Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
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
1499 2060 43 None -63 36 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
3779 2060 43 None -63 36 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
536 2060 43 None -63 36 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
CHEMBL434 2060 43 None -63 36 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
DB01064 2060 43 None -63 36 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
1499 2060 43 None -63 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2060 43 None -63 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2060 43 None -63 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2060 43 None -63 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2060 43 None -63 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
2367 950 83 None -1148 5 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 6 2.9 COc1c(OC)cc2c(c1OC)c1ccc(c(=O)cc1[C@H](CC2)NC(=O)C)OC 20022913
6167 950 83 None -1148 5 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 6 2.9 COc1c(OC)cc2c(c1OC)c1ccc(c(=O)cc1[C@H](CC2)NC(=O)C)OC 20022913
726 950 83 None -1148 5 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 6 2.9 COc1c(OC)cc2c(c1OC)c1ccc(c(=O)cc1[C@H](CC2)NC(=O)C)OC 20022913
CHEMBL107 950 83 None -1148 5 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 6 2.9 COc1c(OC)cc2c(c1OC)c1ccc(c(=O)cc1[C@H](CC2)NC(=O)C)OC 20022913
DB01394 950 83 None -1148 5 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 6 2.9 COc1c(OC)cc2c(c1OC)c1ccc(c(=O)cc1[C@H](CC2)NC(=O)C)OC 20022913
12423 3636 0 None - 1 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 804 9 11 18 -2.9 C[C@@]12CCC[C@@]([C@H]1CC[C@]34[C@H]2CC[C@](C3)(C(=C)C4)O[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O)(C)C(=O)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O)O)O 22616809
442089 3636 0 None - 1 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 804 9 11 18 -2.9 C[C@@]12CCC[C@@]([C@H]1CC[C@]34[C@H]2CC[C@](C3)(C(=C)C4)O[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O)(C)C(=O)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O)O)O 22616809
CHEMBL444122 3636 0 None - 1 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 804 9 11 18 -2.9 C[C@@]12CCC[C@@]([C@H]1CC[C@]34[C@H]2CC[C@](C3)(C(=C)C4)O[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O)(C)C(=O)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O)O)O 22616809
138107041 555 63 None -562 3 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 749 7 5 14 1.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@@H]2O[C@@H](C)[C@@H]([C@](C2)(C)OC)O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@](C[C@H](CN([C@@H]([C@H]([C@]1(C)O)O)C)C)C)(C)O 30011231
276 555 63 None -562 3 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 749 7 5 14 1.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@@H]2O[C@@H](C)[C@@H]([C@](C2)(C)OC)O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@](C[C@H](CN([C@@H]([C@H]([C@]1(C)O)O)C)C)C)(C)O 30011231
447043 555 63 None -562 3 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 749 7 5 14 1.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@@H]2O[C@@H](C)[C@@H]([C@](C2)(C)OC)O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@](C[C@H](CN([C@@H]([C@H]([C@]1(C)O)O)C)C)C)(C)O 30011231
6510 555 63 None -562 3 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 749 7 5 14 1.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@@H]2O[C@@H](C)[C@@H]([C@](C2)(C)OC)O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@](C[C@H](CN([C@@H]([C@H]([C@]1(C)O)O)C)C)C)(C)O 30011231
CHEMBL529 555 63 None -562 3 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 749 7 5 14 1.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@@H]2O[C@@H](C)[C@@H]([C@](C2)(C)OC)O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@](C[C@H](CN([C@@H]([C@H]([C@]1(C)O)O)C)C)C)(C)O 30011231
DB00207 555 63 None -562 3 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 749 7 5 14 1.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@@H]2O[C@@H](C)[C@@H]([C@](C2)(C)OC)O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@](C[C@H](CN([C@@H]([C@H]([C@]1(C)O)O)C)C)C)(C)O 30011231
12424 2340 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 23214402
44398561 2340 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 23214402
CHEMBL434535 2340 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 23214402
10362 225 65 None -1096 2 Human 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 3 2 3 2.3 OC(=O)/C=C(\C=C\C1(O)C(=CC(=O)CC1(C)C)C)/C 25844797
5375199 225 65 None -1096 2 Human 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 3 2 3 2.3 OC(=O)/C=C(\C=C\C1(O)C(=CC(=O)CC1(C)C)C)/C 25844797
CHEMBL379808 225 65 None -1096 2 Human 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 3 2 3 2.3 OC(=O)/C=C(\C=C\C1(O)C(=CC(=O)CC1(C)C)C)/C 25844797




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