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
44439758 91270 0 None 1995 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.0 pEC50 = 8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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
10168108 145303 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 575 8 6 11 1.8 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3cc(C(F)(F)F)ccc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
CHEMBL391317 145303 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 575 8 6 11 1.8 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3cc(C(F)(F)F)ccc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
148197 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptorAgonist activity at P2Y2 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 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptorAgonist activity at P2Y2 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 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptorAgonist activity at P2Y2 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 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptorAgonist activity at P2Y2 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 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptorAgonist activity at P2Y2 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
148197 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptor (unknown origin) expressed in human 1321N1 cellsAgonist activity at P2Y2 receptor (unknown origin) expressed in human 1321N1 cells
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.2017.11.043
1736 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptor (unknown origin) expressed in human 1321N1 cellsAgonist activity at P2Y2 receptor (unknown origin) expressed in human 1321N1 cells
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.2017.11.043
4900 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptor (unknown origin) expressed in human 1321N1 cellsAgonist activity at P2Y2 receptor (unknown origin) expressed in human 1321N1 cells
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.2017.11.043
CHEMBL221326 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptor (unknown origin) expressed in human 1321N1 cellsAgonist activity at P2Y2 receptor (unknown origin) expressed in human 1321N1 cells
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.2017.11.043
DB15919 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptor (unknown origin) expressed in human 1321N1 cellsAgonist activity at P2Y2 receptor (unknown origin) expressed in human 1321N1 cells
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.2017.11.043
1734 3966 50 None 1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptor in human CF/T43 cellsAgonist activity at P2Y2 receptor in human CF/T43 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 10.1016/j.bmc.2017.11.043
3639 3966 50 None 1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptor in human CF/T43 cellsAgonist activity at P2Y2 receptor in human CF/T43 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 10.1016/j.bmc.2017.11.043
6133 3966 50 None 1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptor in human CF/T43 cellsAgonist activity at P2Y2 receptor in human CF/T43 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 10.1016/j.bmc.2017.11.043
CHEMBL336296 3966 50 None 1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptor in human CF/T43 cellsAgonist activity at P2Y2 receptor in human CF/T43 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 10.1016/j.bmc.2017.11.043
DB04005 3966 50 None 1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at P2Y2 receptor in human CF/T43 cellsAgonist activity at P2Y2 receptor in human CF/T43 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 10.1016/j.bmc.2017.11.043
148197 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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/jm901450d
1736 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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/jm901450d
4900 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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/jm901450d
CHEMBL221326 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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/jm901450d
DB15919 1438 23 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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/jm901450d
1734 3966 50 None 1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 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 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 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 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 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 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 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 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 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
44457427 14857 0 None 6 3 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 P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 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 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 P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 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 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 P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 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
1713 520 68 None -9 10 Human 6.0 pEC50 = 6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 6.0 pEC50 = 6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 6.0 pEC50 = 6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 6.0 pEC50 = 6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 6.0 pEC50 = 6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
57394895 71313 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 412 5 5 7 -0.3 Cc1ccc(-c2cn([C@@H]3O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]c2=O)cc1 10.1016/j.bmc.2012.02.012
CHEMBL1957442 71313 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 412 5 5 7 -0.3 Cc1ccc(-c2cn([C@@H]3O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]c2=O)cc1 10.1016/j.bmc.2012.02.012
44219764 193263 2 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
ChEMBL 480 7 7 11 -1.9 O=c1ccn([C@@H]2O[C@H](/C=C/P(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmcl.2009.04.027
CHEMBL523850 193263 2 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
ChEMBL 480 7 7 11 -1.9 O=c1ccn([C@@H]2O[C@H](/C=C/P(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmcl.2009.04.027
1783 3925 25 None -524 7 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cellsAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmc.2009.05.024
8629 3925 25 None -524 7 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cellsAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmc.2009.05.024
CHEMBL375951 3925 25 None -524 7 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cellsAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmc.2009.05.024
DB01861 3925 25 None -524 7 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cellsAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmc.2009.05.024
145968441 163629 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 553 9 6 14 -2.0 O=c1nc(N2CCOCC2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2017.11.043
CHEMBL4203866 163629 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 553 9 6 14 -2.0 O=c1nc(N2CCOCC2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2017.11.043
90656223 110913 0 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
CHEMBL3261372 110913 0 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
90656223 110913 0 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
1734 3966 50 None 1 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
65070 136949 31 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 468 8 6 11 -1.5 O=c1ccn([C@H]2C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]1 10.1021/jm060903o
CHEMBL374361 136949 31 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 468 8 6 11 -1.5 O=c1ccn([C@H]2C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]1 10.1021/jm060903o
145978391 163940 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 728 17 8 15 -1.3 C#CCNC(=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 10.1016/j.bmc.2017.11.043
CHEMBL4207607 163940 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 728 17 8 15 -1.3 C#CCNC(=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 10.1016/j.bmc.2017.11.043
90656227 110917 0 None -2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
1734 3966 50 None 1 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium levelAgonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium level
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/jm070043r
3639 3966 50 None 1 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium levelAgonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium level
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/jm070043r
6133 3966 50 None 1 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium levelAgonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium level
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/jm070043r
CHEMBL336296 3966 50 None 1 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium levelAgonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium level
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/jm070043r
DB04005 3966 50 None 1 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium levelAgonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium level
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/jm070043r
1713 520 68 None -9 10 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
148197 1438 23 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1736 1438 23 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
4900 1438 23 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL221326 1438 23 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB15919 1438 23 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1713 520 68 None -9 10 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44439759 91271 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 542 8 6 12 -0.2 N#Cc1ccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2c1 10.1016/j.bmcl.2006.09.017
CHEMBL240202 91271 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 542 8 6 12 -0.2 N#Cc1ccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2c1 10.1016/j.bmcl.2006.09.017
1713 520 68 None -9 10 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1734 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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.2017.11.043
3639 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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.2017.11.043
6133 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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.2017.11.043
CHEMBL336296 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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.2017.11.043
DB04005 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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.2017.11.043
52952604 61085 0 None 1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
52952281 61339 0 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
53262890 2896 0 None -16 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
1734 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
21706 117147 15 None 5 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL339385 117147 15 None 5 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1734 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1734 3966 50 None 1 7 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)
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.2017.11.043
3639 3966 50 None 1 7 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)
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.2017.11.043
6133 3966 50 None 1 7 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)
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.2017.11.043
CHEMBL336296 3966 50 None 1 7 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)
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.2017.11.043
DB04005 3966 50 None 1 7 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)
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.2017.11.043
1734 3966 50 None -12 7 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence assayAgonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence 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.2009.05.062
3639 3966 50 None -12 7 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence assayAgonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence 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.2009.05.062
6133 3966 50 None -12 7 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence assayAgonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence 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.2009.05.062
CHEMBL336296 3966 50 None -12 7 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence assayAgonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence 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.2009.05.062
DB04005 3966 50 None -12 7 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence assayAgonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence 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.2009.05.062
44439764 148375 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 585 8 6 11 1.3 O=c1c2cc(Cl)c(Cl)cc2ccn1[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
CHEMBL393741 148375 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 585 8 6 11 1.3 O=c1c2cc(Cl)c(Cl)cc2ccn1[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
1734 3966 50 None -1 7 Rat 6.9 pEC50 = 6.9 Functional
Activity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increaseActivity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increase
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/jm050955y
3639 3966 50 None -1 7 Rat 6.9 pEC50 = 6.9 Functional
Activity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increaseActivity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increase
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/jm050955y
6133 3966 50 None -1 7 Rat 6.9 pEC50 = 6.9 Functional
Activity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increaseActivity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increase
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/jm050955y
CHEMBL336296 3966 50 None -1 7 Rat 6.9 pEC50 = 6.9 Functional
Activity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increaseActivity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increase
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/jm050955y
DB04005 3966 50 None -1 7 Rat 6.9 pEC50 = 6.9 Functional
Activity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increaseActivity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increase
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/jm050955y
44457361 10359 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 923 17 10 23 -2.3 CNc1ccccc1C(=O)O[C@H]1[C@@H](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)O[C@@H]1n1ccc(=O)[nH]c1=O 10.1021/jm701348d
CHEMBL1162186 10359 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 923 17 10 23 -2.3 CNc1ccccc1C(=O)O[C@H]1[C@@H](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)O[C@@H]1n1ccc(=O)[nH]c1=O 10.1021/jm701348d
52952494 61348 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 444 8 4 9 0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]2O)c(SCCc2ccccc2)n1 10.1021/jm1016297
CHEMBL1767421 61348 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 444 8 4 9 0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]2O)c(SCCc2ccccc2)n1 10.1021/jm1016297
148197 1438 23 None 1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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
52952605 3208 10 None 52 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 52 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 52 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
44457390 10364 0 None -60 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization 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/jm701348d
CHEMBL1162193 10364 0 None -60 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization 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/jm701348d
1734 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
90656225 110915 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
CHEMBL3261374 110915 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
90656225 110915 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
24799317 10337 0 None -3 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 529 8 4 12 0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@H]2O[C@@H](Cc3ccccc3)O[C@H]21 10.1021/jm701348d
CHEMBL1162160 10337 0 None -3 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 529 8 4 12 0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@H]2O[C@@H](Cc3ccccc3)O[C@H]21 10.1021/jm701348d
24801414 10338 0 None -263 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 648 10 5 12 2.9 O=C(Nc1ccccc1)Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@H]2O[C@@H](Cc3ccccc3)O[C@H]21 10.1021/jm701348d
CHEMBL1162161 10338 0 None -263 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 648 10 5 12 2.9 O=C(Nc1ccccc1)Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@H]2O[C@@H](Cc3ccccc3)O[C@H]21 10.1021/jm701348d
1734 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulationAgonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulation
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.2017.11.043
3639 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulationAgonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulation
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.2017.11.043
6133 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulationAgonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulation
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.2017.11.043
CHEMBL336296 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulationAgonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulation
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.2017.11.043
DB04005 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulationAgonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulation
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.2017.11.043
1734 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GFP-tagged P2Y2 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y2 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human GFP-tagged P2Y2 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y2 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human GFP-tagged P2Y2 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y2 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human GFP-tagged P2Y2 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y2 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human GFP-tagged P2Y2 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y2 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
44439761 91275 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 563 9 6 12 0.7 CSc1ccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2c1 10.1016/j.bmcl.2006.09.017
CHEMBL240203 91275 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 563 9 6 12 0.7 CSc1ccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2c1 10.1016/j.bmcl.2006.09.017
1737 1367 7 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
44586006 184362 0 None 56 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
135528590 188759 0 None 3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
1734 3966 50 None 1 7 Human 6.9 pEC50 = 6.9 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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 6.9 pEC50 = 6.9 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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 6.9 pEC50 = 6.9 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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 6.9 pEC50 = 6.9 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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 6.9 pEC50 = 6.9 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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
497297 187367 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
ChEMBL 491 7 7 13 -1.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2009.04.027
CHEMBL493370 187367 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
ChEMBL 491 7 7 13 -1.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2009.04.027
44420644 83510 5 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 498 9 6 12 -1.8 CO[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
CHEMBL220337 83510 5 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 498 9 6 12 -1.8 CO[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
148197 1438 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1736 1438 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
4900 1438 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL221326 1438 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB15919 1438 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
21706 117147 15 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL339385 117147 15 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44586007 192595 1 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
44457274 10342 0 None -7 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 994 18 6 21 1.1 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](n4ccc(=O)[nH]c4=O)[C@@H]4OC(Cc5ccccc5)O[C@H]34)[C@@H]3OC(Cc4ccccc4)O[C@@H]32)c(=O)[nH]1 10.1021/jm701348d
CHEMBL1162165 10342 0 None -7 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 994 18 6 21 1.1 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](n4ccc(=O)[nH]c4=O)[C@@H]4OC(Cc5ccccc5)O[C@H]34)[C@@H]3OC(Cc4ccccc4)O[C@@H]32)c(=O)[nH]1 10.1021/jm701348d
44457392 10365 0 None 114 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 900 20 8 21 -0.4 CCCCCCCC1O[C@@H]2[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)O[C@@H](n3ccc(=O)[nH]c3=O)[C@@H]2O1 10.1021/jm701348d
CHEMBL1162194 10365 0 None 114 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 900 20 8 21 -0.4 CCCCCCCC1O[C@@H]2[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)O[C@@H](n3ccc(=O)[nH]c3=O)[C@@H]2O1 10.1021/jm701348d
44439752 91841 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 531 8 6 11 0.3 Cc1ccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2c1 10.1016/j.bmcl.2006.09.017
CHEMBL241319 91841 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 531 8 6 11 0.3 Cc1ccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2c1 10.1016/j.bmcl.2006.09.017
10929115 201683 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
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/jm901450d
CHEMBL606210 201683 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
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/jm901450d
10929115 201683 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) 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 7.8 pEC50 = 7.8 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) 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
57403613 71309 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 398 5 5 7 -0.6 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1-c1ccccc1 10.1016/j.bmc.2012.02.012
CHEMBL1957438 71309 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 398 5 5 7 -0.6 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1-c1ccccc1 10.1016/j.bmc.2012.02.012
52952395 61346 0 None 2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
53308961 62923 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
44457247 10334 0 None 85 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 904 16 8 21 -1.1 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](n4ccc(=O)[nH]c4=O)[C@@H]4OC(/C=C/c5ccccc5)O[C@H]34)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1021/jm701348d
CHEMBL1162157 10334 0 None 85 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 904 16 8 21 -1.1 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](n4ccc(=O)[nH]c4=O)[C@@H]4OC(/C=C/c5ccccc5)O[C@H]34)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1021/jm701348d
121487677 164468 1 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 498 9 6 13 -1.8 COc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1 10.1016/j.bmc.2017.11.043
CHEMBL4214093 164468 1 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 498 9 6 13 -1.8 COc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1 10.1016/j.bmc.2017.11.043
1734 3966 50 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44439765 145756 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 553 8 6 11 0.2 O=c1c2cc(F)c(F)cc2ccn1[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
CHEMBL391663 145756 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 553 8 6 11 0.2 O=c1c2cc(F)c(F)cc2ccn1[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
46890111 6752 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
1734 3966 50 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor in BEA cells (unknown origin)Agonist activity at P2Y2 receptor in BEA cells (unknown origin)
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.2017.11.043
3639 3966 50 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor in BEA cells (unknown origin)Agonist activity at P2Y2 receptor in BEA cells (unknown origin)
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.2017.11.043
6133 3966 50 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor in BEA cells (unknown origin)Agonist activity at P2Y2 receptor in BEA cells (unknown origin)
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.2017.11.043
CHEMBL336296 3966 50 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor in BEA cells (unknown origin)Agonist activity at P2Y2 receptor in BEA cells (unknown origin)
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.2017.11.043
DB04005 3966 50 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor in BEA cells (unknown origin)Agonist activity at P2Y2 receptor in BEA cells (unknown origin)
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.2017.11.043
13833909 192722 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
ChEMBL 322 4 5 7 -2.3 O=c1ccn([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmcl.2009.04.027
CHEMBL522015 192722 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
ChEMBL 322 4 5 7 -2.3 O=c1ccn([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmcl.2009.04.027
44585986 184328 0 None 3 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 3 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
146015339 3922 32 None -275 7 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -275 7 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -275 7 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -275 7 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -275 7 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
21706 117147 15 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL339385 117147 15 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
90656224 110914 0 None 2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
1734 3966 50 None 1 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
21706 117147 15 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL339385 117147 15 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
46830491 14189 4 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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
44586044 184298 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
90666798 109427 0 None -13 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -13 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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
440317 21748 17 None -3 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human N-terminal HA-tagged P2Y2 receptor expressed in 1321N1 cellsAgonist activity at human N-terminal HA-tagged P2Y2 receptor expressed in 1321N1 cells
ChEMBL 523 8 7 14 -1.5 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(O)(O)=S)[C@@H](O)[C@H]1O 10.1016/j.bmc.2017.11.043
CHEMBL131890 21748 17 None -3 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human N-terminal HA-tagged P2Y2 receptor expressed in 1321N1 cellsAgonist activity at human N-terminal HA-tagged P2Y2 receptor expressed in 1321N1 cells
ChEMBL 523 8 7 14 -1.5 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(O)(O)=S)[C@@H](O)[C@H]1O 10.1016/j.bmc.2017.11.043
440317 21748 17 None -3 4 Human 5.8 pEC50 = 5.8 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
ChEMBL 523 8 7 14 -1.5 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(O)(O)=S)[C@@H](O)[C@H]1O 10.1021/jm020046y
CHEMBL131890 21748 17 None -3 4 Human 5.8 pEC50 = 5.8 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
ChEMBL 523 8 7 14 -1.5 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(O)(O)=S)[C@@H](O)[C@H]1O 10.1021/jm020046y
44586005 184329 0 None 2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
44439749 91839 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 531 8 6 11 0.3 Cc1cn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)c2ccccc12 10.1016/j.bmcl.2006.09.017
CHEMBL241317 91839 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 531 8 6 11 0.3 Cc1cn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)c2ccccc12 10.1016/j.bmcl.2006.09.017
148197 1438 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1736 1438 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
4900 1438 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL221326 1438 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB15919 1438 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1713 520 68 None -9 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)
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 10.1016/j.bmc.2017.11.043
5957 520 68 None -9 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)
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 10.1016/j.bmc.2017.11.043
91 520 68 None -9 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)
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 10.1016/j.bmc.2017.11.043
CHEMBL14249 520 68 None -9 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)
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 10.1016/j.bmc.2017.11.043
DB00171 520 68 None -9 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin)
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 10.1016/j.bmc.2017.11.043
44420652 83437 2 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 525 9 7 13 -1.6 [N-]=[N+]=Nc1cn([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
CHEMBL219779 83437 2 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 525 9 7 13 -1.6 [N-]=[N+]=Nc1cn([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
52952183 61086 0 None 3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 637 10 7 12 0.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)Nc3ccccc3)[C@@H](O)[C@H]2O)cc1Br 10.1021/jm1016297
CHEMBL1765120 61086 0 None 3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 637 10 7 12 0.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)Nc3ccccc3)[C@@H](O)[C@H]2O)cc1Br 10.1021/jm1016297
52952603 61083 0 None 4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
1713 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
21706 117147 15 None 5 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL339385 117147 15 None 5 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
90656217 110907 0 None -2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
CHEMBL3261366 110907 0 None -2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
90656217 110907 0 None -2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 -2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
44586045 184148 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
44585516 172595 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
44420646 159814 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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 10.1021/jm060903o
CHEMBL410594 159814 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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 10.1021/jm060903o
44585514 180144 5 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
ChEMBL 640 12 7 15 -0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3ccccc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL474886 180144 5 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
ChEMBL 640 12 7 15 -0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3ccccc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
44585514 180144 5 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 640 12 7 15 -0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3ccccc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL474886 180144 5 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 640 12 7 15 -0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3ccccc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
53309380 62921 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
90656213 110903 0 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
CHEMBL3261362 110903 0 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
90656213 110903 0 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
73348762 89523 0 None -630 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 551 8 7 13 -0.3 Nc1nc(Cl)nc2c1ncn2C1C(O)C(O)[C@@]2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@@H]12 10.1021/jm010538v
CHEMBL2373323 89523 0 None -630 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 551 8 7 13 -0.3 Nc1nc(Cl)nc2c1ncn2C1C(O)C(O)[C@@]2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@@H]12 10.1021/jm010538v
44457276 10343 0 None 87 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 878 15 8 21 -1.4 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]4OC(c5ccccc5)O[C@@H]34)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1021/jm701348d
CHEMBL1162166 10343 0 None 87 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 878 15 8 21 -1.4 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]4OC(c5ccccc5)O[C@@H]34)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1021/jm701348d
73348763 89524 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 531 9 7 13 -0.5 CNc1ncnc2c1ncn2C1C(O)C(O)[C@@]2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@@H]12 10.1021/jm010538v
CHEMBL2373324 89524 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 531 9 7 13 -0.5 CNc1ncnc2c1ncn2C1C(O)C(O)[C@@]2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@@H]12 10.1021/jm010538v
1734 3966 50 None 1 7 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
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.2012.02.012
3639 3966 50 None 1 7 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
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.2012.02.012
6133 3966 50 None 1 7 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
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.2012.02.012
CHEMBL336296 3966 50 None 1 7 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
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.2012.02.012
DB04005 3966 50 None 1 7 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
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.2012.02.012
1737 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptorAgonist activity at P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptorAgonist activity at P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptorAgonist activity at P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptorAgonist activity at P2Y2 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
1713 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor in BEA cells (unknown origin)Agonist activity at P2Y2 receptor in BEA cells (unknown origin)
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 10.1016/j.bmc.2017.11.043
5957 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor in BEA cells (unknown origin)Agonist activity at P2Y2 receptor in BEA cells (unknown origin)
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 10.1016/j.bmc.2017.11.043
91 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor in BEA cells (unknown origin)Agonist activity at P2Y2 receptor in BEA cells (unknown origin)
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 10.1016/j.bmc.2017.11.043
CHEMBL14249 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor in BEA cells (unknown origin)Agonist activity at P2Y2 receptor in BEA cells (unknown origin)
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 10.1016/j.bmc.2017.11.043
DB00171 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor in BEA cells (unknown origin)Agonist activity at P2Y2 receptor in BEA cells (unknown origin)
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 10.1016/j.bmc.2017.11.043
1713 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor in human CF/T43 cellsAgonist activity at P2Y2 receptor in human CF/T43 cells
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 10.1016/j.bmc.2017.11.043
5957 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor in human CF/T43 cellsAgonist activity at P2Y2 receptor in human CF/T43 cells
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 10.1016/j.bmc.2017.11.043
91 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor in human CF/T43 cellsAgonist activity at P2Y2 receptor in human CF/T43 cells
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 10.1016/j.bmc.2017.11.043
CHEMBL14249 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor in human CF/T43 cellsAgonist activity at P2Y2 receptor in human CF/T43 cells
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 10.1016/j.bmc.2017.11.043
DB00171 520 68 None -9 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor in human CF/T43 cellsAgonist activity at P2Y2 receptor in human CF/T43 cells
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 10.1016/j.bmc.2017.11.043
44439818 145305 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 504 8 6 11 0.1 Cn1c([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)nc2ccccc21 10.1016/j.bmcl.2006.10.038
CHEMBL391318 145305 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 504 8 6 11 0.1 Cn1c([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)nc2ccccc21 10.1016/j.bmcl.2006.10.038
45104419 200884 2 None -2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 514 9 7 13 -2.5 COc1cn([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/jm901450d
CHEMBL601439 200884 2 None -2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 514 9 7 13 -2.5 COc1cn([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/jm901450d
10432343 199379 4 None 1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 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 P2Y2 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 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 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 P2Y2 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
1731 130 11 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 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 -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 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 -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 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
1734 3966 50 None 1 7 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1734 3966 50 None 1 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
148197 1438 23 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
57398422 71310 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 448 5 5 7 0.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1-c1ccc2ccccc2c1 10.1016/j.bmc.2012.02.012
CHEMBL1957439 71310 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 448 5 5 7 0.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1-c1ccc2ccccc2c1 10.1016/j.bmc.2012.02.012
46830492 6615 0 None -33 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -33 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
46831686 14201 0 None -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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
90656211 110901 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
148197 1438 23 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1736 1438 23 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
4900 1438 23 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL221326 1438 23 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB15919 1438 23 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
10303040 91968 0 None 190 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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
1731 130 11 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor (unknown origin)Agonist activity at P2Y2 receptor (unknown origin)
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 10.1016/j.bmc.2017.11.043
9872620 130 11 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor (unknown origin)Agonist activity at P2Y2 receptor (unknown origin)
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 10.1016/j.bmc.2017.11.043
CHEMBL384527 130 11 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at P2Y2 receptor (unknown origin)Agonist activity at P2Y2 receptor (unknown origin)
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 10.1016/j.bmc.2017.11.043
1737 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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 10.1021/jm901450d
9875516 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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 10.1021/jm901450d
CHEMBL507282 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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 10.1021/jm901450d
DB04983 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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 10.1021/jm901450d
44457390 10364 0 None -60 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptor
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/s0960-894x(00)00612-0
CHEMBL1162193 10364 0 None -60 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptor
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/s0960-894x(00)00612-0
44439748 91836 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 507 8 6 12 -0.4 O=c1c2occc2ccn1[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
CHEMBL241316 91836 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 507 8 6 12 -0.4 O=c1c2occc2ccn1[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
10234467 188455 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
ChEMBL 824 14 10 20 -3.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=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/jm101591j
CHEMBL502712 188455 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
ChEMBL 824 14 10 20 -3.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=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/jm101591j
10234467 188455 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 824 14 10 20 -3.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=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
CHEMBL502712 188455 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 824 14 10 20 -3.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=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
46830493 14194 0 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 566 10 6 13 -0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC3CCCCC3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083258 14194 0 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 566 10 6 13 -0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC3CCCCC3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1198837 14194 0 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 566 10 6 13 -0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC3CCCCC3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
1713 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at P2Y2 receptor (unknown origin)Agonist activity at P2Y2 receptor (unknown origin)
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 10.1016/j.bmc.2017.11.043
5957 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at P2Y2 receptor (unknown origin)Agonist activity at P2Y2 receptor (unknown origin)
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 10.1016/j.bmc.2017.11.043
91 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at P2Y2 receptor (unknown origin)Agonist activity at P2Y2 receptor (unknown origin)
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 10.1016/j.bmc.2017.11.043
CHEMBL14249 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at P2Y2 receptor (unknown origin)Agonist activity at P2Y2 receptor (unknown origin)
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 10.1016/j.bmc.2017.11.043
DB00171 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at P2Y2 receptor (unknown origin)Agonist activity at P2Y2 receptor (unknown origin)
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 10.1016/j.bmc.2017.11.043
1713 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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 -9 10 Human 6.6 pEC50 = 6.6 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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 -9 10 Human 6.6 pEC50 = 6.6 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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 -9 10 Human 6.6 pEC50 = 6.6 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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 -9 10 Human 6.6 pEC50 = 6.6 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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
162565 59 14 None -630 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 541 8 7 14 -1.0 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1nc(Cl)nc2N 10.1021/jm010538v
1716 59 14 None -630 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 541 8 7 14 -1.0 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1nc(Cl)nc2N 10.1021/jm010538v
CHEMBL1368696 59 14 None -630 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 541 8 7 14 -1.0 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1nc(Cl)nc2N 10.1021/jm010538v
148197 1438 23 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1736 1438 23 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
4900 1438 23 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL221326 1438 23 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB15919 1438 23 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1713 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1713 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1735 3967 3 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 500 8 7 12 -2.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=S)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
5311494 3967 3 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 500 8 7 12 -2.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=S)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
CHEMBL220200 3967 3 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 500 8 7 12 -2.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=S)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
44457439 10374 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 926 16 11 22 -1.7 O=C(Nc1ccc(F)cc1)Nc1ccn([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)n1 10.1021/jm701348d
CHEMBL1162203 10374 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 926 16 11 22 -1.7 O=C(Nc1ccc(F)cc1)Nc1ccn([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)n1 10.1021/jm701348d
CHEMBL2029010 209148 0 None -2 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 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
90666790 109422 0 None -131 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -131 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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
90666796 112637 0 None -281 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 1243 23 12 23 2.4 N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCC#Cc5cccc(CO/N=c6/ccn([C@@H]7O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]7O)c(=O)[nH]6)c5)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O 10.1039/c3md00132f
CHEMBL3220052 112637 0 None -281 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 1243 23 12 23 2.4 N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCC#Cc5cccc(CO/N=c6/ccn([C@@H]7O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]7O)c(=O)[nH]6)c5)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O 10.1039/c3md00132f
CHEMBL3302769 112637 0 None -281 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 1243 23 12 23 2.4 N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCC#Cc5cccc(CO/N=c6/ccn([C@@H]7O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]7O)c(=O)[nH]6)c5)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O 10.1039/c3md00132f
44585987 191802 0 None -2 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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/jm101591j
CHEMBL519835 191802 0 None -2 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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/jm101591j
44585987 191802 0 None -2 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
44585987 191802 0 None -2 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins 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/jm101591j
CHEMBL519835 191802 0 None -2 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins 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/jm101591j
CHEMBL2029009 209147 0 None -12 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 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](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC 10.1021/jm2013198
44439760 154458 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 547 9 6 12 -0.0 COc1ccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2c1 10.1016/j.bmcl.2006.09.017
CHEMBL399018 154458 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 547 9 6 12 -0.0 COc1ccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2c1 10.1016/j.bmcl.2006.09.017
1730 125 10 None -3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
189010 184231 12 None 1 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
145971893 164682 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 567 14 7 13 0.2 CCCCCCNc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1 10.1016/j.bmc.2017.11.043
CHEMBL4216941 164682 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 567 14 7 13 0.2 CCCCCCNc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1 10.1016/j.bmc.2017.11.043
53309528 62858 0 None -3 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
1737 1367 7 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
9875516 1367 7 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
CHEMBL507282 1367 7 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
DB04983 1367 7 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
44585514 180144 5 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 640 12 7 15 -0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3ccccc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL474886 180144 5 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 640 12 7 15 -0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3ccccc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
53309379 62919 0 None -4 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
46831692 14196 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 P2Y2 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 P2Y2 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 P2Y2 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 P2Y2 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 P2Y2 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 P2Y2 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
46831384 14199 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
90656222 110912 0 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
52952394 61345 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 354 5 4 9 -1.3 CSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767417 61345 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 354 5 4 9 -1.3 CSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
90666799 109428 0 None -3 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 639 11 6 14 0.8 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3ccc4ccccc4c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL3220055 109428 0 None -3 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 639 11 6 14 0.8 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3ccc4ccccc4c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
145967979 164766 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 511 9 6 13 -1.7 CN(C)c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1 10.1016/j.bmc.2017.11.043
CHEMBL4217962 164766 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 511 9 6 13 -1.7 CN(C)c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1 10.1016/j.bmc.2017.11.043
1713 520 68 None -9 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
90656210 110900 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
10169708 91971 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 525 8 6 11 0.9 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3cc(F)ccc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
CHEMBL241483 91971 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 525 8 6 11 0.9 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3cc(F)ccc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
16216480 166397 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 581 9 6 12 0.8 CSc1cc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2cc1F 10.1016/j.bmcl.2006.09.017
CHEMBL427685 166397 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 581 9 6 12 0.8 CSc1cc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2cc1F 10.1016/j.bmcl.2006.09.017
44439747 91125 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 523 8 6 12 0.0 O=c1c2ccsc2ccn1[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
CHEMBL239815 91125 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 523 8 6 12 0.0 O=c1c2ccsc2ccn1[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
9853990 188674 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 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
1713 520 68 None -9 10 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44585518 188209 0 None 6 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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
44585518 188209 0 None 6 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
45104417 200985 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 514 9 7 13 -2.5 COc1cc(=O)[nH]c(=O)n1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901450d
CHEMBL602071 200985 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 514 9 7 13 -2.5 COc1cc(=O)[nH]c(=O)n1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901450d
CHEMBL2029002 209140 0 None -38 2 Human 4.5 pEC50 = 4.5 Functional
Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increaseActivity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase
ChEMBL None None None BP(=O)(OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O)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.CCCCN(CCCC)CCCC 10.1021/jm050955y
44457262 10339 0 None 2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 966 16 6 21 1.3 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]4OC(c5ccccc5)O[C@H]34)[C@@H]3OC(c4ccccc4)O[C@@H]32)c(=O)[nH]1 10.1021/jm701348d
CHEMBL1162162 10339 0 None 2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 966 16 6 21 1.3 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]4OC(c5ccccc5)O[C@H]34)[C@@H]3OC(c4ccccc4)O[C@@H]32)c(=O)[nH]1 10.1021/jm701348d
44439743 147587 0 None 229 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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
145967007 164421 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 514 9 6 13 -1.1 CSc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1 10.1016/j.bmc.2017.11.043
CHEMBL4213573 164421 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 514 9 6 13 -1.1 CSc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1 10.1016/j.bmc.2017.11.043
57394894 71312 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 424 6 5 7 -0.1 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1/C=C/c1ccccc1 10.1016/j.bmc.2012.02.012
CHEMBL1957441 71312 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 424 6 5 7 -0.1 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1/C=C/c1ccccc1 10.1016/j.bmc.2012.02.012
90656216 110906 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
90656221 110911 0 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
90666793 109425 0 None -81 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -81 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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
44585517 188336 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
53309242 62928 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
21706 117147 15 None 5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL339385 117147 15 None 5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44457427 14857 0 None 6 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
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 10.1021/jm701348d
CHEMBL1207447 14857 0 None 6 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
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 10.1021/jm701348d
CHEMBL406266 14857 0 None 6 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
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 10.1021/jm701348d
90656212 110902 0 None -7 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 -7 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
44219765 188795 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
ChEMBL 388 5 6 9 -2.6 O=c1ccn([C@@H]2O[C@H](CP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmcl.2009.04.027
CHEMBL505857 188795 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
ChEMBL 388 5 6 9 -2.6 O=c1ccn([C@@H]2O[C@H](CP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmcl.2009.04.027
21706 117147 15 None 5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL339385 117147 15 None 5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1731 130 11 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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
44439751 91840 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 531 8 6 11 0.3 Cc1ccc2c(=O)n([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)ccc2c1 10.1016/j.bmcl.2006.09.017
CHEMBL241318 91840 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 531 8 6 11 0.3 Cc1ccc2c(=O)n([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)ccc2c1 10.1016/j.bmcl.2006.09.017
44439744 166772 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 518 8 6 12 -0.6 O=c1c2cccnc2ccn1[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
CHEMBL428387 166772 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 518 8 6 12 -0.6 O=c1c2cccnc2ccn1[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
10174453 90 5 None 17 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
44457249 10335 0 None 12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 1018 18 6 21 2.0 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]4OC(/C=C/c5ccccc5)O[C@H]34)[C@@H]3OC(/C=C/c4ccccc4)O[C@@H]32)c(=O)[nH]1 10.1021/jm701348d
CHEMBL1162158 10335 0 None 12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 1018 18 6 21 2.0 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]4OC(/C=C/c5ccccc5)O[C@H]34)[C@@H]3OC(/C=C/c4ccccc4)O[C@@H]32)c(=O)[nH]1 10.1021/jm701348d
90656215 110905 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
46831386 14234 0 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
11993891 82436 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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
44585521 173990 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
45485253 199027 0 None -7 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -7 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -7 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -7 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -7 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
23379800 80486 0 None -28 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 -28 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 7.4 pEC50 = 7.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6083 204815 95 None -1 7 Human 5.4 pEC50 = 5.4 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell
ChEMBL 347 4 5 10 -1.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm010369e
CHEMBL1315633 204815 95 None -1 7 Human 5.4 pEC50 = 5.4 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell
ChEMBL 347 4 5 10 -1.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm010369e
CHEMBL752 204815 95 None -1 7 Human 5.4 pEC50 = 5.4 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell
ChEMBL 347 4 5 10 -1.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm010369e
53309245 62918 0 None 1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
1741 1217 62 None -4 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 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 10.1016/j.bmc.2017.11.043
6176 1217 62 None -4 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 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 10.1016/j.bmc.2017.11.043
CHEMBL223533 1217 62 None -4 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 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 10.1016/j.bmc.2017.11.043
DB02431 1217 62 None -4 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 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 10.1016/j.bmc.2017.11.043
90666802 109430 0 None -4 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -4 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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
44439816 91224 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 505 8 6 11 0.6 Cc1ccc2oc([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)nc2c1 10.1016/j.bmcl.2006.10.038
CHEMBL240044 91224 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 505 8 6 11 0.6 Cc1ccc2oc([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)nc2c1 10.1016/j.bmcl.2006.10.038
189010 184231 12 None 1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
90666794 109426 0 None -38 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -38 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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
148197 1438 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1736 1438 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
4900 1438 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL221326 1438 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB15919 1438 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44586042 191896 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
44439766 90969 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 578 9 6 12 0.2 CN(C)c1cc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2cc1F 10.1016/j.bmcl.2006.09.017
CHEMBL239573 90969 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 578 9 6 12 0.2 CN(C)c1cc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2cc1F 10.1016/j.bmcl.2006.09.017
57384078 71311 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 416 5 5 7 -0.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1-c1ccc(F)cc1 10.1016/j.bmc.2012.02.012
CHEMBL1957440 71311 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 416 5 5 7 -0.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1-c1ccc(F)cc1 10.1016/j.bmc.2012.02.012
57394897 71591 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 332 4 5 6 -1.6 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(CCP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1016/j.bmc.2012.02.012
CHEMBL1957448 71591 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 332 4 5 6 -1.6 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(CCP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1016/j.bmc.2012.02.012
CHEMBL1963180 71591 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 332 4 5 6 -1.6 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(CCP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1016/j.bmc.2012.02.012
44586042 191896 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
44586043 184275 0 None -1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
148197 1438 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1736 1438 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
4900 1438 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL221326 1438 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB15919 1438 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44439812 90645 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 537 9 6 12 0.8 COc1ccc2nc([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)sc2c1 10.1016/j.bmcl.2006.10.038
CHEMBL238957 90645 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 537 9 6 12 0.8 COc1ccc2nc([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)sc2c1 10.1016/j.bmcl.2006.10.038
21706 117147 15 None 5 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL339385 117147 15 None 5 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1734 3966 50 None 1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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
44457414 10369 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 789 14 10 22 -3.9 Nc1ccn([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)n1 10.1021/jm701348d
CHEMBL1162198 10369 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 789 14 10 22 -3.9 Nc1ccn([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)n1 10.1021/jm701348d
1734 3966 50 None 1 7 Human 6.4 pEC50 = 6.4 Functional
Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increaseActivity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase
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/jm050955y
3639 3966 50 None 1 7 Human 6.4 pEC50 = 6.4 Functional
Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increaseActivity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase
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/jm050955y
6133 3966 50 None 1 7 Human 6.4 pEC50 = 6.4 Functional
Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increaseActivity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase
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/jm050955y
CHEMBL336296 3966 50 None 1 7 Human 6.4 pEC50 = 6.4 Functional
Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increaseActivity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase
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/jm050955y
DB04005 3966 50 None 1 7 Human 6.4 pEC50 = 6.4 Functional
Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increaseActivity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase
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/jm050955y
90656218 110908 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
90656219 110909 0 None -5 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
90656220 110910 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
CHEMBL3261369 110910 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
90656220 110910 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
44420650 84256 0 None 17 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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
451388 84231 6 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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
52952396 61347 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 382 7 4 9 -0.5 CCCSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767419 61347 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 382 7 4 9 -0.5 CCCSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
135973538 3710 33 None -15 10 Human 4.3 pEC50 = 4.3 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm020046y
1728 3710 33 None -15 10 Human 4.3 pEC50 = 4.3 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm020046y
2966 3710 33 None -15 10 Human 4.3 pEC50 = 4.3 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm020046y
4261196 3710 33 None -15 10 Human 4.3 pEC50 = 4.3 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm020046y
5361 3710 33 None -15 10 Human 4.3 pEC50 = 4.3 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm020046y
CHEMBL265502 3710 33 None -15 10 Human 4.3 pEC50 = 4.3 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm020046y
DB04786 3710 33 None -15 10 Human 4.3 pEC50 = 4.3 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm020046y
44585519 169986 0 None -1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
53309105 62927 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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)Oc3ccc([N+](=O)[O-])cc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784899 62927 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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)Oc3ccc([N+](=O)[O-])cc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
1734 3966 50 None 1 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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
53309381 62929 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
11606036 61084 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 518 8 7 11 -1.8 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(=O)[nH]1 10.1021/jm1016297
CHEMBL1765117 61084 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 518 8 7 11 -1.8 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(=O)[nH]1 10.1021/jm1016297
44439757 154452 0 None 707 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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
44439757 154452 0 None 707 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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.2006.10.038
CHEMBL399017 154452 0 None 707 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.3 pEC50 = 8.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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.2006.10.038
1734 3966 50 None 1 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
3639 3966 50 None 1 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
6133 3966 50 None 1 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
CHEMBL336296 3966 50 None 1 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
DB04005 3966 50 None 1 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
10174453 90 5 None 17 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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
46831692 14196 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
57384080 71315 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 404 5 5 8 -0.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1-c1cccs1 10.1016/j.bmc.2012.02.012
CHEMBL1957444 71315 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 404 5 5 8 -0.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1-c1cccs1 10.1016/j.bmc.2012.02.012
53309529 62859 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
54584406 62920 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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
13833909 192722 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 322 4 5 7 -2.3 O=c1ccn([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2012.02.012
CHEMBL522015 192722 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 322 4 5 7 -2.3 O=c1ccn([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2012.02.012
44457294 10347 0 None 125 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 938 16 8 25 0.2 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]3OC(Cc4ccccc4)O[C@H]23)[C@H](O)[C@@H]1O 10.1021/jm701348d
CHEMBL1162170 10347 0 None 125 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 938 16 8 25 0.2 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]3OC(Cc4ccccc4)O[C@H]23)[C@H](O)[C@@H]1O 10.1021/jm701348d
90666791 109423 0 None -165 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -165 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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
52952280 61338 0 None 2 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
44439755 91843 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 551 8 6 11 0.6 O=c1c2ccc(Cl)cc2ccn1[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
CHEMBL241321 91843 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 551 8 6 11 0.6 O=c1c2ccc(Cl)cc2ccn1[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
52952283 61341 0 None 4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 524 10 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(SCCc2ccccc2)n1 10.1021/jm1016297
CHEMBL1767413 61341 0 None 4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 524 10 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(SCCc2ccccc2)n1 10.1021/jm1016297
44457347 10356 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 891 16 8 22 -1.3 Nc1ccn([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]3OC(Cc4ccccc4)O[C@H]32)c(=O)n1 10.1021/jm701348d
CHEMBL1162183 10356 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 891 16 8 22 -1.3 Nc1ccn([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]3OC(Cc4ccccc4)O[C@H]32)c(=O)n1 10.1021/jm701348d
90656214 110904 0 None -5 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
44457338 10354 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 1056 20 10 25 -0.4 CNc1ccccc1C(=O)O[C@H]1[C@@H](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]2OC(=O)c2ccccc2NC)O[C@@H]1n1ccc(=O)[nH]c1=O 10.1021/jm701348d
CHEMBL1162181 10354 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 1056 20 10 25 -0.4 CNc1ccccc1C(=O)O[C@H]1[C@@H](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]2OC(=O)c2ccccc2NC)O[C@@H]1n1ccc(=O)[nH]c1=O 10.1021/jm701348d
44439745 91124 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 521 8 6 11 -0.3 O=c1c2c(ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O)CCCC2 10.1016/j.bmcl.2006.09.017
CHEMBL239814 91124 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 521 8 6 11 -0.3 O=c1c2c(ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O)CCCC2 10.1016/j.bmcl.2006.09.017
1734 3966 50 None 1 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
44439750 147590 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 531 8 6 11 0.3 Cc1cccc2c(=O)n([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)ccc12 10.1016/j.bmcl.2006.09.017
CHEMBL393102 147590 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 531 8 6 11 0.3 Cc1cccc2c(=O)n([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)ccc12 10.1016/j.bmcl.2006.09.017
10207117 83464 0 None -16 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 499 8 8 13 -2.9 Nc1cn([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
CHEMBL220011 83464 0 None -16 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 499 8 8 13 -2.9 Nc1cn([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
71459957 79198 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptor
ChEMBL 870 16 11 23 -4.1 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=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
CHEMBL2113401 79198 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptor
ChEMBL 870 16 11 23 -4.1 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=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
44417696 81155 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y2 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
44586027 184117 1 None 9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
148197 1438 23 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1736 1438 23 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
4900 1438 23 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL221326 1438 23 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB15919 1438 23 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
90656229 112807 0 None -2 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 -2 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 -2 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
44585515 180146 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 646 12 7 15 -0.0 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC3CCCCC3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL474887 180146 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 646 12 7 15 -0.0 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC3CCCCC3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
1734 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44439767 90301 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 565 9 6 12 0.1 COc1cc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2cc1F 10.1016/j.bmcl.2006.09.017
CHEMBL238542 90301 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 565 9 6 12 0.1 COc1cc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2cc1F 10.1016/j.bmcl.2006.09.017
148197 1438 23 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
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/jm2013198
1736 1438 23 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
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/jm2013198
4900 1438 23 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
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/jm2013198
CHEMBL221326 1438 23 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
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/jm2013198
DB15919 1438 23 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
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/jm2013198
1734 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
1734 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
44586025 184084 1 None 9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
10255482 61884 18 None -10 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation 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 5.2 pEC50 = 5.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation 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
52952392 61343 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 403 6 6 11 -2.3 Nc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767415 61343 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 403 6 6 11 -2.3 Nc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
11534074 61081 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 550 8 7 11 -1.3 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(=O)[nH]1 10.1021/jm1016297
CHEMBL1765114 61081 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 550 8 7 11 -1.3 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(=O)[nH]1 10.1021/jm1016297
11525909 141605 5 None 19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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
53309530 62860 0 None -2 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
53308272 62924 0 None -6 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -6 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -6 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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 -6 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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
52952282 61340 0 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
90666789 109421 0 None -158 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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\OCc2cccc(Br)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL3220046 109421 0 None -158 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y2 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 P2Y2 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\OCc2cccc(Br)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
1713 520 68 None -9 10 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1734 3966 50 None 1 7 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y2 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
4044 2665 3 None -26 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
CHEMBL2029005 209143 0 None -40 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL None None None BP(=O)(OP(=O)(O)OC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O)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
CHEMBL2029009 209147 0 None -12 2 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 2 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](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC 10.1021/jm2013198
44439763 90968 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 595 9 6 13 -0.6 CS(=O)(=O)c1ccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2c1 10.1016/j.bmcl.2006.09.017
CHEMBL239572 90968 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 595 9 6 13 -0.6 CS(=O)(=O)c1ccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c2c1 10.1016/j.bmcl.2006.09.017
16114624 137978 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 541 9 7 12 -1.0 CC(=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
CHEMBL376430 137978 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 541 9 7 12 -1.0 CC(=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
90656230 2666 0 None -2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 -2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 -2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
53308962 62925 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 674 12 7 15 0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3ccc(Cl)cc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784895 62925 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 674 12 7 15 0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3ccc(Cl)cc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
21706 117147 15 None 5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL339385 117147 15 None 5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44457247 10334 0 None 85 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 904 16 8 21 -1.1 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](n4ccc(=O)[nH]c4=O)[C@@H]4OC(/C=C/c5ccccc5)O[C@H]34)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1021/jm701348d
CHEMBL1162157 10334 0 None 85 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 904 16 8 21 -1.1 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](n4ccc(=O)[nH]c4=O)[C@@H]4OC(/C=C/c5ccccc5)O[C@H]34)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1021/jm701348d
44439746 147589 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 507 8 6 12 -0.4 O=c1c2ccoc2ccn1[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
CHEMBL393101 147589 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 507 8 6 12 -0.4 O=c1c2ccoc2ccn1[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
1734 3966 50 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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
10191162 147417 0 None 602 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 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
44586026 192591 1 None 4 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
1734 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
3639 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
6133 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
CHEMBL336296 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
DB04005 3966 50 None 1 7 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
44439814 91223 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 537 9 6 12 0.8 COc1cccc2sc([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)nc12 10.1016/j.bmcl.2006.10.038
CHEMBL240043 91223 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 537 9 6 12 0.8 COc1cccc2sc([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)nc12 10.1016/j.bmcl.2006.10.038
57384079 71314 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 388 5 5 8 -1.0 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1-c1ccco1 10.1016/j.bmc.2012.02.012
CHEMBL1957443 71314 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation countingAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
ChEMBL 388 5 5 8 -1.0 O=c1[nH]c(=O)n([C@@H]2O[C@H](CCP(=O)(O)O)[C@@H](O)[C@H]2O)cc1-c1ccco1 10.1016/j.bmc.2012.02.012
1730 125 10 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
3033941 125 10 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
CHEMBL1767409 125 10 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
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 10.1016/j.bmc.2017.11.043
53262904 62930 0 None -11 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
13455593 10372 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
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/jm701348d
CHEMBL1162201 10372 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
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/jm701348d
21706 117147 15 None 5 2 Human 6.1 pEC50 = 6.1 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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 Human 6.1 pEC50 = 6.1 Functional
Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)
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
1731 130 11 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
9872620 130 11 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
CHEMBL384527 130 11 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
52952393 61344 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 417 7 6 11 -1.9 CNc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767416 61344 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 417 7 6 11 -1.9 CNc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
44439754 91842 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 535 8 6 11 0.1 O=c1c2ccc(F)cc2ccn1[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
CHEMBL241320 91842 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 535 8 6 11 0.1 O=c1c2ccc(F)cc2ccn1[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
53309244 62917 0 None -4 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
44585523 181105 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 856 14 10 20 -2.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=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
CHEMBL476021 181105 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 856 14 10 20 -2.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=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
1734 3966 50 None 1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44585987 191802 0 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
16116566 2656 10 None 301 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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/jm101591j
1733 2656 10 None 301 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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/jm101591j
CHEMBL373780 2656 10 None 301 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2Agonist activity at human P2Y2
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/jm101591j
9916559 91970 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 541 8 6 11 1.5 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3ccc(Cl)cc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
CHEMBL241482 91970 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 541 8 6 11 1.5 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3ccc(Cl)cc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
16116566 2656 10 None 301 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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 10.1021/jm901450d
1733 2656 10 None 301 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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 10.1021/jm901450d
CHEMBL373780 2656 10 None 301 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM 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 10.1021/jm901450d
16116566 2656 10 None 301 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 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
10929115 201683 0 None 5 2 Human 8.1 pEC50 = 8.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) 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 8.1 pEC50 = 8.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) 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
24857827 189047 0 None 8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
46890063 14192 0 None 3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
108643 3215 6 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
9468 3215 6 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
CHEMBL1207381 3215 6 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
1734 3966 50 None 1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
3639 3966 50 None 1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
6133 3966 50 None 1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL336296 3966 50 None 1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB04005 3966 50 None 1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
15485121 14180 0 None 3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP productionAgonist activity at human recombinant P2Y2 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 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP productionAgonist activity at human recombinant P2Y2 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 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP productionAgonist activity at human recombinant P2Y2 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
21706 117147 15 None 5 2 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL339385 117147 15 None 5 2 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
53308826 62922 0 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
52952497 61082 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
9830339 83541 2 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 610 8 7 12 -1.9 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)cc1I 10.1021/jm060903o
CHEMBL220398 83541 2 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 610 8 7 12 -1.9 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)cc1I 10.1021/jm060903o
71721777 164807 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 584 14 6 13 0.9 CCCCCCSc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1 10.1016/j.bmc.2017.11.043
CHEMBL4218507 164807 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic methodAgonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method
ChEMBL 584 14 6 13 0.9 CCCCCCSc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1 10.1016/j.bmc.2017.11.043
53309102 62926 0 None 4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 674 12 7 15 0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3cccc(Cl)c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784896 62926 0 None 4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 674 12 7 15 0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3cccc(Cl)c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
73356385 89526 0 None -1380 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 565 9 7 13 0.1 CNc1nc(Cl)nc2c1ncn2C1C(O)C(O)[C@@]2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@@H]12 10.1021/jm010538v
CHEMBL2373377 89526 0 None -1380 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 565 9 7 13 0.1 CNc1nc(Cl)nc2c1ncn2C1C(O)C(O)[C@@]2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@@H]12 10.1021/jm010538v
71459956 79194 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptor
ChEMBL 1030 20 13 27 -3.8 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=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
CHEMBL2113398 79194 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptor
ChEMBL 1030 20 13 27 -3.8 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=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
44439753 144899 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 531 8 6 11 0.3 Cc1cccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c12 10.1016/j.bmcl.2006.09.017
CHEMBL391012 144899 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 531 8 6 11 0.3 Cc1cccc2ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)c12 10.1016/j.bmcl.2006.09.017
1713 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
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 10.1016/j.bmcl.2009.04.027
5957 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
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 10.1016/j.bmcl.2009.04.027
91 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
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 10.1016/j.bmcl.2009.04.027
CHEMBL14249 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
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 10.1016/j.bmcl.2009.04.027
DB00171 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
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 10.1016/j.bmcl.2009.04.027
1713 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
5957 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
91 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
CHEMBL14249 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
DB00171 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
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/jm060903o
1713 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
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/jm010538v
5957 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
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/jm010538v
91 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
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/jm010538v
CHEMBL14249 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
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/jm010538v
DB00171 520 68 None -9 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
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/jm010538v
10994891 78429 0 None 2 4 Human 7.1 pEC50 = 7.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell
ChEMBL 517 8 7 13 -1.0 Nc1ncnc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]12 10.1021/jm010369e
CHEMBL2111533 78429 0 None 2 4 Human 7.1 pEC50 = 7.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell
ChEMBL 517 8 7 13 -1.0 Nc1ncnc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]12 10.1021/jm010369e
6083 204815 95 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell
ChEMBL 347 4 5 10 -1.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm010369e
CHEMBL1315633 204815 95 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell
ChEMBL 347 4 5 10 -1.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm010369e
CHEMBL752 204815 95 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell
ChEMBL 347 4 5 10 -1.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm010369e
44219763 187368 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
ChEMBL 468 7 7 11 -2.4 O=c1ccn([C@@H]2O[C@H](CP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmcl.2009.04.027
CHEMBL493371 187368 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
ChEMBL 468 7 7 11 -2.4 O=c1ccn([C@@H]2O[C@H](CP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmcl.2009.04.027
44439756 91207 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 542 8 6 12 -0.2 N#Cc1ccc2c(=O)n([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)ccc2c1 10.1016/j.bmcl.2006.09.017
CHEMBL239991 91207 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 542 8 6 12 -0.2 N#Cc1ccc2c(=O)n([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)ccc2c1 10.1016/j.bmcl.2006.09.017
52952391 61342 0 None 1 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 1 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
44306835 102070 0 None -6 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 517 8 7 13 -1.0 Nc1ncnc2c1ncn2C1C(O)C(O)C2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)CC12 10.1021/jm010538v
CHEMBL302077 102070 0 None -6 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2
ChEMBL 517 8 7 13 -1.0 Nc1ncnc2c1ncn2C1C(O)C(O)C2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)CC12 10.1021/jm010538v
10994891 78429 0 None 2 4 Human 7.0 pEC50 = 7.0 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell
ChEMBL 517 8 7 13 -1.0 Nc1ncnc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]12 10.1021/jm010369e
CHEMBL2111533 78429 0 None 2 4 Human 7.0 pEC50 = 7.0 Functional
Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell
ChEMBL 517 8 7 13 -1.0 Nc1ncnc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]12 10.1021/jm010369e
44585988 184083 0 None 5 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 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
1734 3966 50 None 1 7 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
3639 3966 50 None 1 7 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
6133 3966 50 None 1 7 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
CHEMBL336296 3966 50 None 1 7 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
DB04005 3966 50 None 1 7 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
90656226 110916 0 None -19 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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 -19 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y2 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
44457290 10345 0 None 288 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 892 16 8 21 -1.6 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]4OC(Cc5ccccc5)O[C@@H]34)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1021/jm701348d
CHEMBL1162168 10345 0 None 288 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 892 16 8 21 -1.6 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]4OC(Cc5ccccc5)O[C@@H]34)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1021/jm701348d
148197 1438 23 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
1736 1438 23 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
4900 1438 23 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL221326 1438 23 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB15919 1438 23 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
44585519 169986 0 None -1 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 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
10098947 10340 0 None -3 4 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 546 8 7 12 0.3 O=C(Nc1ccccc1)Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm701348d
CHEMBL1162163 10340 0 None -3 4 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 546 8 7 12 0.3 O=C(Nc1ccccc1)Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm701348d
1713 520 68 None -9 10 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
5957 520 68 None -9 10 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
91 520 68 None -9 10 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
CHEMBL14249 520 68 None -9 10 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
DB00171 520 68 None -9 10 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium levelAgonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level
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/jm801442p
11534074 61081 0 None 2 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 550 8 7 11 -1.3 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(=O)[nH]1 10.1021/jm101591j
CHEMBL1765114 61081 0 None 2 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 550 8 7 11 -1.3 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(=O)[nH]1 10.1021/jm101591j
44457429 10373 0 None 309 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 844 16 8 21 -2.0 CCCC1O[C@@H]2[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)O[C@@H](n3ccc(=O)[nH]c3=O)[C@@H]2O1 10.1021/jm701348d
CHEMBL1162202 10373 0 None 309 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assayAgonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay
ChEMBL 844 16 8 21 -2.0 CCCC1O[C@@H]2[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)O[C@@H](n3ccc(=O)[nH]c3=O)[C@@H]2O1 10.1021/jm701348d
71459959 79262 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptor
ChEMBL 950 18 12 25 -4.0 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=O)(O)OP(=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
CHEMBL2113465 79262 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptor
ChEMBL 950 18 12 25 -4.0 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=O)(O)OP(=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
52952495 61349 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 338 5 4 9 -2.0 COc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767422 61349 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 338 5 4 9 -2.0 COc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
10577679 201611 0 None - 1 Mouse 4.0 pEC50 = 4 Functional
Agonist activity at mouse P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at mouse P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 512 9 7 12 -1.9 CCc1cn([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/jm901450d
CHEMBL605786 201611 0 None - 1 Mouse 4.0 pEC50 = 4 Functional
Agonist activity at mouse P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at mouse P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 512 9 7 12 -1.9 CCc1cn([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/jm901450d
1734 3966 50 None 1 7 Human 6.0 pEC50 = 6 Functional
Agonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
3639 3966 50 None 1 7 Human 6.0 pEC50 = 6 Functional
Agonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
6133 3966 50 None 1 7 Human 6.0 pEC50 = 6 Functional
Agonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
CHEMBL336296 3966 50 None 1 7 Human 6.0 pEC50 = 6 Functional
Agonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
DB04005 3966 50 None 1 7 Human 6.0 pEC50 = 6 Functional
Agonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assayAgonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence 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/acs.jmedchem.7b00854
44585522 188642 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 938 14 7 19 -1.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc(I)c(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@H]3OC(Cc4ccccc4)O[C@H]32)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL503256 188642 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 938 14 7 19 -1.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc(I)c(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@H]3OC(Cc4ccccc4)O[C@H]32)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
136677322 3296 24 None -112 9 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
1739 3296 24 None -112 9 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
656725 3296 24 None -112 9 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
CHEMBL1160031 3296 24 None -112 9 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
21130371 14887 0 None -2 4 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/jm1012193
CHEMBL1207842 14887 0 None -2 4 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/jm1012193
CHEMBL445413 14887 0 None -2 4 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/jm1012193
3018777 60250 6 None -2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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
25863 60262 56 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 636 6 5 12 3.5 Nc1c(S(=O)(=O)O)cc(Nc2ccc(S(=O)(=O)O)c(Nc3nc(Cl)nc(Cl)n3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1672104 60262 56 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 636 6 5 12 3.5 Nc1c(S(=O)(=O)O)cc(Nc2ccc(S(=O)(=O)O)c(Nc3nc(Cl)nc(Cl)n3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1741102 60262 56 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 636 6 5 12 3.5 Nc1c(S(=O)(=O)O)cc(Nc2ccc(S(=O)(=O)O)c(Nc3nc(Cl)nc(Cl)n3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
51050236 60263 0 None -2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 486 5 3 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Oc3ccccc3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1672101 60263 0 None -2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 486 5 3 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Oc3ccccc3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1741104 60263 0 None -2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 486 5 3 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Oc3ccccc3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
45141783 14964 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 494 3 3 6 5.3 Nc1c(S(=O)(=O)O)cc(Nc2ccc3cc4ccccc4cc3c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL1208533 14964 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 494 3 3 6 5.3 Nc1c(S(=O)(=O)O)cc(Nc2ccc3cc4ccccc4cc3c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL608559 14964 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 494 3 3 6 5.3 Nc1c(S(=O)(=O)O)cc(Nc2ccc3cc4ccccc4cc3c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
162646235 179515 0 None -2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 476 6 1 6 4.4 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(Br)c1 10.1016/j.ejmech.2019.111789
CHEMBL4741242 179515 0 None -2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 476 6 1 6 4.4 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(Br)c1 10.1016/j.ejmech.2019.111789
117530 14732 5 None -2 3 Mouse 5.0 pIC50 = 5 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1206282 14732 5 None -2 3 Mouse 5.0 pIC50 = 5 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL256864 14732 5 None -2 3 Mouse 5.0 pIC50 = 5 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
11451 3211 0 None -30 5 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -30 5 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -30 5 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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
136677322 3296 24 None -112 9 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
1739 3296 24 None -112 9 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
656725 3296 24 None -112 9 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
CHEMBL1160031 3296 24 None -112 9 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
22916 14725 22 None -3 6 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 -3 6 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 -3 6 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 -3 6 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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 -3 6 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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 -3 6 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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
22916 14725 22 None -3 6 Mouse 5.0 pIC50 = 5.0 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1206272 14725 22 None -3 6 Mouse 5.0 pIC50 = 5.0 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL256057 14725 22 None -3 6 Mouse 5.0 pIC50 = 5.0 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
108643 3215 6 None -3 3 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1016/j.bmcl.2007.10.082
9468 3215 6 None -3 3 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1016/j.bmcl.2007.10.082
CHEMBL1207381 3215 6 None -3 3 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1016/j.bmcl.2007.10.082
20363247 14753 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL1206420 14753 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL271881 14753 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
136677322 3296 24 None -112 9 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 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 -112 9 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 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 -112 9 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 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 -112 9 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 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
22936 14752 13 None -2 2 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 451 4 4 7 3.0 CC(=O)Nc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL1206417 14752 13 None -2 2 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 451 4 4 7 3.0 CC(=O)Nc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL271688 14752 13 None -2 2 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 451 4 4 7 3.0 CC(=O)Nc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
25125168 14918 0 None -1 3 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 4.9 pIC50 = 4.9 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 4.9 pIC50 = 4.9 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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
137630492 161077 0 None -32 4 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -32 4 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -32 4 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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
44456166 14836 0 None -5 3 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1016/j.bmcl.2007.10.082
CHEMBL1207392 14836 0 None -5 3 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1016/j.bmcl.2007.10.082
CHEMBL402239 14836 0 None -5 3 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1016/j.bmcl.2007.10.082
162652460 180424 0 None -9 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 392 5 1 5 3.9 Cc1cccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc(C#N)c3)cc2)c1 10.1016/j.ejmech.2019.111789
CHEMBL4752357 180424 0 None -9 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 392 5 1 5 3.9 Cc1cccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc(C#N)c3)cc2)c1 10.1016/j.ejmech.2019.111789
44456117 14841 0 None 1 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1207400 14841 0 None 1 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL403051 14841 0 None 1 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
1734 3966 50 None -12 7 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence assayAntagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence 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.2009.05.062
3639 3966 50 None -12 7 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence assayAntagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence 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.2009.05.062
6133 3966 50 None -12 7 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence assayAntagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence 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.2009.05.062
CHEMBL336296 3966 50 None -12 7 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence assayAntagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence 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.2009.05.062
DB04005 3966 50 None -12 7 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence assayAntagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence 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.2009.05.062
136677322 3296 24 None -112 9 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
1739 3296 24 None -112 9 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
656725 3296 24 None -112 9 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
CHEMBL1160031 3296 24 None -112 9 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
136677322 3296 24 None -112 9 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
1739 3296 24 None -112 9 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
656725 3296 24 None -112 9 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
CHEMBL1160031 3296 24 None -112 9 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
117530 14732 5 None -4 3 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1206282 14732 5 None -4 3 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL256864 14732 5 None -4 3 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
137630841 161113 0 None -269 5 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -269 5 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -269 5 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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
108643 3215 6 None -6 3 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1016/j.bmcl.2007.10.082
9468 3215 6 None -6 3 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1016/j.bmcl.2007.10.082
CHEMBL1207381 3215 6 None -6 3 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1016/j.bmcl.2007.10.082
44152335 14730 1 None -1 3 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
CHEMBL1206280 14730 1 None -1 3 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
CHEMBL256689 14730 1 None -1 3 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
44456117 14841 0 None -1 2 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1207400 14841 0 None -1 2 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL403051 14841 0 None -1 2 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
22916 14725 22 None -3 6 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -3 6 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -3 6 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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
108643 3215 6 None -3 3 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
9468 3215 6 None -3 3 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
CHEMBL1207381 3215 6 None -3 3 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
136677322 3296 24 None -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
1739 3296 24 None -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
656725 3296 24 None -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
CHEMBL1160031 3296 24 None -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
136677322 3296 24 None -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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 -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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 -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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 -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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
136677322 3296 24 None -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced 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 10.1016/j.bmcl.2007.10.082
1739 3296 24 None -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced 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 10.1016/j.bmcl.2007.10.082
656725 3296 24 None -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced 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 10.1016/j.bmcl.2007.10.082
CHEMBL1160031 3296 24 None -112 9 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced 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 10.1016/j.bmcl.2007.10.082
136677322 3296 24 None -112 9 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
1739 3296 24 None -112 9 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
656725 3296 24 None -112 9 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
CHEMBL1160031 3296 24 None -112 9 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
13782419 14751 2 None -6 3 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1206416 14751 2 None -6 3 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL271673 14751 2 None -6 3 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
108643 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
9468 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
CHEMBL1207381 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
108643 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
9468 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
CHEMBL1207381 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
108643 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
9468 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
CHEMBL1207381 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
21130371 14887 0 None -9 4 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
CHEMBL1207842 14887 0 None -9 4 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
CHEMBL445413 14887 0 None -9 4 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
108643 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
9468 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
CHEMBL1207381 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
44456161 14835 0 None -6 3 Mouse 4.6 pIC50 = 4.6 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1207391 14835 0 None -6 3 Mouse 4.6 pIC50 = 4.6 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL402238 14835 0 None -6 3 Mouse 4.6 pIC50 = 4.6 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
25123183 14936 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 632 7 5 13 2.9 COc1nc(Cl)nc(Nc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2S(=O)(=O)O)n1 10.1021/jm1012193
CHEMBL1208235 14936 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 632 7 5 13 2.9 COc1nc(Cl)nc(Nc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2S(=O)(=O)O)n1 10.1021/jm1012193
CHEMBL509572 14936 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 632 7 5 13 2.9 COc1nc(Cl)nc(Nc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2S(=O)(=O)O)n1 10.1021/jm1012193
53308119 60256 0 None -2 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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
25124484 14750 0 None -3 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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
108643 3215 6 None -3 3 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
9468 3215 6 None -3 3 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
CHEMBL1207381 3215 6 None -3 3 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
117532 14851 8 None -8 3 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL1207421 14851 8 None -8 3 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL404450 14851 8 None -8 3 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
108643 3215 6 None -3 3 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
9468 3215 6 None -3 3 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
CHEMBL1207381 3215 6 None -3 3 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
117532 14851 8 None -9 3 Mouse 4.6 pIC50 = 4.6 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL1207421 14851 8 None -9 3 Mouse 4.6 pIC50 = 4.6 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL404450 14851 8 None -9 3 Mouse 4.6 pIC50 = 4.6 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
45141594 14960 0 None -3 2 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 456 4 4 7 2.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(F)cc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL1208510 14960 0 None -3 2 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 456 4 4 7 2.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(F)cc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL590956 14960 0 None -3 2 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 456 4 4 7 2.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(F)cc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
53326685 60257 0 None -3 2 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 4.5 pIC50 = 4.5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 4.5 pIC50 = 4.5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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
25123180 14834 0 None -15 3 Mouse 4.5 pIC50 = 4.5 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1207384 14834 0 None -15 3 Mouse 4.5 pIC50 = 4.5 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL401859 14834 0 None -15 3 Mouse 4.5 pIC50 = 4.5 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
162647196 179658 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111789
CHEMBL4743246 179658 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111789
44152335 14730 1 None -2 3 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
CHEMBL1206280 14730 1 None -2 3 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
CHEMBL256689 14730 1 None -2 3 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
21130371 14887 0 None -2 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
CHEMBL1207842 14887 0 None -2 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
CHEMBL445413 14887 0 None -2 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1016/j.bmcl.2007.10.082
162653582 180551 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2019.111789
CHEMBL4753843 180551 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2019.111789
25124828 14931 0 None -2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 -2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 -2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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
129834484 182037 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 412 6 1 6 3.9 Cc1cccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc([N+](=O)[O-])c3)cc2)c1 10.1016/j.ejmech.2019.111789
CHEMBL4780920 182037 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 412 6 1 6 3.9 Cc1cccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc([N+](=O)[O-])c3)cc2)c1 10.1016/j.ejmech.2019.111789
108643 3215 6 None -3 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
9468 3215 6 None -3 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
CHEMBL1207381 3215 6 None -3 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/jm801442p
25123180 14834 0 None -2 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1207384 14834 0 None -2 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL401859 14834 0 None -2 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
106250 14916 6 None -1 4 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 5.3 pIC50 = 5.3 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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 5.3 pIC50 = 5.3 Functional
Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y2 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
106250 14916 6 None -1 4 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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
136677322 3296 24 None -199 9 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced 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 10.1016/j.bmcl.2007.10.082
1739 3296 24 None -199 9 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced 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 10.1016/j.bmcl.2007.10.082
656725 3296 24 None -199 9 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced 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 10.1016/j.bmcl.2007.10.082
CHEMBL1160031 3296 24 None -199 9 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced 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 10.1016/j.bmcl.2007.10.082
135973538 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm800175e
1728 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm800175e
2966 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm800175e
4261196 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm800175e
5361 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm800175e
CHEMBL265502 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm800175e
DB04786 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10.1021/jm800175e
13782419 14751 2 None -1 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1206416 14751 2 None -1 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL271673 14751 2 None -1 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
109055 14729 1 None -1 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1016/j.bmcl.2007.10.082
CHEMBL1206279 14729 1 None -1 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1016/j.bmcl.2007.10.082
CHEMBL256688 14729 1 None -1 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1016/j.bmcl.2007.10.082
162646518 179550 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 416 6 1 6 3.8 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(F)c1 10.1016/j.ejmech.2019.111789
CHEMBL4741688 179550 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 416 6 1 6 3.8 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(F)c1 10.1016/j.ejmech.2019.111789
22916 14725 22 None -3 6 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1206272 14725 22 None -3 6 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL256057 14725 22 None -3 6 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
54210200 460 24 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1016/j.ejmech.2019.111789
5907 460 24 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1016/j.ejmech.2019.111789
CHEMBL4082045 460 24 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1016/j.ejmech.2019.111789
162646428 179677 6 None -3 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccccc1Cl 10.1016/j.ejmech.2019.111789
CHEMBL4743510 179677 6 None -3 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccccc1Cl 10.1016/j.ejmech.2019.111789
22936 14752 13 None 2 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 451 4 4 7 3.0 CC(=O)Nc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL1206417 14752 13 None 2 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 451 4 4 7 3.0 CC(=O)Nc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL271688 14752 13 None 2 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 451 4 4 7 3.0 CC(=O)Nc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
137630586 161087 0 None -16 5 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -16 5 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -16 5 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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
25124826 14926 2 None 1 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y2 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
25124827 14853 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 439 4 3 8 2.9 Nc1c(S(=O)(=O)O)cc(Nc2cccc([N+](=O)[O-])c2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1207423 14853 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 439 4 3 8 2.9 Nc1c(S(=O)(=O)O)cc(Nc2cccc([N+](=O)[O-])c2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL404659 14853 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 439 4 3 8 2.9 Nc1c(S(=O)(=O)O)cc(Nc2cccc([N+](=O)[O-])c2)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
44456166 14836 0 None -3 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1016/j.bmcl.2007.10.082
CHEMBL1207392 14836 0 None -3 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1016/j.bmcl.2007.10.082
CHEMBL402239 14836 0 None -3 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1016/j.bmcl.2007.10.082
137630000 161030 0 None -36 5 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -36 5 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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 -36 5 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y2 receptor transfected in human 1321N1 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 P2Y2 receptor transfected in human 1321N1 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
109055 14729 1 None -2 3 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1016/j.bmcl.2007.10.082
CHEMBL1206279 14729 1 None -2 3 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1016/j.bmcl.2007.10.082
CHEMBL256688 14729 1 None -2 3 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1016/j.bmcl.2007.10.082
3018582 14737 6 None 1 3 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
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 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
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 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
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
20363247 14753 0 None 1 2 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL1206420 14753 0 None 1 2 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
CHEMBL271881 14753 0 None 1 2 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 438 5 3 7 3.4 CCOc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1016/j.bmcl.2007.10.082
45481634 197881 0 None - 1 Mouse 4.0 pIC50 = 4.0 Functional
Antagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence assayAntagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence assay
ChEMBL 408 9 5 8 -0.3 O=c1ccn(CCCCP(=O)(O)OP(=O)(O)OP(=O)(O)O)c(=O)[nH]1 10.1016/j.bmc.2009.05.062
CHEMBL572657 197881 0 None - 1 Mouse 4.0 pIC50 = 4.0 Functional
Antagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence assayAntagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence assay
ChEMBL 408 9 5 8 -0.3 O=c1ccn(CCCCP(=O)(O)OP(=O)(O)OP(=O)(O)O)c(=O)[nH]1 10.1016/j.bmc.2009.05.062
44456161 14835 0 None -2 3 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1207391 14835 0 None -2 3 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL402238 14835 0 None -2 3 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
136677322 3296 24 None -112 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
1739 3296 24 None -112 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
656725 3296 24 None -112 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
CHEMBL1160031 3296 24 None -112 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced 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/jm801442p
3018582 14737 6 None -1 3 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
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 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
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 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilizationAntagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
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
137630763 161105 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 758 9 7 11 3.4 O=c1[nH]c(=S)c(C2c3ccccc3CCc3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4086462 161105 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 758 9 7 11 3.4 O=c1[nH]c(=S)c(C2c3ccccc3CCc3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4117043 161105 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 758 9 7 11 3.4 O=c1[nH]c(=S)c(C2c3ccccc3CCc3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
22117190 159771 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 470 4 2 5 5.5 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)O)o2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
CHEMBL4105209 159771 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 470 4 2 5 5.5 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)O)o2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
137628891 160977 0 None - 0 Human 6.0 pKd = 6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 732 11 7 11 3.3 O=c1[nH]c(=S)c(C(c2ccccc2)c2ccccc2)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4061969 160977 0 None - 0 Human 6.0 pKd = 6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 732 11 7 11 3.3 O=c1[nH]c(=S)c(C(c2ccccc2)c2ccccc2)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4115998 160977 0 None - 0 Human 6.0 pKd = 6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 732 11 7 11 3.3 O=c1[nH]c(=S)c(C(c2ccccc2)c2ccccc2)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
137629685 161164 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 800 11 7 11 4.6 O=c1[nH]c(=S)c(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4090014 161164 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 800 11 7 11 4.6 O=c1[nH]c(=S)c(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4117478 161164 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 800 11 7 11 4.6 O=c1[nH]c(=S)c(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
22117224 156494 0 None - 0 Human 5.9 pKd = 5.9 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 442 4 2 5 4.9 O=C(O)c1ccc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)o1 10.1016/j.bmcl.2017.09.043
CHEMBL4067621 156494 0 None - 0 Human 5.9 pKd = 5.9 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 442 4 2 5 4.9 O=C(O)c1ccc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)o1 10.1016/j.bmcl.2017.09.043
54210200 460 24 None - 1 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1016/j.bmcl.2017.09.043
5907 460 24 None - 1 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1016/j.bmcl.2017.09.043
CHEMBL4082045 460 24 None - 1 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1016/j.bmcl.2017.09.043
137629841 161198 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 760 11 7 11 3.9 Cc1ccc(C(c2ccc(C)cc2)c2cn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]c2=S)cc1 10.1016/j.bmcl.2017.09.043
CHEMBL4084674 161198 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 760 11 7 11 3.9 Cc1ccc(C(c2ccc(C)cc2)c2cn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]c2=S)cc1 10.1016/j.bmcl.2017.09.043
CHEMBL4117735 161198 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 760 11 7 11 3.9 Cc1ccc(C(c2ccc(C)cc2)c2cn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]c2=S)cc1 10.1016/j.bmcl.2017.09.043
22117209 159012 0 None - 0 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 443 4 2 6 4.3 O=C(O)c1coc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)n1 10.1016/j.bmcl.2017.09.043
CHEMBL4096541 159012 0 None - 0 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 443 4 2 6 4.3 O=C(O)c1coc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)n1 10.1016/j.bmcl.2017.09.043
137640848 161205 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 868 11 7 11 5.9 O=c1[nH]c(=S)c(C(c2ccc(Cl)c(Cl)c2)c2ccc(Cl)c(Cl)c2)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4073600 161205 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 868 11 7 11 5.9 O=c1[nH]c(=S)c(C(c2ccc(Cl)c(Cl)c2)c2ccc(Cl)c(Cl)c2)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4117812 161205 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 868 11 7 11 5.9 O=c1[nH]c(=S)c(C(c2ccc(Cl)c(Cl)c2)c2ccc(Cl)c(Cl)c2)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
22117247 157608 0 None - 0 Human 6.7 pKd = 6.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 510 4 2 5 6.2 O=C(O)c1ccc(Cn2cc(C3c4ccc(Cl)cc4C=Cc4cc(Cl)ccc43)c(=S)[nH]c2=O)o1 10.1016/j.bmcl.2017.09.043
CHEMBL4080964 157608 0 None - 0 Human 6.7 pKd = 6.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 510 4 2 5 6.2 O=C(O)c1ccc(Cn2cc(C3c4ccc(Cl)cc4C=Cc4cc(Cl)ccc43)c(=S)[nH]c2=O)o1 10.1016/j.bmcl.2017.09.043
21250855 156504 0 None - 0 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 466 5 2 4 5.2 O=C(O)Cc1cccc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)c1 10.1016/j.bmcl.2017.09.043
CHEMBL4067715 156504 0 None - 0 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 466 5 2 4 5.2 O=C(O)Cc1cccc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)c1 10.1016/j.bmcl.2017.09.043
9804249 158277 0 None - 0 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 459 4 2 6 4.8 O=C(O)c1csc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)n1 10.1016/j.bmcl.2017.09.043
CHEMBL4088846 158277 0 None - 0 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 459 4 2 6 4.8 O=C(O)c1csc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)n1 10.1016/j.bmcl.2017.09.043
18394899 157417 1 None - 0 Human 4.7 pKd = 4.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 450 3 4 7 2.2 O=c1[nH]c(=S)c(C2c3ccccc3C=Cc3ccccc32)cn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4078610 157417 1 None - 0 Human 4.7 pKd = 4.7 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 450 3 4 7 2.2 O=c1[nH]c(=S)c(C2c3ccccc3C=Cc3ccccc32)cn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
53889506 158325 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 585 8 4 7 4.5 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)o2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
CHEMBL4089252 158325 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 585 8 4 7 4.5 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)o2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
22117231 157707 0 None - 0 Human 6.6 pKd = 6.6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 487 4 2 6 5.4 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2nc(C(=O)O)cs2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
CHEMBL4081909 157707 0 None - 0 Human 6.6 pKd = 6.6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 487 4 2 6 5.4 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2nc(C(=O)O)cs2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
22117220 156731 0 None - 0 Human 5.6 pKd = 5.6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 458 4 2 5 5.4 O=C(O)c1cc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)cs1 10.1016/j.bmcl.2017.09.043
CHEMBL4070330 156731 0 None - 0 Human 5.6 pKd = 5.6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 458 4 2 5 5.4 O=C(O)c1cc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)cs1 10.1016/j.bmcl.2017.09.043
54210053 158164 0 None - 0 Human 5.6 pKd = 5.6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 482 6 2 5 5.1 O=C(O)COc1cccc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)c1 10.1016/j.bmcl.2017.09.043
CHEMBL4087442 158164 0 None - 0 Human 5.6 pKd = 5.6 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 482 6 2 5 5.1 O=C(O)COc1cccc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)c1 10.1016/j.bmcl.2017.09.043
9832003 161227 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 756 9 7 11 3.8 O=c1[nH]c(=S)c(C2c3ccccc3C=Cc3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4066222 161227 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 756 9 7 11 3.8 O=c1[nH]c(=S)c(C2c3ccccc3C=Cc3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4117999 161227 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 756 9 7 11 3.8 O=c1[nH]c(=S)c(C2c3ccccc3C=Cc3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
22117245 156535 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 610 7 3 8 6.2 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)Nc3nc(CC(=O)O)cs3)o2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
CHEMBL4068069 156535 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 610 7 3 8 6.2 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)Nc3nc(CC(=O)O)cs3)o2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
20638645 159324 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 602 8 4 8 4.3 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2nc(C(=O)N[C@@H](CC(=O)O)C(=O)O)cs2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
CHEMBL4099908 159324 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 602 8 4 8 4.3 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2nc(C(=O)N[C@@H](CC(=O)O)C(=O)O)cs2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
54423501 158880 0 None - 0 Human 5.4 pKd = 5.4 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 452 4 2 4 5.3 O=C(O)c1cccc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)c1 10.1016/j.bmcl.2017.09.043
CHEMBL4095137 158880 0 None - 0 Human 5.4 pKd = 5.4 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 452 4 2 4 5.3 O=C(O)c1cccc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)c1 10.1016/j.bmcl.2017.09.043
18689756 159781 0 None - 0 Human 5.4 pKd = 5.4 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 453 4 2 5 4.7 O=C(O)c1cccc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)n1 10.1016/j.bmcl.2017.09.043
CHEMBL4105297 159781 0 None - 0 Human 5.4 pKd = 5.4 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 453 4 2 5 4.7 O=C(O)c1cccc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)n1 10.1016/j.bmcl.2017.09.043
22117287 157409 0 None - 0 Human 4.4 pKd = 4.4 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 443 4 2 6 3.4 O=C(O)c1csc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=O)[nH]c2=O)n1 10.1016/j.bmcl.2017.09.043
CHEMBL4078514 157409 0 None - 0 Human 4.4 pKd = 4.4 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 443 4 2 6 3.4 O=C(O)c1csc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=O)[nH]c2=O)n1 10.1016/j.bmcl.2017.09.043
137630470 161068 0 None - 0 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 746 9 7 12 3.4 O=c1[nH]c(=S)c(C2c3ccccc3Oc3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4065010 161068 0 None - 0 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 746 9 7 12 3.4 O=c1[nH]c(=S)c(C2c3ccccc3Oc3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4116657 161068 0 None - 0 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 746 9 7 12 3.4 O=c1[nH]c(=S)c(C2c3ccccc3Oc3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
53767718 157646 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 725 11 5 10 5.1 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)Nc3nc(CC(=O)N[C@@H](CC(=O)O)C(=O)O)cs3)o2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
CHEMBL4081384 157646 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 725 11 5 10 5.1 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)Nc3nc(CC(=O)N[C@@H](CC(=O)O)C(=O)O)cs3)o2)c(=O)[nH]c1=S 10.1016/j.bmcl.2017.09.043
137630562 161085 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 730 9 7 11 3.3 O=c1[nH]c(=S)c(C2c3ccccc3-c3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4094225 161085 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 730 9 7 11 3.3 O=c1[nH]c(=S)c(C2c3ccccc3-c3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
CHEMBL4116814 161085 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 730 9 7 11 3.3 O=c1[nH]c(=S)c(C2c3ccccc3-c3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2017.09.043
22117234 159102 0 None - 0 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 459 4 2 6 4.8 O=C(O)c1cnc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)s1 10.1016/j.bmcl.2017.09.043
CHEMBL4097505 159102 0 None - 0 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 459 4 2 6 4.8 O=C(O)c1cnc(Cn2cc(C3c4ccccc4C=Cc4ccccc43)c(=S)[nH]c2=O)s1 10.1016/j.bmcl.2017.09.043
137630093 161047 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 792 13 7 13 3.3 COc1ccc(C(c2ccc(OC)cc2)c2cn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]c2=S)cc1 10.1016/j.bmcl.2017.09.043
CHEMBL4063008 161047 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 792 13 7 13 3.3 COc1ccc(C(c2ccc(OC)cc2)c2cn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]c2=S)cc1 10.1016/j.bmcl.2017.09.043
CHEMBL4116515 161047 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assayAntagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
ChEMBL 792 13 7 13 3.3 COc1ccc(C(c2ccc(OC)cc2)c2cn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]c2=S)cc1 10.1016/j.bmcl.2017.09.043
1713 520 68 None -9 10 Human 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 -9 10 Human 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 -9 10 Human 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 -9 10 Human 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 -9 10 Human 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
148197 1438 23 None 1 3 Human 8.1 pEC50 = 8.1 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 8.1 pEC50 = 8.1 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 8.1 pEC50 = 8.1 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 8.1 pEC50 = 8.1 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 8.1 pEC50 = 8.1 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
1734 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 8.1 pEC50 = 8.1 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 8.1 pEC50 = 8.1 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 8.1 pEC50 = 8.1 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 8.1 pEC50 = 8.1 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
4043 2657 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 636 12 5 13 2.3 C[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(Oc2ccccc2)O)O)O)O)O[C@H]([C@@H]1C)n1ccc(=O)[nH]c1=O 18514530
73755072 2657 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 636 12 5 13 2.3 C[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(Oc2ccccc2)O)O)O)O)O[C@H]([C@@H]1C)n1ccc(=O)[nH]c1=O 18514530
1735 3967 3 None - 1 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 8 7 12 -2.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=S)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 8564228
5311494 3967 3 None - 1 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 8 7 12 -2.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=S)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 8564228
CHEMBL220200 3967 3 None - 1 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 8 7 12 -2.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=S)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 8564228
1738 461 0 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 1 1 5 4.2 Clc1ccc2c(c1)C=Cc1c(C2c2cn(C)c(=O)[nH]c2=S)ncs1 17302398
22003577 461 0 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 1 1 5 4.2 Clc1ccc2c(c1)C=Cc1c(C2c2cn(C)c(=O)[nH]c2=S)ncs1 17302398
1732 450 0 None -3 4 Human 6.1 pEC50 = 6.1 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 11711032
1732 450 0 None -3 4 Human 6.1 pEC50 = 6.1 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 1393282
25243905 450 0 None -3 4 Human 6.1 pEC50 = 6.1 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 11711032
25243905 450 0 None -3 4 Human 6.1 pEC50 = 6.1 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 1393282
1737 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 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 11206448
1737 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 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
1737 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 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 8825364
9875516 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 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 11206448
9875516 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 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 6.7 pEC50 = 6.7 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 8825364
CHEMBL507282 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 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 11206448
CHEMBL507282 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 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 6.7 pEC50 = 6.7 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 8825364
DB04983 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 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 11206448
DB04983 1367 7 None 2 3 Human 6.7 pEC50 = 6.7 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 6.7 pEC50 = 6.7 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 8825364
1713 520 68 None -9 10 Human 6.9 pEC50 = 6.9 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 11754592
1713 520 68 None -9 10 Human 6.9 pEC50 = 6.9 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 -9 10 Human 6.9 pEC50 = 6.9 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 8564228
5957 520 68 None -9 10 Human 6.9 pEC50 = 6.9 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 11754592
5957 520 68 None -9 10 Human 6.9 pEC50 = 6.9 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 -9 10 Human 6.9 pEC50 = 6.9 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 8564228
91 520 68 None -9 10 Human 6.9 pEC50 = 6.9 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 11754592
91 520 68 None -9 10 Human 6.9 pEC50 = 6.9 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 -9 10 Human 6.9 pEC50 = 6.9 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 8564228
CHEMBL14249 520 68 None -9 10 Human 6.9 pEC50 = 6.9 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 11754592
CHEMBL14249 520 68 None -9 10 Human 6.9 pEC50 = 6.9 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 -9 10 Human 6.9 pEC50 = 6.9 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 8564228
DB00171 520 68 None -9 10 Human 6.9 pEC50 = 6.9 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 11754592
DB00171 520 68 None -9 10 Human 6.9 pEC50 = 6.9 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 -9 10 Human 6.9 pEC50 = 6.9 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 8564228
52952605 3208 10 None 52 3 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17088057
52952605 3208 10 None 52 3 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17125260
52952605 3208 10 None 52 3 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 21417463
5902 3208 10 None 52 3 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17088057
5902 3208 10 None 52 3 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17125260
5902 3208 10 None 52 3 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 21417463
CHEMBL1765119 3208 10 None 52 3 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17088057
CHEMBL1765119 3208 10 None 52 3 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17125260
CHEMBL1765119 3208 10 None 52 3 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 21417463
148197 1438 23 None 1 3 Human 7.0 pEC50 = 7 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 11206448
1736 1438 23 None 1 3 Human 7.0 pEC50 = 7 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 11206448
4900 1438 23 None 1 3 Human 7.0 pEC50 = 7 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 11206448
CHEMBL221326 1438 23 None 1 3 Human 7.0 pEC50 = 7 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 11206448
DB15919 1438 23 None 1 3 Human 7.0 pEC50 = 7 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 11206448
10174453 90 5 None 17 3 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17125260
3398 90 5 None 17 3 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17125260
CHEMBL217803 90 5 None 17 3 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17125260
16116566 2656 10 None 301 2 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17302398
1733 2656 10 None 301 2 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17302398
CHEMBL373780 2656 10 None 301 2 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 17302398
1734 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 11754592
1734 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 8564228
3639 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 11754592
3639 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 8564228
6133 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 11754592
6133 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 8564228
CHEMBL336296 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 11754592
CHEMBL336296 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 8564228
DB04005 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 11754592
DB04005 3966 50 None 1 7 Human 8.1 pEC50 = 8.1 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 8564228
1731 130 11 None -1 3 Human 5.7 pEC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 8564228
9872620 130 11 None -1 3 Human 5.7 pEC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 8564228
CHEMBL384527 130 11 None -1 3 Human 5.7 pEC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 8564228
1730 125 10 None -3 2 Human 7.5 pEC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 16475938
3033941 125 10 None -3 2 Human 7.5 pEC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 16475938
CHEMBL1767409 125 10 None -3 2 Human 7.5 pEC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 16475938
135973538 3710 33 None -15 10 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O None
1728 3710 33 None -15 10 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O None
2966 3710 33 None -15 10 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O None
4261196 3710 33 None -15 10 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O None
5361 3710 33 None -15 10 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O None
CHEMBL265502 3710 33 None -15 10 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O None
DB04786 3710 33 None -15 10 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O None
135973538 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10401562
135973538 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 9154346
1728 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10401562
1728 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 9154346
2966 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10401562
2966 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 9154346
4261196 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10401562
4261196 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 9154346
5361 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10401562
5361 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 9154346
CHEMBL265502 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10401562
CHEMBL265502 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 9154346
DB04786 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 10401562
DB04786 3710 33 None -15 10 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 1296 16 12 17 6.7 O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O 9154346
108643 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 19419204
9468 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 19419204
CHEMBL1207381 3215 6 None -3 3 Human 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 19419204
136677322 3296 24 None -112 9 Human 6.0 pIC50 = 6 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 10401562
1739 3296 24 None -112 9 Human 6.0 pIC50 = 6 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 10401562
656725 3296 24 None -112 9 Human 6.0 pIC50 = 6 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 10401562
CHEMBL1160031 3296 24 None -112 9 Human 6.0 pIC50 = 6 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 10401562
54210200 460 24 None - 1 Human 6.0 pIC50 ~ 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 15231488
5907 460 24 None - 1 Human 6.0 pIC50 ~ 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 15231488
CHEMBL4082045 460 24 None - 1 Human 6.0 pIC50 ~ 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 15231488


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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
1734 3966 50 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human P2Y2 transfected in human 1321N1 cellsAgonist activity at human P2Y2 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 6.9 pEC50 = 6.9 Binding
Agonist activity at human P2Y2 transfected in human 1321N1 cellsAgonist activity at human P2Y2 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 6.9 pEC50 = 6.9 Binding
Agonist activity at human P2Y2 transfected in human 1321N1 cellsAgonist activity at human P2Y2 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 6.9 pEC50 = 6.9 Binding
Agonist activity at human P2Y2 transfected in human 1321N1 cellsAgonist activity at human P2Y2 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 6.9 pEC50 = 6.9 Binding
Agonist activity at human P2Y2 transfected in human 1321N1 cellsAgonist activity at human P2Y2 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
1737 1367 7 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human P2Y2Agonist activity at human P2Y2
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/acs.jmedchem.5b01972
9875516 1367 7 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human P2Y2Agonist activity at human P2Y2
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/acs.jmedchem.5b01972
CHEMBL507282 1367 7 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human P2Y2Agonist activity at human P2Y2
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/acs.jmedchem.5b01972
DB04983 1367 7 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human P2Y2Agonist activity at human P2Y2
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/acs.jmedchem.5b01972
1713 520 68 None - 2 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human P2Y2 transfected in human 1321N1 cellsAgonist activity at human P2Y2 transfected in human 1321N1 cells
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 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human P2Y2 transfected in human 1321N1 cellsAgonist activity at human P2Y2 transfected in human 1321N1 cells
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 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human P2Y2 transfected in human 1321N1 cellsAgonist activity at human P2Y2 transfected in human 1321N1 cells
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 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human P2Y2 transfected in human 1321N1 cellsAgonist activity at human P2Y2 transfected in human 1321N1 cells
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 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human P2Y2 transfected in human 1321N1 cellsAgonist activity at human P2Y2 transfected in human 1321N1 cells
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
90656231 110918 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells by functional assayAgonist activity at human P2Y2 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 6.4 pEC50 = 6.4 Binding
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells by functional assayAgonist activity at human P2Y2 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
68077 204688 97 None - 2 Mouse 4.9 pIC50 = 4.9 Binding
Antagonist activity at mouse P2Y2Antagonist activity at mouse P2Y2
ChEMBL 372 6 0 7 3.5 COc1ccc(-c2cc(=O)c3c(OC)c(OC)c(OC)c(OC)c3o2)cc1 10.1021/acs.jmedchem.5b01972
CHEMBL73930 204688 97 None - 2 Mouse 4.9 pIC50 = 4.9 Binding
Antagonist activity at mouse P2Y2Antagonist activity at mouse P2Y2
ChEMBL 372 6 0 7 3.5 COc1ccc(-c2cc(=O)c3c(OC)c(OC)c(OC)c(OC)c3o2)cc1 10.1021/acs.jmedchem.5b01972
145962035 161612 0 None - 1 Human 4.9 pKd = 4.9 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 776 11 4 9 5.8 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(C)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
CHEMBL4129692 161612 0 None - 1 Human 4.9 pKd = 4.9 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 776 11 4 9 5.8 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(C)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
145963055 161535 0 None - 1 Human 6.9 pKd = 6.9 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1241 24 7 18 8.6 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCNc1nc2c(s1)C=Cc1cc(Cl)ccc1C2c1cn(Cc2nc(C(=O)Nc3nnn[nH]3)cs2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4128532 161535 0 None - 1 Human 6.9 pKd = 6.9 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1241 24 7 18 8.6 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCNc1nc2c(s1)C=Cc1cc(Cl)ccc1C2c1cn(Cc2nc(C(=O)Nc3nnn[nH]3)cs2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
145962783 161438 0 None - 1 Human 5.8 pKd = 5.8 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1180 21 6 13 9.0 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCNC(=O)CCCCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(C=C4)Cc4ccc(-c6cccs6)n4[B-]5(F)F)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4127230 161438 0 None - 1 Human 5.8 pKd = 5.8 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1180 21 6 13 9.0 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCNC(=O)CCCCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(C=C4)Cc4ccc(-c6cccs6)n4[B-]5(F)F)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
145962823 161521 0 None - 1 Human 5.7 pKd = 5.7 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 889 17 5 10 6.4 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(C)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
CHEMBL4128318 161521 0 None - 1 Human 5.7 pKd = 5.7 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 889 17 5 10 6.4 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(C)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
145961060 161420 0 None - 1 Human 5.6 pKd = 5.6 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1065 15 5 12 8.8 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(=Cc6ccc(-c7cccs7)n6[B-]5(F)F)C=C4)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4126826 161420 0 None - 1 Human 5.6 pKd = 5.6 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1065 15 5 12 8.8 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(=Cc6ccc(-c7cccs7)n6[B-]5(F)F)C=C4)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
145962183 161498 0 None - 1 Human 6.5 pKd = 6.5 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 526 5 3 5 5.2 Cc1ccc2c(c1)CCc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)O)cc(C(=O)O)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4128024 161498 0 None - 1 Human 6.5 pKd = 6.5 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 526 5 3 5 5.2 Cc1ccc2c(c1)CCc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)O)cc(C(=O)O)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
145961793 161576 0 None - 1 Human 5.4 pKd = 5.4 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 977 23 5 12 6.5 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCOCCOCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(C)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
CHEMBL4129129 161576 0 None - 1 Human 5.4 pKd = 5.4 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 977 23 5 12 6.5 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCOCCOCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(C)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
145961053 161408 0 None - 1 Human 6.3 pKd = 6.3 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1185 23 7 16 8.0 Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(CCC(=O)NCCCCCC(=O)NCCNC(=O)CCNc4nc5c(s4)C=Cc4cc(Cl)ccc4C5c4cn(Cc5nc(C(=O)Nc6nnn[nH]6)cs5)c(=O)[nH]c4=S)cc3)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
CHEMBL4126655 161408 0 None - 1 Human 6.3 pKd = 6.3 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1185 23 7 16 8.0 Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(CCC(=O)NCCCCCC(=O)NCCNC(=O)CCNc4nc5c(s4)C=Cc4cc(Cl)ccc4C5c4cn(Cc5nc(C(=O)Nc6nnn[nH]6)cs5)c(=O)[nH]c4=S)cc3)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
145961148 161586 0 None - 1 Human 5.3 pKd = 5.3 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1137 26 5 14 8.5 Cn1cc(C2c3ccc(Cl)cc3C=Cc3sc(NCCC(=O)NCCOCCOCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(C=C5)Cc5ccc(-c7cccs7)n5[B-]6(F)F)cc4)nc32)c(=S)[nH]c1=O 10.1021/acs.jmedchem.8b00139
CHEMBL4129299 161586 0 None - 1 Human 5.3 pKd = 5.3 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1137 26 5 14 8.5 Cn1cc(C2c3ccc(Cl)cc3C=Cc3sc(NCCC(=O)NCCOCCOCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(C=C5)Cc5ccc(-c7cccs7)n5[B-]6(F)F)cc4)nc32)c(=S)[nH]c1=O 10.1021/acs.jmedchem.8b00139
145962951 161346 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1153 21 5 14 8.8 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCOCCOCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(=Cc6ccc(-c7cccs7)n6[B-]5(F)F)C=C4)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4125853 161346 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1153 21 5 14 8.8 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCOCCOCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(=Cc6ccc(-c7cccs7)n6[B-]5(F)F)C=C4)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
145961026 161353 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1268 27 6 15 9.0 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCOCCOCCNC(=O)CCCCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(C=C4)Cc4ccc(-c6cccs6)n4[B-]5(F)F)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4125987 161353 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1268 27 6 15 9.0 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCOCCOCCNC(=O)CCCCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(C=C4)Cc4ccc(-c6cccs6)n4[B-]5(F)F)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
145960452 161490 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 970 15 6 15 5.5 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(Cc4nc(C(=O)Nc5nnn[nH]5)cs4)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
CHEMBL4127889 161490 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 970 15 6 15 5.5 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(Cc4nc(C(=O)Nc5nnn[nH]5)cs4)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
145962507 161342 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1128 18 6 17 7.9 O=C(CCNc1nc2c(s1)C=Cc1cc(Cl)ccc1C2c1cn(Cc2nc(C(=O)Nc3nnn[nH]3)cs2)c(=O)[nH]c1=S)NCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1021/acs.jmedchem.8b00139
CHEMBL4125833 161342 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assayBinding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
ChEMBL 1128 18 6 17 7.9 O=C(CCNc1nc2c(s1)C=Cc1cc(Cl)ccc1C2c1cn(Cc2nc(C(=O)Nc3nnn[nH]3)cs2)c(=O)[nH]c1=S)NCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1021/acs.jmedchem.8b00139
145962594 161506 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 554 5 3 9 4.5 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2nc(C(=O)Nc3nnn[nH]3)cs2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4128126 161506 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 554 5 3 9 4.5 Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2nc(C(=O)Nc3nnn[nH]3)cs2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
145962183 161498 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 526 5 3 5 5.2 Cc1ccc2c(c1)CCc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)O)cc(C(=O)O)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4128024 161498 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 526 5 3 5 5.2 Cc1ccc2c(c1)CCc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)O)cc(C(=O)O)c2)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
88151531 161493 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 387 1 1 5 4.5 Cc1nc2c(s1)C=Cc1cc(Cl)ccc1C2c1cn(C)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4127983 161493 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 387 1 1 5 4.5 Cc1nc2c(s1)C=Cc1cc(Cl)ccc1C2c1cn(C)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
54210200 460 24 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(2-(4-(2-(5,5-difluoro-7-(thiophen-2-yl)-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-vinyl)phenoxy)acetamido)hexanamido)ethyl)amino)-3-oxopropyl)-amino)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)-thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(2-(4-(2-(5,5-difluoro-7-(thiophen-2-yl)-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-vinyl)phenoxy)acetamido)hexanamido)ethyl)amino)-3-oxopropyl)-amino)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)-thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
5907 460 24 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(2-(4-(2-(5,5-difluoro-7-(thiophen-2-yl)-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-vinyl)phenoxy)acetamido)hexanamido)ethyl)amino)-3-oxopropyl)-amino)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)-thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(2-(4-(2-(5,5-difluoro-7-(thiophen-2-yl)-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-vinyl)phenoxy)acetamido)hexanamido)ethyl)amino)-3-oxopropyl)-amino)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)-thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
CHEMBL4082045 460 24 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(2-(4-(2-(5,5-difluoro-7-(thiophen-2-yl)-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-vinyl)phenoxy)acetamido)hexanamido)ethyl)amino)-3-oxopropyl)-amino)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)-thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(2-(4-(2-(5,5-difluoro-7-(thiophen-2-yl)-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-vinyl)phenoxy)acetamido)hexanamido)ethyl)amino)-3-oxopropyl)-amino)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)-thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
68530100 87463 0 None -134 3 Human 5.6 pKi = 5.6 Binding
Inhibition of human P2Y2 receptorInhibition of human P2Y2 receptor
ChEMBL 391 4 2 3 6.5 Cc1ccc(NC(=O)Nc2cccnc2Sc2ccccc2C(C)(C)C)cc1 10.1021/jm301708u
CHEMBL2333767 87463 0 None -134 3 Human 5.6 pKi = 5.6 Binding
Inhibition of human P2Y2 receptorInhibition of human P2Y2 receptor
ChEMBL 391 4 2 3 6.5 Cc1ccc(NC(=O)Nc2cccnc2Sc2ccccc2C(C)(C)C)cc1 10.1021/jm301708u
145962191 161513 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 460 6 2 7 4.7 CCOCCNc1nc2c(s1)C=Cc1cc(Cl)ccc1[C@H]2c1cn(C)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4128208 161513 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 460 6 2 7 4.7 CCOCCNc1nc2c(s1)C=Cc1cc(Cl)ccc1[C@H]2c1cn(C)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
1735 3967 3 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 500 8 7 12 -2.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=S)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.8b00139
5311494 3967 3 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 500 8 7 12 -2.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=S)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.8b00139
CHEMBL220200 3967 3 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 500 8 7 12 -2.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=S)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.8b00139
54210200 460 24 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of N-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)-amino)propanamido)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lamba4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of N-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)-amino)propanamido)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lamba4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
5907 460 24 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of N-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)-amino)propanamido)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lamba4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of N-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)-amino)propanamido)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lamba4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
CHEMBL4082045 460 24 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of N-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)-amino)propanamido)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lamba4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of N-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)-amino)propanamido)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lamba4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
145962823 161521 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 889 17 5 10 6.4 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(C)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
CHEMBL4128318 161521 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 889 17 5 10 6.4 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(C)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.8b00139
54210200 460 24 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
5907 460 24 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
CHEMBL4082045 460 24 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
54210200 460 24 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of N-(2-(2-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)amino)propanamido)ethoxy)ethoxy)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of N-(2-(2-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)amino)propanamido)ethoxy)ethoxy)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
5907 460 24 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of N-(2-(2-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)amino)propanamido)ethoxy)ethoxy)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of N-(2-(2-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)amino)propanamido)ethoxy)ethoxy)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
CHEMBL4082045 460 24 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of N-(2-(2-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)amino)propanamido)ethoxy)ethoxy)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of N-(2-(2-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)amino)propanamido)ethoxy)ethoxy)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 537 5 3 8 4.6 Cc1ccc2c(c1)C=Cc1c(C2c2cn(Cc3ccc(o3)C(=O)Nc3nnn[nH]3)c(=O)[nH]c2=S)ccc(c1)C 10.1021/acs.jmedchem.8b00139
145963427 161501 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 460 6 2 7 4.7 CCOCCNc1nc2c(s1)C=Cc1cc(Cl)ccc1[C@@H]2c1cn(C)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
CHEMBL4128059 161501 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 460 6 2 7 4.7 CCOCCNc1nc2c(s1)C=Cc1cc(Cl)ccc1[C@@H]2c1cn(C)c(=O)[nH]c1=S 10.1021/acs.jmedchem.8b00139
11510273 87467 0 None -407 3 Human 5.2 pKi = 5.2 Binding
Inhibition of human P2Y2 receptorInhibition of human P2Y2 receptor
ChEMBL 431 6 2 4 6.5 CC(C)c1ccccc1Oc1ncccc1NC(=O)Nc1ccc(OC(F)(F)F)cc1 10.1021/jm301708u
CHEMBL2333773 87467 0 None -407 3 Human 5.2 pKi = 5.2 Binding
Inhibition of human P2Y2 receptorInhibition of human P2Y2 receptor
ChEMBL 431 6 2 4 6.5 CC(C)c1ccccc1Oc1ncccc1NC(=O)Nc1ccc(OC(F)(F)F)cc1 10.1021/jm301708u
137630763 161105 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 758 9 7 11 3.4 O=c1[nH]c(=S)c(C2c3ccccc3CCc3ccccc32)cn1[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/acs.jmedchem.8b00139
CHEMBL4086462 161105 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 758 9 7 11 3.4 O=c1[nH]c(=S)c(C2c3ccccc3CCc3ccccc32)cn1[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/acs.jmedchem.8b00139
CHEMBL4117043 161105 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assayDisplacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
ChEMBL 758 9 7 11 3.4 O=c1[nH]c(=S)c(C2c3ccccc3CCc3ccccc32)cn1[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/acs.jmedchem.8b00139