CHEMBL333979 114295 0 None -269 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
11613179 71444 0 None -83 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 511 7 3 3 7.1 Cc1cc(C)c(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
CHEMBL196745 71444 0 None -83 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 511 7 3 3 7.1 Cc1cc(C)c(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
11555166 139300 0 None -54 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 502 7 2 5 5.5 CNc1cccc(NC(=O)C[C@H]2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
CHEMBL379902 139300 0 None -54 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 502 7 2 5 5.5 CNc1cccc(NC(=O)C[C@H]2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
44356654 27899 0 None 1 2 Guinea pig 5.1 pKi = 5.1 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 691 9 3 3 7.8 Cc1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1C 10.1021/jm00021a019
CHEMBL137308 27899 0 None 1 2 Guinea pig 5.1 pKi = 5.1 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 691 9 3 3 7.8 Cc1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1C 10.1021/jm00021a019
10555899 112874 0 None -2344 2 Rat 5.1 pKi = 5.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 623 8 5 6 5.2 CC(O)C(O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL331763 112874 0 None -2344 2 Rat 5.1 pKi = 5.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 623 8 5 6 5.2 CC(O)C(O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
9986662 101558 6 None -977 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 643 11 6 6 4.8 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL301777 101558 6 None -977 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 643 11 6 6 4.8 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm9508907
44346825 114275 0 None -77 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
CHEMBL333920 114275 0 None -77 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
11802426 99819 0 None -50 2 Guinea pig 6.1 pKi = 6.1 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 653 8 3 5 6.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1C[C@H](Oc2ccc(Cl)cc2Cl)C[C@@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
CHEMBL289021 99819 0 None -50 2 Guinea pig 6.1 pKi = 6.1 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 653 8 3 5 6.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1C[C@H](Oc2ccc(Cl)cc2Cl)C[C@@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
10255015 206562 0 None 4 2 Guinea pig 6.1 pKi = 6.1 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 490 8 4 2 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc2ccccc2c1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL99065 206562 0 None 4 2 Guinea pig 6.1 pKi = 6.1 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 490 8 4 2 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc2ccccc2c1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
44346176 112835 0 None -21 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 496 6 3 3 6.2 CC(CC1CCCC1)c1cccc2c1NC(=O)C(NC(=O)Nc1ccccc1)C(=O)N2c1ccccc1 10.1021/jm990967h
CHEMBL331651 112835 0 None -21 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 496 6 3 3 6.2 CC(CC1CCCC1)c1cccc2c1NC(=O)C(NC(=O)Nc1ccccc1)C(=O)N2c1ccccc1 10.1021/jm990967h
11498528 72131 0 None -1096 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 503 7 3 4 6.1 O=C(O)c1cccc(NC(=O)c2[nH]c(C34CCC(CC3)CC4)nc2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL198933 72131 0 None -1096 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 503 7 3 4 6.1 O=C(O)c1cccc(NC(=O)c2[nH]c(C34CCC(CC3)CC4)nc2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL384035 210569 1 None -8 4 Guinea pig 7.1 pKi = 7.1 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80678-2
CHEMBL428666 210569 1 None -8 4 Guinea pig 7.1 pKi = 7.1 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80678-2
9914672 108055 0 None -31 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 521 5 2 4 3.7 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCC2)C1=O 10.1016/j.bmc.2007.12.047
CHEMBL320141 108055 0 None -31 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 521 5 2 4 3.7 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCC2)C1=O 10.1016/j.bmc.2007.12.047
11534407 195260 0 None 6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 584 8 3 7 4.9 O=C(N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL566359 195260 0 None 6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 584 8 3 7 4.9 O=C(N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
11627917 195853 0 None 7 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 CC(CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
CHEMBL570163 195853 0 None 7 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 CC(CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
45487003 195913 0 None 100 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 540 7 2 6 5.4 O=C(NCCc1ccc(Cl)c(Cl)c1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL570521 195913 0 None 100 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 540 7 2 6 5.4 O=C(NCCc1ccc(Cl)c(Cl)c1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
11584582 197190 0 None 19 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 C[C@@H](CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
CHEMBL584063 197190 0 None 19 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 C[C@@H](CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
9914672 108055 0 None -31 2 Human 7.1 pKi = 7.1 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 521 5 2 4 3.7 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00613-0
CHEMBL320141 108055 0 None -31 2 Human 7.1 pKi = 7.1 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 521 5 2 4 3.7 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00613-0
44329156 205900 0 None -50 2 Human 7.1 pKi = 7.1 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 535 5 2 4 4.0 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCCC2)C1=O 10.1016/S0960-894X(96)00613-0
CHEMBL95200 205900 0 None -50 2 Human 7.1 pKi = 7.1 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 535 5 2 4 4.0 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCCC2)C1=O 10.1016/S0960-894X(96)00613-0
11505870 72162 0 None -2 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 526 8 3 4 6.6 Cc1ccccc1-c1nc(CCC23CC4CC(CC(C4)C2)C3)c(C(=O)Nc2ccc(N(C)C)c(C(=O)O)c2)[nH]1 10.1021/jm0490686
CHEMBL199032 72162 0 None -2 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 526 8 3 4 6.6 Cc1ccccc1-c1nc(CCC23CC4CC(CC(C4)C2)C3)c(C(=O)Nc2ccc(N(C)C)c(C(=O)O)c2)[nH]1 10.1021/jm0490686
10652143 94163 0 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 679 11 5 6 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3sccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL252150 94163 0 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 679 11 5 6 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3sccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
11802624 101566 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL2067966 101566 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL301810 101566 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
44331479 4306 0 None -27 2 Rat 6.1 pKi = 6.1 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 494 9 1 5 4.7 CC(C)CCN1C(=O)C(NC(=O)Oc2cccc(N(C)C)c2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL101208 4306 0 None -27 2 Rat 6.1 pKi = 6.1 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 494 9 1 5 4.7 CC(C)CCN1C(=O)C(NC(=O)Oc2cccc(N(C)C)c2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
11802624 101566 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067966 101566 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL301810 101566 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
10555325 12840 0 None -45 2 Guinea pig 5.1 pKi = 5.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 585 7 2 5 4.2 CC(=O)N1[C@H](C(=O)NCC(=O)O)CC(=O)c2ccccc2N(Cc2ccccc2)C(=O)[C@H]1CC12CC3CC(CC(C3)C1)C2 10.1021/jm070880t
CHEMBL118930 12840 0 None -45 2 Guinea pig 5.1 pKi = 5.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 585 7 2 5 4.2 CC(=O)N1[C@H](C(=O)NCC(=O)O)CC(=O)c2ccccc2N(Cc2ccccc2)C(=O)[C@H]1CC12CC3CC(CC(C3)C1)C2 10.1021/jm070880t
44272229 98291 0 None - 1 Guinea pig 5.1 pKi = 5.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 635 15 6 6 3.5 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NCCc1ccccc1 10.1021/jm070880t
CHEMBL278032 98291 0 None - 1 Guinea pig 5.1 pKi = 5.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 635 15 6 6 3.5 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NCCc1ccccc1 10.1021/jm070880t
16090701 141222 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 383 4 2 3 3.6 O=C(c1ccccc1NS(=O)(=O)c1cc2ccccc2[nH]1)N1CCCCC1 10.1021/jm060590x
CHEMBL385963 141222 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 383 4 2 3 3.6 O=C(c1ccccc1NS(=O)(=O)c1cc2ccccc2[nH]1)N1CCCCC1 10.1021/jm060590x
16732755 85025 0 None -10000 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 544 8 2 5 5.7 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C2CCCCC2)C1=O)Nc1cccc(C(=O)O)c1 10.1021/jm070139l
CHEMBL226622 85025 0 None -10000 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 544 8 2 5 5.7 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C2CCCCC2)C1=O)Nc1cccc(C(=O)O)c1 10.1021/jm070139l
11518254 11696 0 None -31 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 460 7 4 3 5.8 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1181918 11696 0 None -31 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 460 7 4 3 5.8 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067948 11696 0 None -31 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 460 7 4 3 5.8 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
9870515 12155 0 None -63 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 498 7 4 3 6.1 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184696 12155 0 None -63 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 498 7 4 3 6.1 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067955 12155 0 None -63 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 498 7 4 3 6.1 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
11554414 12174 0 None -7 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 461 7 4 4 5.2 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184820 12174 0 None -7 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 461 7 4 4 5.2 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067965 12174 0 None -7 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 461 7 4 4 5.2 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL320868 209483 0 None 70 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL3351060 209795 0 None 20 2 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CN(C(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)c1ccccc1)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
4627 809 44 None -1 5 Rat 8.1 pKi = 8.1 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None None 10.1021/jm00389a002
864 809 44 None -1 5 Rat 8.1 pKi = 8.1 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None None 10.1021/jm00389a002
9833444 809 44 None -1 5 Rat 8.1 pKi = 8.1 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None None 10.1021/jm00389a002
CHEMBL1121 809 44 None -1 5 Rat 8.1 pKi = 8.1 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None None 10.1021/jm00389a002
DB09142 809 44 None -1 5 Rat 8.1 pKi = 8.1 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None None 10.1021/jm00389a002
10027864 106798 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccc(F)cc21 10.1016/0960-894X(95)00528-2
CHEMBL317081 106798 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccc(F)cc21 10.1016/0960-894X(95)00528-2
44265928 205544 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 342 5 2 1 5.2 Cc1cccc(NC(=O)NCC=C(c2ccccc2)c2ccccc2)c1 10.1021/jm00084a009
CHEMBL9312 205544 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 342 5 2 1 5.2 Cc1cccc(NC(=O)NCC=C(c2ccccc2)c2ccccc2)c1 10.1021/jm00084a009
CHEMBL3351049 209787 0 None -2 2 Guinea pig 5.1 pKi = 5.1 Binding
Affinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membraneAffinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membrane
ChEMBL None None None CN(C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)[C@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
10651325 13765 0 None -275 2 Rat 6.1 pKi = 6.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 606 7 2 5 6.3 CCOC(=O)c1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL119608 13765 0 None -275 2 Rat 6.1 pKi = 6.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 606 7 2 5 6.3 CCOC(=O)c1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
16732592 143050 0 None -870 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3c(cnn3CC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL389933 143050 0 None -870 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3c(cnn3CC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44296980 101552 0 None -9 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 538 5 2 3 4.9 O=C(NCC12CC3CC(CC(C3)C1)C2)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm9508907
CHEMBL301740 101552 0 None -9 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 538 5 2 3 4.9 O=C(NCC12CC3CC(CC(C3)C1)C2)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm9508907
44346952 113614 0 None -9 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 538 5 2 3 4.8 O=C(NCC1C2CC3CC(C2)CC1C3)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm00048a001
CHEMBL332782 113614 0 None -9 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 538 5 2 3 4.8 O=C(NCC1C2CC3CC(C2)CC1C3)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm00048a001
10674395 110284 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm9703247
CHEMBL326064 110284 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm9703247
44331489 4210 0 None -32 2 Rat 7.1 pKi = 7.1 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 493 9 2 4 4.7 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL100618 4210 0 None -32 2 Rat 7.1 pKi = 7.1 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 493 9 2 4 4.7 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
10768658 114304 0 None -42 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.0 O=C(Nc1ccccc1)NC1C(=O)N(CC2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL334020 114304 0 None -42 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.0 O=C(Nc1ccccc1)NC1C(=O)N(CC2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
16100408 141259 0 None -1202 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL386186 141259 0 None -1202 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
19700621 63815 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 509 8 3 6 2.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(O)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808409 63815 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 509 8 3 6 2.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(O)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
15249830 101465 0 None -15 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 441 4 2 2 4.9 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm9508907
CHEMBL301095 101465 0 None -15 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 441 4 2 2 4.9 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm9508907
44347142 113632 0 None -15 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 441 4 2 2 4.8 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL332873 113632 0 None -15 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 441 4 2 2 4.8 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
44408632 157692 0 None -3630 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL408832 157692 0 None -3630 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
11802624 101566 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL2067966 101566 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL301810 101566 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
16733463 13889 0 None -1380 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 547 9 3 6 5.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(NCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL1197033 13889 0 None -1380 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 547 9 3 6 5.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(NCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL559157 13889 0 None -1380 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 547 9 3 6 5.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(NCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44346947 15126 0 None 1 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 389 4 2 2 4.3 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1CCCCC1 10.1021/jm00048a001
CHEMBL121342 15126 0 None 1 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 389 4 2 2 4.3 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1CCCCC1 10.1021/jm00048a001
CHEMBL336381 209837 0 None -354 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm0303103
11584903 140208 0 None -295 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell line
ChEMBL 560 10 2 6 5.1 CNCCN(C)c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
CHEMBL381805 140208 0 None -295 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell line
ChEMBL 560 10 2 6 5.1 CNCCN(C)c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
10604847 193011 0 None -218 2 Guinea pig 6.1 pKi = 6.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 711 11 6 10 3.8 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
CHEMBL53237 193011 0 None -218 2 Guinea pig 6.1 pKi = 6.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 711 11 6 10 3.8 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
CHEMBL1172252 206842 0 None -12 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
CHEMBL208479 207455 0 None -3 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
19043361 4551 0 None 162 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 524 6 2 3 6.2 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(Cl)c(Cl)cc21 10.1016/0960-894X(95)00528-2
CHEMBL102867 4551 0 None 162 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 524 6 2 3 6.2 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(Cl)c(Cl)cc21 10.1016/0960-894X(95)00528-2
44265973 205539 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 362 5 2 1 5.6 O=C(NCC=C(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
CHEMBL9308 205539 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 362 5 2 1 5.6 O=C(NCC=C(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
CHEMBL408083 210951 0 None -2 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
46235271 73301 2 None 2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73301 2 None 2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
10580503 101220 0 None -234 2 Guinea pig 6.0 pKi = 6.0 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 691 11 6 10 3.7 O=C(NCC1CCCCCC1)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1F)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
CHEMBL299387 101220 0 None -234 2 Guinea pig 6.0 pKi = 6.0 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 691 11 6 10 3.7 O=C(NCC1CCCCCC1)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1F)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
44356430 114732 0 None -70 2 Guinea pig 6.0 pKi = 6.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL334714 114732 0 None -70 2 Guinea pig 6.0 pKi = 6.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
21476261 4230 0 None -169 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 571 8 2 4 5.9 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL100776 4230 0 None -169 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 571 8 2 4 5.9 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
44357011 116070 0 None 1 2 Guinea pig 5.0 pKi = 5.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 779 11 3 7 6.8 COC(=O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)OC)c1 10.1021/jm00021a019
CHEMBL336453 116070 0 None 1 2 Guinea pig 5.0 pKi = 5.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 779 11 3 7 6.8 COC(=O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)OC)c1 10.1021/jm00021a019
44212463 63825 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 555 7 2 4 4.9 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808419 63825 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 555 7 2 4 4.9 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL411271 211128 0 None -630 3 Guinea pig 7.0 pKi = 7.0 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0000416
10838957 12366 0 None -151 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 495 5 2 4 5.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL118622 12366 0 None -151 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 495 5 2 4 5.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
44346326 112840 0 None -46 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 588 5 2 7 6.5 O=C(Nc1cccc(C2N=NN=N2)c1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)C1=O 10.1021/jm990967h
CHEMBL331688 112840 0 None -46 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 588 5 2 7 6.5 O=C(Nc1cccc(C2N=NN=N2)c1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)C1=O 10.1021/jm990967h
53465843 69067 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933103 69067 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL382051 210546 0 None -489 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
CHEMBL3351055 209793 0 None -70 2 Guinea pig 6.0 pKi = 6 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)c1ccccc1 10.1021/jm00053a022
2118 201792 35 None - 2 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
Drug Central 308 1 0 4 3.6 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
CHEMBL661 201792 35 None - 2 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
Drug Central 308 1 0 4 3.6 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
5556 201569 26 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
Drug Central 342 1 0 4 4.2 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1Cl)=NC2 None
CHEMBL646 201569 26 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
Drug Central 342 1 0 4 4.2 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1Cl)=NC2 None
11954224 214174 0 None - 59 Mouse 8.4 pIC50 = 8.4 Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
9853654 22588 37 None - 2 Rat 8.2 pIC50 = 8.2 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
Drug Central 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O None
CHEMBL1328 22588 37 None - 2 Rat 8.2 pIC50 = 8.2 Binding
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
Drug Central 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O None
1614 2317 60 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
60182 2317 60 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
892 2317 60 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
CHEMBL206025 2317 60 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
16129670 803 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
860 803 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
91898395 803 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
3476 1373 8 None 2 3 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 3018478
59751 1373 8 None 2 3 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 3018478
878 1373 8 None 2 3 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 3018478
CHEMBL39263 1373 8 None 2 3 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 3018478
4627 809 44 None -1 5 Rat 8.0 pKi = 8 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
Drug Central None None None None None
864 809 44 None -1 5 Rat 8.0 pKi = 8 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
Drug Central None None None None None
9833444 809 44 None -1 5 Rat 8.0 pKi = 8 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
Drug Central None None None None None
CHEMBL1121 809 44 None -1 5 Rat 8.0 pKi = 8 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
Drug Central None None None None None
DB09142 809 44 None -1 5 Rat 8.0 pKi = 8 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
Drug Central None None None None None
138106885 166358 71 None -1 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
Drug Central 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C None
36314 166358 71 None -1 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
Drug Central 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C None
CHEMBL428647 166358 71 None -1 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
Drug Central 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C None
4627 809 44 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
Drug Central None None None None None
864 809 44 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
Drug Central None None None None None
9833444 809 44 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
Drug Central None None None None None
CHEMBL1121 809 44 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
Drug Central None None None None None
DB09142 809 44 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
Drug Central None None None None None
4627 809 44 None -1 5 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
Drug Central None None None None None
864 809 44 None -1 5 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
Drug Central None None None None None
9833444 809 44 None -1 5 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
Drug Central None None None None None
CHEMBL1121 809 44 None -1 5 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
Drug Central None None None None None
DB09142 809 44 None -1 5 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
Drug Central None None None None None
859 469 0 None 7943 2 Rat 10.5 pKi None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476993
3074331 912 0 None - 1 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 493 6 4 4 4.6 O=C(N[C@@](C(=O)N[C@H]1CCCC[C@@H]1O)(Cc1c[nH]c2c1cccc2)C)OC12CC3CC(C2)CC(C1)C3 9438020
872 912 0 None - 1 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 493 6 4 4 4.6 O=C(N[C@@](C(=O)N[C@H]1CCCC[C@@H]1O)(Cc1c[nH]c2c1cccc2)C)OC12CC3CC(C2)CC(C1)C3 9438020
132980 2209 8 None - 1 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 7969084
881 2209 8 None - 1 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 7969084
CHEMBL420783 2209 8 None - 1 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 7969084
6439414 2976 11 None -2454 2 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 7516969
867 2976 11 None -2454 2 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 7516969
CHEMBL3351022 2976 11 None -2454 2 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 7516969
CHEMBL341460 2976 11 None -2454 2 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 7516969
122130 4052 33 None - 1 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 7910212
888 4052 33 None - 1 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 7910212
CHEMBL115121 4052 33 None - 1 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 7910212
65937 1376 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 17684117
834 1376 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 17684117
889 1376 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 17684117
CHEMBL550781 1376 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 17684117
DB04856 1376 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 17684117
11488979 2105 0 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 7 1 4 6.6 COc1ccc(cc1)n1nc(cc1c1ccc(c(c1)Cl)Cl)C[C@@H](c1cccc(c1)C)C(=O)O 17684117
877 2105 0 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 7 1 4 6.6 COc1ccc(cc1)n1nc(cc1c1ccc(c(c1)Cl)Cl)C[C@@H](c1cccc(c1)C)C(=O)O 17684117
CHEMBL400111 2105 0 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 7 1 4 6.6 COc1ccc(cc1)n1nc(cc1c1ccc(c(c1)Cl)Cl)C[C@@H](c1cccc(c1)C)C(=O)O 17684117
885 3787 0 None 1584 2 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 10 3 6 5.1 O=C([C@@H](NC(=O)c1cc2c([nH]1)cccc2)CSc1ncccc1C(=O)O)N1CCN(CC1)C(c1ccccc1)c1ccccc1 8730754
9873836 3787 0 None 1584 2 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 10 3 6 5.1 O=C([C@@H](NC(=O)c1cc2c([nH]1)cccc2)CSc1ncccc1C(=O)O)N1CCN(CC1)C(c1ccccc1)c1ccccc1 8730754