Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
90656213 110903 0 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 635 13 7 13 -0.3 O=c1[nH]/c(=N\OCCCc2cccc(F)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261362 110903 0 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 635 13 7 13 -0.3 O=c1[nH]/c(=N\OCCCc2cccc(F)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
1734 3966 50 None -1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/s0960-894x(00)00612-0
3639 3966 50 None -1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/s0960-894x(00)00612-0
6133 3966 50 None -1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/s0960-894x(00)00612-0
CHEMBL336296 3966 50 None -1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/s0960-894x(00)00612-0
DB04005 3966 50 None -1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/s0960-894x(00)00612-0
1731 130 11 None -10 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm901450d
9872620 130 11 None -10 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm901450d
CHEMBL384527 130 11 None -10 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm901450d
90656214 110904 0 None 5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 635 13 7 13 -0.3 O=c1[nH]/c(=N\OCCCc2ccc(F)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261363 110904 0 None 5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 635 13 7 13 -0.3 O=c1[nH]/c(=N\OCCCc2ccc(F)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
54584406 62920 0 None 4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 509 9 6 12 -1.2 [N-]=[N+]=N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1021/jm101591j
CHEMBL1784888 62920 0 None 4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 509 9 6 12 -1.2 [N-]=[N+]=N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1021/jm101591j
44586045 184148 0 None 1 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 638 14 9 17 -3.0 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OCC(O)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL482895 184148 0 None 1 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 638 14 9 17 -3.0 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OCC(O)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
90656216 110906 0 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 743 13 7 13 0.2 O=c1[nH]/c(=N\OCCCc2cccc(I)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261365 110906 0 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 743 13 7 13 0.2 O=c1[nH]/c(=N\OCCCc2cccc(I)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
46831686 14201 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm100287t
CHEMBL1084612 14201 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm100287t
CHEMBL1198872 14201 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm100287t
CHEMBL4866937 14201 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm100287t
46831686 14201 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL1084612 14201 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL1198872 14201 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL4866937 14201 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
11525909 141605 5 None -19 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 483 8 7 12 -2.5 N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
CHEMBL385098 141605 5 None -19 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 483 8 7 12 -2.5 N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
11525909 141605 5 None -19 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 483 8 7 12 -2.5 N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1021/jm060903o
CHEMBL385098 141605 5 None -19 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 483 8 7 12 -2.5 N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1021/jm060903o
44586007 192595 1 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 498 8 7 12 -2.1 C[C@@]1(O)[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
CHEMBL521487 192595 1 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 498 8 7 12 -2.1 C[C@@]1(O)[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
90656225 110915 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 667 13 7 13 0.8 O=c1[nH]/c(=N\OCCCc2ccc3ccccc3c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261374 110915 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 667 13 7 13 0.8 O=c1[nH]/c(=N\OCCCc2ccc3ccccc3c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
148197 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
1736 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
4900 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
CHEMBL221326 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
DB15919 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
148197 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
1736 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
4900 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
CHEMBL221326 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
DB15919 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
148197 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
1736 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
4900 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
CHEMBL221326 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
DB15919 1438 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
1737 1367 7 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1016/j.bmc.2008.05.013
9875516 1367 7 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1016/j.bmc.2008.05.013
CHEMBL507282 1367 7 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1016/j.bmc.2008.05.013
DB04983 1367 7 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1016/j.bmc.2008.05.013
146015339 3922 32 None -234 7 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
1749 3922 32 None -234 7 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
6031 3922 32 None -234 7 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
CHEMBL130266 3922 32 None -234 7 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
DB03435 3922 32 None -234 7 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
90656215 110905 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 695 13 7 13 0.4 O=c1[nH]/c(=N\OCCCc2ccc(Br)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261364 110905 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 695 13 7 13 0.4 O=c1[nH]/c(=N\OCCCc2ccc(Br)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
52952280 61338 0 None -2 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 434 7 5 11 -1.2 CSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767410 61338 0 None -2 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 434 7 5 11 -1.2 CSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL2029010 209148 0 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL None None None BP(=O)(OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC 10.1021/jm2013198
10174453 90 5 None -17 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060848j
3398 90 5 None -17 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060848j
CHEMBL217803 90 5 None -17 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060848j
44585519 169986 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL444212 169986 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
44585519 169986 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL444212 169986 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
46831384 14199 0 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 447 8 6 11 -2.1 CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1084295 14199 0 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 447 8 6 11 -2.1 CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1198862 14199 0 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 447 8 6 11 -2.1 CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
1713 520 68 None -20 10 Rat 5.8 pEC50 = 5.8 Functional
The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
5957 520 68 None -20 10 Rat 5.8 pEC50 = 5.8 Functional
The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
91 520 68 None -20 10 Rat 5.8 pEC50 = 5.8 Functional
The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
CHEMBL14249 520 68 None -20 10 Rat 5.8 pEC50 = 5.8 Functional
The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
DB00171 520 68 None -20 10 Rat 5.8 pEC50 = 5.8 Functional
The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
53309244 62917 0 None 4 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784885 62917 0 None 4 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
44586044 184298 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 617 13 7 16 -1.4 N#CCCOP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL484105 184298 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 617 13 7 16 -1.4 N#CCCOP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
44586044 184298 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 617 13 7 16 -1.4 N#CCCOP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm101591j
CHEMBL484105 184298 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 617 13 7 16 -1.4 N#CCCOP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm101591j
90656223 110913 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 623 13 7 14 -0.3 O=c1[nH]/c(=N\OCCCc2ccsc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261372 110913 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 623 13 7 14 -0.3 O=c1[nH]/c(=N\OCCCc2ccsc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
90656229 112807 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1400 31 14 27 1.7 N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCNC(=O)COc5ccc(CCCO/N=c6/ccn([C@@H]7O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]7O)c(=O)[nH]6)cc5)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O 10.1021/jm500367e
CHEMBL3261377 112807 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1400 31 14 27 1.7 N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCNC(=O)COc5ccc(CCCO/N=c6/ccn([C@@H]7O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]7O)c(=O)[nH]6)cc5)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O 10.1021/jm500367e
CHEMBL3306844 112807 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1400 31 14 27 1.7 N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCNC(=O)COc5ccc(CCCO/N=c6/ccn([C@@H]7O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]7O)c(=O)[nH]6)cc5)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O 10.1021/jm500367e
44439758 91270 0 None -1995 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 551 8 6 11 0.6 O=c1c2cc(Cl)ccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
CHEMBL240201 91270 0 None -1995 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 551 8 6 11 0.6 O=c1c2cc(Cl)ccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
44585518 188209 0 None -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL499138 188209 0 None -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
44585518 188209 0 None -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL499138 188209 0 None -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
53308826 62922 0 None 3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 527 10 7 13 -2.0 CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784890 62922 0 None 3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 527 10 7 13 -2.0 CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
53308961 62923 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 555 9 7 13 -1.2 CC(C)(C)O/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784891 62923 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 555 9 7 13 -1.2 CC(C)(C)O/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
53309530 62860 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 728 13 10 19 -3.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](F)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784293 62860 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 728 13 10 19 -3.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](F)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
90666793 109425 0 None -53 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 554 10 6 13 -1.0 O=c1[nH]/c(=N\OCc2ccc([N+](=O)[O-])cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL3220050 109425 0 None -53 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 554 10 6 13 -1.0 O=c1[nH]/c(=N\OCc2ccc([N+](=O)[O-])cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
53309381 62929 0 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 740 13 11 20 -4.5 O=C(O)[C@H]1O[C@H](OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O 10.1021/jm101591j
CHEMBL1784902 62929 0 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 740 13 11 20 -4.5 O=C(O)[C@H]1O[C@H](OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O 10.1021/jm101591j
1730 125 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
3033941 125 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
CHEMBL1767409 125 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
90656220 110910 0 None 2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 647 14 7 14 -0.4 COc1ccc(CCCO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)cc1 10.1021/jm500367e
CHEMBL3261369 110910 0 None 2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 647 14 7 14 -0.4 COc1ccc(CCCO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)cc1 10.1021/jm500367e
1730 125 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
3033941 125 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
CHEMBL1767409 125 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
4044 2665 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
53262902 2665 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
CHEMBL1784894 2665 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
16116566 2656 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
1733 2656 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
CHEMBL373780 2656 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
16116566 2656 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
1733 2656 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
CHEMBL373780 2656 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
46831692 14196 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1083764 14196 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1198849 14196 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
46831692 14196 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL1083764 14196 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL1198849 14196 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
90656222 110912 0 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 618 13 7 14 -1.0 O=c1[nH]/c(=N\OCCCc2ccncc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261371 110912 0 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 618 13 7 14 -1.0 O=c1[nH]/c(=N\OCCCc2ccncc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
1734 3966 50 None -1 7 Human 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
3639 3966 50 None -1 7 Human 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
6133 3966 50 None -1 7 Human 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
CHEMBL336296 3966 50 None -1 7 Human 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
DB04005 3966 50 None -1 7 Human 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
44586043 184275 0 None 1 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 562 10 7 14 -1.7 CP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL483913 184275 0 None 1 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 562 10 7 14 -1.7 CP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
53309242 62928 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 685 13 7 17 -0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3cccc([N+](=O)[O-])c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784900 62928 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 685 13 7 17 -0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3cccc([N+](=O)[O-])c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
1734 3966 50 None -3 7 Rat 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
3639 3966 50 None -3 7 Rat 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
6133 3966 50 None -3 7 Rat 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
CHEMBL336296 3966 50 None -3 7 Rat 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
DB04005 3966 50 None -3 7 Rat 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
44586042 191896 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 578 11 7 15 -1.7 COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL519991 191896 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 578 11 7 15 -1.7 COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
44586042 191896 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 578 11 7 15 -1.7 COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm101591j
CHEMBL519991 191896 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 578 11 7 15 -1.7 COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm101591j
44586026 192591 1 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 580 10 8 14 -1.0 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL521451 192591 1 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 580 10 8 14 -1.0 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
44417696 81155 0 None -5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 498 8 6 13 -2.5 Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c1=O 10.1021/jm060848j
CHEMBL215783 81155 0 None -5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 498 8 6 13 -2.5 Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c1=O 10.1021/jm060848j
90656221 110911 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 618 13 7 14 -1.0 O=c1[nH]/c(=N\OCCCc2cccnc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261370 110911 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 618 13 7 14 -1.0 O=c1[nH]/c(=N\OCCCc2cccnc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
46890063 14192 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 494 8 7 11 -2.1 O=c1ccn([C@@]23C[C@H]2[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083148 14192 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 494 8 7 11 -2.1 O=c1ccn([C@@]23C[C@H]2[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1198833 14192 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 494 8 7 11 -2.1 O=c1ccn([C@@]23C[C@H]2[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]1 10.1021/jm100287t
21706 117147 15 None -5 2 Rat 5.5 pEC50 = 5.5 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 836 14 10 25 -2.4 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1021/jm020046y
CHEMBL339385 117147 15 None -5 2 Rat 5.5 pEC50 = 5.5 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 836 14 10 25 -2.4 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1021/jm020046y
53309529 62859 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 757 14 10 20 -3.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](F)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784292 62859 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 757 14 10 20 -3.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](F)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
15485121 14180 0 None -3 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP productionAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP production
ChEMBL 388 6 5 9 -1.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)C[C@H]2O)c(=O)[nH]1 10.1021/jm060485n
CHEMBL1198709 14180 0 None -3 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP productionAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP production
ChEMBL 388 6 5 9 -1.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)C[C@H]2O)c(=O)[nH]1 10.1021/jm060485n
CHEMBL612021 14180 0 None -3 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP productionAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP production
ChEMBL 388 6 5 9 -1.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)C[C@H]2O)c(=O)[nH]1 10.1021/jm060485n
90666802 109430 0 None -3 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 769 18 7 18 -0.8 CC(=O)NCCn1cc(CCOP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cc/c(=N/OCc4ccccc4)[nH]c3=O)[C@H](O)[C@@H]2O)nn1 10.1039/c3md00132f
CHEMBL3220058 109430 0 None -3 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 769 18 7 18 -0.8 CC(=O)NCCn1cc(CCOP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cc/c(=N/OCc4ccccc4)[nH]c3=O)[C@H](O)[C@@H]2O)nn1 10.1039/c3md00132f
1731 130 11 None -10 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm060848j
9872620 130 11 None -10 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm060848j
CHEMBL384527 130 11 None -10 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm060848j
10174453 90 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
3398 90 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
CHEMBL217803 90 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
10174453 90 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
3398 90 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
CHEMBL217803 90 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
10174453 90 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm101591j
3398 90 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm101591j
CHEMBL217803 90 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm101591j
10432343 199379 4 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assay
ChEMBL 422 6 6 10 -2.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/jm901450d
CHEMBL590981 199379 4 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assay
ChEMBL 422 6 6 10 -2.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/jm901450d
90666790 109422 0 None -18 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 635 9 6 11 -0.3 O=c1[nH]/c(=N\OCc2cccc(I)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL3220047 109422 0 None -18 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 635 9 6 11 -0.3 O=c1[nH]/c(=N\OCc2cccc(I)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
44439757 154452 0 None -707 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 535 8 6 11 0.1 O=c1c2cc(F)ccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
CHEMBL399017 154452 0 None -707 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 535 8 6 11 0.1 O=c1c2cc(F)ccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
44585987 191802 0 None 2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1021/jm1016297
CHEMBL519835 191802 0 None 2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1021/jm1016297
1734 3966 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.09.017
1734 3966 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.10.038
3639 3966 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.09.017
3639 3966 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.10.038
6133 3966 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.09.017
6133 3966 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.10.038
CHEMBL336296 3966 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.09.017
CHEMBL336296 3966 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.10.038
DB04005 3966 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.09.017
DB04005 3966 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.10.038
451388 84231 6 None -27 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 498 8 7 12 -2.2 Cc1cn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]c1=O 10.1021/jm060903o
CHEMBL220940 84231 6 None -27 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 498 8 7 12 -2.2 Cc1cn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]c1=O 10.1021/jm060903o
52952604 61085 0 None -3 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 636 11 6 13 -0.4 O=C(Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)c1=O)c1ccccc1 10.1021/jm1016297
CHEMBL1765118 61085 0 None -3 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 636 11 6 13 -0.4 O=C(Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)c1=O)c1ccccc1 10.1021/jm1016297
11993891 82436 0 None -33 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 628 8 7 11 -0.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br 10.1021/jm060848j
CHEMBL217467 82436 0 None -33 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 628 8 7 11 -0.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br 10.1021/jm060848j
90656227 110917 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 742 18 8 15 -0.9 C#CCCNC(=O)COc1ccc(CCCO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)cc1 10.1021/jm500367e
CHEMBL3261376 110917 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 742 18 8 15 -0.9 C#CCCNC(=O)COc1ccc(CCCO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)cc1 10.1021/jm500367e
148197 1438 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
1736 1438 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
4900 1438 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
CHEMBL221326 1438 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
DB15919 1438 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
44457427 14857 0 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1016/s0960-894x(00)00612-0
CHEMBL1207447 14857 0 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1016/s0960-894x(00)00612-0
CHEMBL406266 14857 0 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1016/s0960-894x(00)00612-0
90656224 110914 0 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 565 12 7 13 -1.6 C#CCCCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
CHEMBL3261373 110914 0 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 565 12 7 13 -1.6 C#CCCCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
10303040 91968 0 None -190 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 507 8 6 11 0.8 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3ccccc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
CHEMBL241481 91968 0 None -190 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 507 8 6 11 0.8 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3ccccc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
10191162 147417 0 None -602 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 559 8 6 11 1.6 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3c(F)cc(Cl)cc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
CHEMBL392989 147417 0 None -602 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 559 8 6 11 1.6 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3c(F)cc(Cl)cc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
90656212 110902 0 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 619 13 7 14 -1.0 O=c1[nH]/c(=N\OCCOc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261361 110902 0 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 619 13 7 14 -1.0 O=c1[nH]/c(=N\OCCOc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
1713 520 68 None -630 10 Human 4.4 pEC50 = 4.4 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
5957 520 68 None -630 10 Human 4.4 pEC50 = 4.4 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
91 520 68 None -630 10 Human 4.4 pEC50 = 4.4 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
CHEMBL14249 520 68 None -630 10 Human 4.4 pEC50 = 4.4 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
DB00171 520 68 None -630 10 Human 4.4 pEC50 = 4.4 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
44585521 173990 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 710 13 10 19 -3.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3OC(O)C[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL454230 173990 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 710 13 10 19 -3.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3OC(O)C[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
52952395 61346 0 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 368 6 4 9 -0.9 CCSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767418 61346 0 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 368 6 4 9 -0.9 CCSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
53309245 62918 0 None -1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784886 62918 0 None -1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
52952391 61342 0 None -4 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 418 7 5 11 -1.9 COc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767414 61342 0 None -4 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 418 7 5 11 -1.9 COc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
189010 184231 12 None -1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 564 10 8 14 -2.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL483502 184231 12 None -1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 564 10 8 14 -2.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
44586005 184329 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 526 9 8 12 -2.8 NC(=O)N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
CHEMBL484295 184329 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 526 9 8 12 -2.8 NC(=O)N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
90656226 110916 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 718 14 7 14 0.9 N#CC(CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1)(c1ccccc1)c1ccccc1 10.1021/jm500367e
CHEMBL3261375 110916 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 718 14 7 14 0.9 N#CC(CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1)(c1ccccc1)c1ccccc1 10.1021/jm500367e
90656210 110900 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 585 13 8 14 -2.2 O=C(O)CCCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
CHEMBL3261359 110900 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 585 13 8 14 -2.2 O=C(O)CCCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
44585516 172595 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 696 13 10 19 -3.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@@H]3OC(O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL448985 172595 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 696 13 10 19 -3.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@@H]3OC(O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
1734 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm2013198
3639 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm2013198
6133 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm2013198
CHEMBL336296 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm2013198
DB04005 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm2013198
1734 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.ejmech.2008.07.015
3639 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.ejmech.2008.07.015
6133 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.ejmech.2008.07.015
CHEMBL336296 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.ejmech.2008.07.015
DB04005 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.ejmech.2008.07.015
10929115 201683 0 None -5 2 Human 7.3 pEC50 = 7.3 Functional
Measure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cell
ChEMBL 494 8 7 11 -1.8 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm010369e
CHEMBL606210 201683 0 None -5 2 Human 7.3 pEC50 = 7.3 Functional
Measure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cell
ChEMBL 494 8 7 11 -1.8 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm010369e
52952281 61339 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 462 9 5 11 -0.4 CCCSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767411 61339 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 462 9 5 11 -0.4 CCCSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
49867142 52 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 10.1021/jm1016297
6201 52 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 10.1021/jm1016297
CHEMBL1233534 52 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 10.1021/jm1016297
46831692 14196 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083764 14196 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1198849 14196 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
1734 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901450d
3639 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901450d
6133 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901450d
CHEMBL336296 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901450d
DB04005 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901450d
44586027 184117 1 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 660 12 9 16 -0.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL482683 184117 1 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 660 12 9 16 -0.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
44585988 184083 0 None -5 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 530 9 6 13 0.3 CSc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)n1 10.1016/j.bmc.2008.05.013
CHEMBL482472 184083 0 None -5 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 530 9 6 13 0.3 CSc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)n1 10.1016/j.bmc.2008.05.013
90656211 110901 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 631 14 7 13 -0.0 O=c1[nH]/c(=N\OCCCCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261360 110901 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 631 14 7 13 -0.0 O=c1[nH]/c(=N\OCCCCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
135528590 188759 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 813 14 10 22 -3.0 Nc1nc(=O)c2ncn([C@H]3C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]4O[C@@H](n5ccc(=O)[nH]c5=O)[C@H](O)[C@@H]4O)O3)c2[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL505403 188759 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 813 14 10 22 -3.0 Nc1nc(=O)c2ncn([C@H]3C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]4O[C@@H](n5ccc(=O)[nH]c5=O)[C@H](O)[C@@H]4O)O3)c2[nH]1 10.1016/j.bmc.2008.05.013
44586025 184084 1 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 580 10 8 14 -1.0 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL482485 184084 1 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 580 10 8 14 -1.0 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
46830492 6615 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 768 14 9 21 -4.1 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OC)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083257 6615 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 768 14 9 21 -4.1 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OC)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
52952282 61340 0 None 1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 510 9 5 11 0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(SCc2ccccc2)n1 10.1021/jm1016297
CHEMBL1767412 61340 0 None 1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 510 9 5 11 0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(SCc2ccccc2)n1 10.1021/jm1016297
10255482 61884 18 None 10 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assay
ChEMBL 502 8 7 12 -2.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/jm901450d
CHEMBL1774 61884 18 None 10 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assay
ChEMBL 502 8 7 12 -2.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/jm901450d
53262904 62930 0 None 11 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 728 13 10 19 -3.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](F)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784904 62930 0 None 11 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 728 13 10 19 -3.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](F)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
53309379 62919 0 None 4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 696 12 10 19 -3.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3OC[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784887 62919 0 None 4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 696 12 10 19 -3.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3OC[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
46831386 14234 0 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 475 7 6 11 -1.3 CC(C)(C)O/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1084296 14234 0 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 475 7 6 11 -1.3 CC(C)(C)O/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1199210 14234 0 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 475 7 6 11 -1.3 CC(C)(C)O/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
44585517 188336 0 None -1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 724 14 10 19 -3.1 CC[C@]1(O)O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)[C@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL500840 188336 0 None -1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 724 14 10 19 -3.1 CC[C@]1(O)O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)[C@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
90666798 109427 0 None -5 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 815 15 9 20 -2.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OCc5ccccc5)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL3220054 109427 0 None -5 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 815 15 9 20 -2.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OCc5ccccc5)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
45485253 199027 0 None -12 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1084020 199027 0 None -12 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1204010 199027 0 None -12 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL4846821 199027 0 None -12 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL585870 199027 0 None -12 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
53309528 62858 0 None 3 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 833 16 10 20 -1.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](F)[C@H]2O)[C@@H](O)[C@H]1O 10.1021/jm101591j
CHEMBL1784291 62858 0 None 3 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 833 16 10 20 -1.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](F)[C@H]2O)[C@@H](O)[C@H]1O 10.1021/jm101591j
90656230 2666 0 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1387 36 10 24 4.5 O=C(COc1ccc(cc1)CCCONc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O)NCCc1nnn(c1)CCCNC(=O)CCCCCNC(=O)COc1ccc(cc1)/C=C/c1ccc2n1[B-](F)(F)[N+]1=C(C=CC1=C2)c1cccs1 10.1021/jm500367e
9469 2666 0 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1387 36 10 24 4.5 O=C(COc1ccc(cc1)CCCONc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O)NCCc1nnn(c1)CCCNC(=O)CCCCCNC(=O)COc1ccc(cc1)/C=C/c1ccc2n1[B-](F)(F)[N+]1=C(C=CC1=C2)c1cccs1 10.1021/jm500367e
CHEMBL3261378 2666 0 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1387 36 10 24 4.5 O=C(COc1ccc(cc1)CCCONc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O)NCCc1nnn(c1)CCCNC(=O)CCCCCNC(=O)COc1ccc(cc1)/C=C/c1ccc2n1[B-](F)(F)[N+]1=C(C=CC1=C2)c1cccs1 10.1021/jm500367e
44439743 147587 0 None -229 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 517 8 6 11 -0.0 O=c1c2ccccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
CHEMBL393100 147587 0 None -229 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 517 8 6 11 -0.0 O=c1c2ccccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
24857827 189047 0 None -8 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 789 14 9 21 -1.5 Nc1ccn([C@H]2C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=S)[C@H](O)[C@@H]3O)O2)c(=O)n1 10.1016/j.bmc.2008.05.013
CHEMBL509434 189047 0 None -8 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 789 14 9 21 -1.5 Nc1ccn([C@H]2C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=S)[C@H](O)[C@@H]3O)O2)c(=O)n1 10.1016/j.bmc.2008.05.013
23379800 80486 0 None -56 4 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 482 6 6 10 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br 10.1021/jm060848j
CHEMBL214698 80486 0 None -56 4 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 482 6 6 10 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br 10.1021/jm060848j
1734 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
3639 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
6133 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
CHEMBL336296 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
DB04005 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
53262890 2896 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
6200 2896 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
CHEMBL1784893 2896 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
52952497 61082 0 None -51 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 668 11 6 13 0.1 O=C(Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c1=O)c1ccccc1 10.1021/jm1016297
CHEMBL1765115 61082 0 None -51 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 668 11 6 13 0.1 O=C(Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c1=O)c1ccccc1 10.1021/jm1016297
189010 184231 12 None -1 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 564 10 8 14 -2.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL483502 184231 12 None -1 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 564 10 8 14 -2.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
90666791 109423 0 None -234 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 587 9 6 11 -0.2 O=c1[nH]/c(=N\OCc2ccc(Br)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL3220048 109423 0 None -234 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 587 9 6 11 -0.2 O=c1[nH]/c(=N\OCc2ccc(Br)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
52952603 61083 0 None -4 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1765116 61083 0 None -4 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
46830491 14189 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083256 14189 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1198754 14189 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL4279296 14189 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
46830491 14189 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL1083256 14189 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL1198754 14189 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL4279296 14189 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
44586006 184362 0 None -56 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL484494 184362 0 None -56 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
9853990 188674 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 822 14 10 21 -1.5 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=S)[nH]c3=O)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL503798 188674 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 822 14 10 21 -1.5 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=S)[nH]c3=O)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
1734 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
3639 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
6133 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
CHEMBL336296 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
DB04005 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
1737 1367 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1021/jm1016297
9875516 1367 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1021/jm1016297
CHEMBL507282 1367 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1021/jm1016297
DB04983 1367 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1021/jm1016297
44585986 184328 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 534 8 7 11 -0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL484290 184328 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 534 8 7 11 -0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
44420650 84256 0 None -17 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 583 9 7 12 0.0 CC(C)(C)C(=O)N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=S 10.1021/jm060903o
CHEMBL221162 84256 0 None -17 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 583 9 7 12 0.0 CC(C)(C)C(=O)N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=S 10.1021/jm060903o
90656219 110909 0 None 5 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 662 14 7 15 -0.5 O=c1[nH]/c(=N\OCCCc2ccc([N+](=O)[O-])cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261368 110909 0 None 5 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 662 14 7 15 -0.5 O=c1[nH]/c(=N\OCCCc2ccc([N+](=O)[O-])cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
46890111 6752 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 478 8 6 10 -0.8 O=c1ccn([C@H]2C[C@H](O)[C@@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083763 6752 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 478 8 6 10 -0.8 O=c1ccn([C@H]2C[C@H](O)[C@@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm100287t
10929115 201683 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cell
ChEMBL 494 8 7 11 -1.8 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm010369e
CHEMBL606210 201683 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cell
ChEMBL 494 8 7 11 -1.8 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm010369e
1734 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060848j
3639 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060848j
6133 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060848j
CHEMBL336296 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060848j
DB04005 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060848j
148197 1438 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
1736 1438 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
4900 1438 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
CHEMBL221326 1438 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
DB15919 1438 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
9875011 90715 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL239151 90715 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
9875011 90715 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL239151 90715 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
9875011 90715 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL239151 90715 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
1734 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
3639 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
6133 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
CHEMBL336296 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
DB04005 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
1734 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
3639 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
6133 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
CHEMBL336296 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
DB04005 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
1734 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
3639 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
6133 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
CHEMBL336296 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
DB04005 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
44585987 191802 0 None 2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL519835 191802 0 None 2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
1734 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
3639 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
6133 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
CHEMBL336296 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
DB04005 3966 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
1734 3966 50 None -1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2012.07.042
3639 3966 50 None -1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2012.07.042
6133 3966 50 None -1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2012.07.042
CHEMBL336296 3966 50 None -1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2012.07.042
DB04005 3966 50 None -1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2012.07.042
90656217 110907 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 743 13 7 13 0.2 O=c1[nH]/c(=N\OCCCc2ccc(I)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261366 110907 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 743 13 7 13 0.2 O=c1[nH]/c(=N\OCCCc2ccc(I)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
53309380 62921 0 None 2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 767 14 11 20 -4.4 CC(=O)N[C@H]1[C@@H](OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)O[C@H](CO)[C@@H](O)[C@@H]1O 10.1021/jm101591j
CHEMBL1784889 62921 0 None 2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 767 14 11 20 -4.4 CC(=O)N[C@H]1[C@@H](OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)O[C@H](CO)[C@@H](O)[C@@H]1O 10.1021/jm101591j
52952605 3208 10 None -70 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 534 8 7 11 -0.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(C(P(=O)(O)O)(F)F)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
5902 3208 10 None -70 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 534 8 7 11 -0.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(C(P(=O)(O)O)(F)F)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
CHEMBL1765119 3208 10 None -70 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 534 8 7 11 -0.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(C(P(=O)(O)O)(F)F)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
CHEMBL2029010 209148 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL None None None BP(=O)(OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC 10.1021/jm2013198
90656218 110908 0 None 4 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 662 14 7 15 -0.5 O=c1[nH]/c(=N\OCCCc2cccc([N+](=O)[O-])c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261367 110908 0 None 4 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 662 14 7 15 -0.5 O=c1[nH]/c(=N\OCCCc2cccc([N+](=O)[O-])c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
90666794 109426 0 None -9 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 585 10 6 11 -0.2 C#CCCC#Cc1cccc(CO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)c1 10.1039/c3md00132f
CHEMBL3220051 109426 0 None -9 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 585 10 6 11 -0.2 C#CCCC#Cc1cccc(CO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)c1 10.1039/c3md00132f
53308272 62924 0 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 589 11 7 13 -0.8 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm101591j
CHEMBL1784892 62924 0 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 589 11 7 13 -0.8 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm101591j
53308272 62924 0 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 589 11 7 13 -0.8 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL1784892 62924 0 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 589 11 7 13 -0.8 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
25125168 14918 0 None 1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Cl)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1208098 14918 0 None 1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Cl)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL496401 14918 0 None 1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Cl)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
3018777 60250 6 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/jm1012193
CHEMBL1671995 60250 6 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/jm1012193
CHEMBL1741070 60250 6 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/jm1012193
53308119 60256 0 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Nc3nc(Cl)nc(Cl)n3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1672105 60256 0 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Nc3nc(Cl)nc(Cl)n3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1741085 60256 0 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Nc3nc(Cl)nc(Cl)n3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
53326685 60257 0 None 3 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 520 5 6 12 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(O)nc(O)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1672106 60257 0 None 3 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 520 5 6 12 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(O)nc(O)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1741086 60257 0 None 3 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 520 5 6 12 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(O)nc(O)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
137648293 157575 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 390 3 3 5 3.9 Cc1cc(Nc2ccc(F)cc2C(=O)O)c2c(c1N)C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4080560 157575 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 390 3 3 5 3.9 Cc1cc(Nc2ccc(F)cc2C(=O)O)c2c(c1N)C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25124826 14926 2 None -1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL1208118 14926 2 None -1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL498423 14926 2 None -1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
44152335 14730 1 None 1 3 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1206280 14730 1 None 1 3 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL256689 14730 1 None 1 3 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
136677322 3296 24 None -158 9 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.7b00030
1739 3296 24 None -158 9 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.7b00030
656725 3296 24 None -158 9 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.7b00030
CHEMBL1160031 3296 24 None -158 9 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.7b00030
25128135 14919 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 502 5 3 7 5.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Sc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208102 14919 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 502 5 3 7 5.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Sc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL496620 14919 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 502 5 3 7 5.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Sc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
51050135 60255 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 430 3 3 6 3.3 Nc1c(S(=O)(=O)O)cc(Nc2cc(F)cc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1672099 60255 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 430 3 3 6 3.3 Nc1c(S(=O)(=O)O)cc(Nc2cc(F)cc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1741083 60255 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 430 3 3 6 3.3 Nc1c(S(=O)(=O)O)cc(Nc2cc(F)cc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
46504926 191332 31 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y4R expressed in HEK293 cells assessed as inhibition of UTP-induced IP3 production preincubated for 0.5 hrs followed by UTP stimulation by ELISAAntagonist activity at human P2Y4R expressed in HEK293 cells assessed as inhibition of UTP-induced IP3 production preincubated for 0.5 hrs followed by UTP stimulation by ELISA
ChEMBL 522 4 1 3 5.2 O=C(C1CC1)N1CCc2cc(Br)c(S(=O)(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc21 10.1021/acs.jmedchem.2c01632
CHEMBL5191550 191332 31 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y4R expressed in HEK293 cells assessed as inhibition of UTP-induced IP3 production preincubated for 0.5 hrs followed by UTP stimulation by ELISAAntagonist activity at human P2Y4R expressed in HEK293 cells assessed as inhibition of UTP-induced IP3 production preincubated for 0.5 hrs followed by UTP stimulation by ELISA
ChEMBL 522 4 1 3 5.2 O=C(C1CC1)N1CCc2cc(Br)c(S(=O)(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc21 10.1021/acs.jmedchem.2c01632
51050133 60261 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1671997 60261 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1741100 60261 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
20658940 14923 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 4 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208114 14923 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 4 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL498223 14923 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 4 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25124828 14931 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 600 6 5 11 4.0 Nc1c(S(=O)(=O)O)cc(Nc2cc(Nc3nc(Cl)nc(Cl)n3)cc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1208131 14931 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 600 6 5 11 4.0 Nc1c(S(=O)(=O)O)cc(Nc2cc(Nc3nc(Cl)nc(Cl)n3)cc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL499580 14931 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 600 6 5 11 4.0 Nc1c(S(=O)(=O)O)cc(Nc2cc(Nc3nc(Cl)nc(Cl)n3)cc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
51050129 60253 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1671993 60253 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1741081 60253 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
137630446 161065 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 4 3 7 3.2 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1F 10.1021/acs.jmedchem.7b00030
CHEMBL4090513 161065 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 4 3 7 3.2 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1F 10.1021/acs.jmedchem.7b00030
CHEMBL4116637 161065 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 4 3 7 3.2 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1F 10.1021/acs.jmedchem.7b00030
137631028 161146 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
CHEMBL4082692 161146 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
CHEMBL4117312 161146 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
137630150 161052 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 504 5 3 7 5.0 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(F)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4074456 161052 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 504 5 3 7 5.0 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(F)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116573 161052 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 504 5 3 7 5.0 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(F)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
3018777 60250 6 None 2 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1671995 60250 6 None 2 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1741070 60250 6 None 2 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
137630536 161079 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 564 5 3 7 5.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Br)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4065831 161079 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 564 5 3 7 5.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Br)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116759 161079 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 564 5 3 7 5.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Br)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25123180 14834 0 None 2 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1207384 14834 0 None 2 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL401859 14834 0 None 2 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25127814 14951 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 486 5 3 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208433 14951 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 486 5 3 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL597203 14951 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 486 5 3 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
22916 14725 22 None -2 6 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1206272 14725 22 None -2 6 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL256057 14725 22 None -2 6 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137629896 161017 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 4 5 8 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4067679 161017 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 4 5 8 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116314 161017 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 4 5 8 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25124484 14750 0 None 3 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1206415 14750 0 None 3 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL271672 14750 0 None 3 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
71531032 161006 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Cl)ccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4060811 161006 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Cl)ccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116227 161006 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Cl)ccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
106250 14916 6 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1208092 14916 6 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL496030 14916 6 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
21130371 14887 0 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1207842 14887 0 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL445413 14887 0 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
137630000 161030 0 None 10 5 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c(C)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4087247 161030 0 None 10 5 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c(C)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4116405 161030 0 None 10 5 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c(C)c1 10.1021/acs.jmedchem.7b00030
25124484 14750 0 None 3 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1206415 14750 0 None 3 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL271672 14750 0 None 3 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
11970419 14953 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208450 14953 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL598857 14953 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
106250 14916 6 None 1 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL1208092 14916 6 None 1 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL496030 14916 6 None 1 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
22916 14725 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1206272 14725 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL256057 14725 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
22916 14725 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL1206272 14725 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL256057 14725 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
108643 3215 6 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/acs.jmedchem.7b00030
9468 3215 6 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/acs.jmedchem.7b00030
CHEMBL1207381 3215 6 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/acs.jmedchem.7b00030
44456166 14836 0 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1021/acs.jmedchem.7b00030
CHEMBL1207392 14836 0 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1021/acs.jmedchem.7b00030
CHEMBL402239 14836 0 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1021/acs.jmedchem.7b00030
16120270 14944 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 4 4 7 3.4 Nc1c(S(=O)(=O)O)cc(Nc2cc(Cl)ccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208282 14944 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 4 4 7 3.4 Nc1c(S(=O)(=O)O)cc(Nc2cc(Cl)ccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL522053 14944 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 4 4 7 3.4 Nc1c(S(=O)(=O)O)cc(Nc2cc(Cl)ccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
117532 14851 8 None 8 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
CHEMBL1207421 14851 8 None 8 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
CHEMBL404450 14851 8 None 8 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
137630776 161107 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 436 5 3 6 4.0 CCCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4063945 161107 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 436 5 3 6 4.0 CCCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4117065 161107 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 436 5 3 6 4.0 CCCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
25114303 14956 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(C(=O)O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208486 14956 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(C(=O)O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL604300 14956 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(C(=O)O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
51050133 60261 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1671997 60261 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1741100 60261 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
13782419 14751 2 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1206416 14751 2 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL271673 14751 2 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
106250 14916 6 None 1 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208092 14916 6 None 1 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL496030 14916 6 None 1 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
56944331 161106 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
CHEMBL4078095 161106 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
CHEMBL4117064 161106 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
46228693 14954 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Br)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208451 14954 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Br)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL599050 14954 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Br)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137630585 161086 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 458 4 3 7 3.7 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
CHEMBL4081964 161086 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 458 4 3 7 3.7 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
CHEMBL4116837 161086 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 458 4 3 7 3.7 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
25127813 14913 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 484 5 3 6 4.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208083 14913 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 484 5 3 6 4.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL495605 14913 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 484 5 3 6 4.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
117530 14732 5 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1206282 14732 5 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL256864 14732 5 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
44456161 14835 0 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1207391 14835 0 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL402238 14835 0 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
109055 14729 1 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1206279 14729 1 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1021/acs.jmedchem.7b00030
CHEMBL256688 14729 1 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1021/acs.jmedchem.7b00030
137629897 161018 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 520 5 3 7 5.5 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Cl)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4094930 161018 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 520 5 3 7 5.5 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Cl)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116315 161018 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 520 5 3 7 5.5 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Cl)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137630586 161087 0 None 6 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(C)c(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4081274 161087 0 None 6 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(C)c(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4116838 161087 0 None 6 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(C)c(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c1 10.1021/acs.jmedchem.7b00030
3018582 14737 6 None -1 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1206290 14737 6 None -1 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL257495 14737 6 None -1 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25124160 14955 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(F)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208485 14955 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(F)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL604158 14955 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(F)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137630492 161077 0 None 8 4 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 517 6 3 8 4.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(SCc3cccnc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4090874 161077 0 None 8 4 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 517 6 3 8 4.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(SCc3cccnc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116755 161077 0 None 8 4 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 517 6 3 8 4.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(SCc3cccnc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137629595 161133 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 3 7 3.4 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1C 10.1021/acs.jmedchem.7b00030
CHEMBL4072198 161133 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 3 7 3.4 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1C 10.1021/acs.jmedchem.7b00030
CHEMBL4117231 161133 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 3 7 3.4 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1C 10.1021/acs.jmedchem.7b00030
11451 3211 0 None 6 5 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 10.1021/acs.jmedchem.7b00030
132574707 3211 0 None 6 5 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 10.1021/acs.jmedchem.7b00030
CHEMBL4116316 3211 0 None 6 5 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 10.1021/acs.jmedchem.7b00030
137635750 161220 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1OC 10.1021/acs.jmedchem.7b00030
CHEMBL4063599 161220 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1OC 10.1021/acs.jmedchem.7b00030
CHEMBL4117950 161220 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1OC 10.1021/acs.jmedchem.7b00030
3018582 14737 6 None -1 3 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y4 receptorAntagonist activity at human P2Y4 receptor
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1206290 14737 6 None -1 3 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y4 receptorAntagonist activity at human P2Y4 receptor
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL257495 14737 6 None -1 3 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y4 receptorAntagonist activity at human P2Y4 receptor
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
136677322 3296 24 None -158 9 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm800175e
1739 3296 24 None -158 9 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm800175e
656725 3296 24 None -158 9 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm800175e
CHEMBL1160031 3296 24 None -158 9 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm800175e
25114519 14946 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208288 14946 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL524064 14946 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
136677323 10212 6 None -7 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Nc4ccc(S(=O)(=O)O)cc4)n3)c(S(=O)(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
3638737 10212 6 None -7 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Nc4ccc(S(=O)(=O)O)cc4)n3)c(S(=O)(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1160025 10212 6 None -7 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Nc4ccc(S(=O)(=O)O)cc4)n3)c(S(=O)(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1365553 10212 6 None -7 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Nc4ccc(S(=O)(=O)O)cc4)n3)c(S(=O)(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25124162 60259 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cc(C)cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1671994 60259 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cc(C)cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1741096 60259 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cc(C)cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
25124161 60254 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Br)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1672098 60254 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Br)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1741082 60254 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Br)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
15404279 14924 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 5 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208115 14924 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 5 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL498224 14924 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 5 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
136126658 54969 0 None -1 2 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 510 8 5 10 2.0 Cc1cc(/N=N/c2ccc(S(=O)(=O)O)cc2S(=O)(=O)O)c(COP(=O)(O)O)c(C=O)c1O 10.1021/jm800175e
CHEMBL1615626 54969 0 None -1 2 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 510 8 5 10 2.0 Cc1cc(/N=N/c2ccc(S(=O)(=O)O)cc2S(=O)(=O)O)c(COP(=O)(O)O)c(C=O)c1O 10.1021/jm800175e
CHEMBL477339 54969 0 None -1 2 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 510 8 5 10 2.0 Cc1cc(/N=N/c2ccc(S(=O)(=O)O)cc2S(=O)(=O)O)c(COP(=O)(O)O)c(C=O)c1O 10.1021/jm800175e
25124826 14926 2 None -1 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208118 14926 2 None -1 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL498423 14926 2 None -1 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137630841 161113 0 None -12 5 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 3 4 7 3.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1O 10.1021/acs.jmedchem.7b00030
CHEMBL4069492 161113 0 None -12 5 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 3 4 7 3.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1O 10.1021/acs.jmedchem.7b00030
CHEMBL4117118 161113 0 None -12 5 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 3 4 7 3.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1O 10.1021/acs.jmedchem.7b00030
51050131 60251 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc(OC)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1671996 60251 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc(OC)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1741071 60251 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc(OC)c1 10.1021/acs.jmedchem.7b00030
137645876 161207 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2Cl)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4084432 161207 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2Cl)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4117856 161207 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2Cl)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
136677322 3296 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm1012193
1739 3296 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm1012193
656725 3296 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm1012193
CHEMBL1160031 3296 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm1012193
136677322 3296 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm901851t
1739 3296 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm901851t
656725 3296 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm901851t
CHEMBL1160031 3296 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm901851t
1734 3966 50 None -3 7 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
3639 3966 50 None -3 7 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
6133 3966 50 None -3 7 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
CHEMBL336296 3966 50 None -3 7 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
DB04005 3966 50 None -3 7 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
1713 520 68 None -20 10 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
5957 520 68 None -20 10 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
91 520 68 None -20 10 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
CHEMBL14249 520 68 None -20 10 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
DB00171 520 68 None -20 10 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
1734 3966 50 None -1 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
3639 3966 50 None -1 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
6133 3966 50 None -1 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
CHEMBL336296 3966 50 None -1 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
DB04005 3966 50 None -1 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
148197 1438 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
1736 1438 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
4900 1438 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
CHEMBL221326 1438 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
DB15919 1438 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
1725 3153 17 None -100 6 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 511 8 5 11 1.4 O=Cc1c(COP(=O)(O)O)c(/N=N/c2ccc(cc2S(=O)(=O)O)S(=O)(=O)O)nc(c1O)C 18600475
4881 3153 17 None -100 6 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 511 8 5 11 1.4 O=Cc1c(COP(=O)(O)O)c(/N=N/c2ccc(cc2S(=O)(=O)O)S(=O)(=O)O)nc(c1O)C 18600475
CHEMBL1437958 3153 17 None -100 6 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 511 8 5 11 1.4 O=Cc1c(COP(=O)(O)O)c(/N=N/c2ccc(cc2S(=O)(=O)O)S(=O)(=O)O)nc(c1O)C 18600475
CHEMBL69234 3153 17 None -100 6 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 511 8 5 11 1.4 O=Cc1c(COP(=O)(O)O)c(/N=N/c2ccc(cc2S(=O)(=O)O)S(=O)(=O)O)nc(c1O)C 18600475
49867142 52 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 21417463
6201 52 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 21417463
CHEMBL1233534 52 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 21417463
1713 520 68 None -630 10 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21193033
5957 520 68 None -630 10 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21193033
91 520 68 None -630 10 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21193033
CHEMBL14249 520 68 None -630 10 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21193033
DB00171 520 68 None -630 10 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21193033
1713 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
1713 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 12213051
1713 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 9647463
5957 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
5957 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 12213051
5957 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 9647463
91 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
91 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 12213051
91 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 9647463
CHEMBL14249 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
CHEMBL14249 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 12213051
CHEMBL14249 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 9647463
DB00171 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
DB00171 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 12213051
DB00171 520 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 9647463
1737 1367 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 12183642
9875516 1367 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 12183642
CHEMBL507282 1367 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 12183642
DB04983 1367 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 12183642
1734 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10779375
3639 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10779375
6133 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10779375
CHEMBL336296 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10779375
DB04005 3966 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10779375
148197 1438 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
1736 1438 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
4900 1438 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
CHEMBL221326 1438 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
DB15919 1438 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
1740 2833 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 8 7 11 -1.8 OC1C(n2ccc(=O)[nH]c2=O)C2C(C1O)(C2)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 11754592
44309485 2833 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 8 7 11 -1.8 OC1C(n2ccc(=O)[nH]c2=O)C2C(C1O)(C2)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 11754592
53262890 2896 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
6200 2896 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
CHEMBL1784893 2896 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
6199 2661 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 727 13 10 18 -3.4 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)C2C=CC(=O)NC2=O)O)O)O)O)[C@@H]([C@H]([C@@H]1O)F)O 21528910
91827350 2661 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 727 13 10 18 -3.4 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)C2C=CC(=O)NC2=O)O)O)O)O)[C@@H]([C@H]([C@@H]1O)F)O 21528910
4044 2665 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
53262902 2665 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
CHEMBL1784894 2665 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
1741 1217 62 None 4 2 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 483 8 7 13 -2.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(nc1=O)N 10779375
6176 1217 62 None 4 2 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 483 8 7 13 -2.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(nc1=O)N 10779375
CHEMBL223533 1217 62 None 4 2 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 483 8 7 13 -2.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(nc1=O)N 10779375
DB02431 1217 62 None 4 2 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 483 8 7 13 -2.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(nc1=O)N 10779375
135398643 2101 0 None -4 2 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
1743 2101 0 None -4 2 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
CHEMBL1233686 2101 0 None -4 2 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
135398633 1890 0 None -2 2 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
1742 1890 0 None -2 2 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
CHEMBL1233147 1890 0 None -2 2 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
DB04137 1890 0 None -2 2 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
135398633 1890 0 None 2 2 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
1742 1890 0 None 2 2 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
CHEMBL1233147 1890 0 None 2 2 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
DB04137 1890 0 None 2 2 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
1734 3966 50 None -3 7 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 9647463
3639 3966 50 None -3 7 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 9647463
6133 3966 50 None -3 7 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 9647463
CHEMBL336296 3966 50 None -3 7 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 9647463
DB04005 3966 50 None -3 7 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 9647463
135398643 2101 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
135398643 2101 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 9647463
1743 2101 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
1743 2101 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 9647463
CHEMBL1233686 2101 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
CHEMBL1233686 2101 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 9647463
1732 450 0 None -6 4 Rat 5.9 pEC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 832 14 6 29 -5.0 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2cnc3c2ncnc3N)[O-])[O-])[O-])[O-])O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
25243905 450 0 None -6 4 Rat 5.9 pEC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 832 14 6 29 -5.0 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2cnc3c2ncnc3N)[O-])[O-])[O-])[O-])O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
136677322 3296 24 None -446 9 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 9647463
1739 3296 24 None -446 9 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 9647463
656725 3296 24 None -446 9 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 9647463
CHEMBL1160031 3296 24 None -446 9 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 9647463
11451 3211 0 None 6 5 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 28306255
132574707 3211 0 None 6 5 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 28306255
CHEMBL4116316 3211 0 None 6 5 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 28306255


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
1713 520 68 None - 2 Rat 5.9 pEC50 = 5.9 Binding
Antagonist activity at rat P2Y4Antagonist activity at rat P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
5957 520 68 None - 2 Rat 5.9 pEC50 = 5.9 Binding
Antagonist activity at rat P2Y4Antagonist activity at rat P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
91 520 68 None - 2 Rat 5.9 pEC50 = 5.9 Binding
Antagonist activity at rat P2Y4Antagonist activity at rat P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
CHEMBL14249 520 68 None - 2 Rat 5.9 pEC50 = 5.9 Binding
Antagonist activity at rat P2Y4Antagonist activity at rat P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
DB00171 520 68 None - 2 Rat 5.9 pEC50 = 5.9 Binding
Antagonist activity at rat P2Y4Antagonist activity at rat P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
90656232 110919 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assay
ChEMBL 1056 24 10 23 0.0 O=c1[nH]/c(=N\OCCCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cc/c(=N/OCCCc4ccccc4)[nH]c3=O)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261380 110919 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assay
ChEMBL 1056 24 10 23 0.0 O=c1[nH]/c(=N\OCCCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cc/c(=N/OCCCc4ccccc4)[nH]c3=O)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1021/jm500367e
1734 3966 50 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human P2Y4 transfected in human 1321N1 cellsAgonist activity at human P2Y4 transfected in human 1321N1 cells
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.5b01972
3639 3966 50 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human P2Y4 transfected in human 1321N1 cellsAgonist activity at human P2Y4 transfected in human 1321N1 cells
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.5b01972
6133 3966 50 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human P2Y4 transfected in human 1321N1 cellsAgonist activity at human P2Y4 transfected in human 1321N1 cells
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.5b01972
CHEMBL336296 3966 50 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human P2Y4 transfected in human 1321N1 cellsAgonist activity at human P2Y4 transfected in human 1321N1 cells
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.5b01972
DB04005 3966 50 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human P2Y4 transfected in human 1321N1 cellsAgonist activity at human P2Y4 transfected in human 1321N1 cells
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.5b01972
1713 520 68 None 257 2 Human 5.2 pEC50 = 5.2 Binding
Antagonist activity at human P2Y4Antagonist activity at human P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
5957 520 68 None 257 2 Human 5.2 pEC50 = 5.2 Binding
Antagonist activity at human P2Y4Antagonist activity at human P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
91 520 68 None 257 2 Human 5.2 pEC50 = 5.2 Binding
Antagonist activity at human P2Y4Antagonist activity at human P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
CHEMBL14249 520 68 None 257 2 Human 5.2 pEC50 = 5.2 Binding
Antagonist activity at human P2Y4Antagonist activity at human P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
DB00171 520 68 None 257 2 Human 5.2 pEC50 = 5.2 Binding
Antagonist activity at human P2Y4Antagonist activity at human P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
136677322 3296 24 None - 1 Rat 5.2 pEC50 = 5.2 Binding
Antagonist activity at rat P2Y4 transfected in xenopus oocyte cellAntagonist activity at rat P2Y4 transfected in xenopus oocyte cell
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.5b01972
1739 3296 24 None - 1 Rat 5.2 pEC50 = 5.2 Binding
Antagonist activity at rat P2Y4 transfected in xenopus oocyte cellAntagonist activity at rat P2Y4 transfected in xenopus oocyte cell
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.5b01972
656725 3296 24 None - 1 Rat 5.2 pEC50 = 5.2 Binding
Antagonist activity at rat P2Y4 transfected in xenopus oocyte cellAntagonist activity at rat P2Y4 transfected in xenopus oocyte cell
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.5b01972
CHEMBL1160031 3296 24 None - 1 Rat 5.2 pEC50 = 5.2 Binding
Antagonist activity at rat P2Y4 transfected in xenopus oocyte cellAntagonist activity at rat P2Y4 transfected in xenopus oocyte cell
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.5b01972
90656231 110918 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assay
ChEMBL 923 19 10 22 -2.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OCCCc5ccccc5)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
CHEMBL3261379 110918 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assay
ChEMBL 923 19 10 22 -2.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OCCCc5ccccc5)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
1713 520 68 None 257 2 Human 6.2 pKd = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
5957 520 68 None 257 2 Human 6.2 pKd = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
91 520 68 None 257 2 Human 6.2 pKd = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
CHEMBL14249 520 68 None 257 2 Human 6.2 pKd = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
DB00171 520 68 None 257 2 Human 6.2 pKd = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
1713 520 68 None 257 2 Human 8.2 pKi = 8.2 Binding
GRAC: human P2Y4 selective antagonistGRAC: human P2Y4 selective antagonist
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
5957 520 68 None 257 2 Human 8.2 pKi = 8.2 Binding
GRAC: human P2Y4 selective antagonistGRAC: human P2Y4 selective antagonist
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
91 520 68 None 257 2 Human 8.2 pKi = 8.2 Binding
GRAC: human P2Y4 selective antagonistGRAC: human P2Y4 selective antagonist
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
CHEMBL14249 520 68 None 257 2 Human 8.2 pKi = 8.2 Binding
GRAC: human P2Y4 selective antagonistGRAC: human P2Y4 selective antagonist
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
DB00171 520 68 None 257 2 Human 8.2 pKi = 8.2 Binding
GRAC: human P2Y4 selective antagonistGRAC: human P2Y4 selective antagonist
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None