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 98045 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 98045 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 152081 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 152081 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 10738 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 10738 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 10738 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 10738 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 10738 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 8220 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 8220 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 8220 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 8220 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 8220 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 10738 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 10738 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 10738 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 10738 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 10738 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 21629 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 21629 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 21629 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 7308 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 7308 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 7308 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 7308 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 7308 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 78088 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 78088 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 200042 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 200042 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 10697 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 10697 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 10697 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 10697 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 170408 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 170408 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 117690 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 117690 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 117690 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 117690 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 10738 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 10738 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 10738 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 10738 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 10738 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 143727 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 143727 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 170719 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 170719 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 117694 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 117694 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 10738 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 10738 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 10738 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 10738 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 10738 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 7308 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 7308 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 7308 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 7308 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 7308 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 8220 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 8220 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 8220 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 8220 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 8220 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 7308 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 7308 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 7308 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 7308 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 7308 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 98046 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 98046 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 7308 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 7308 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 7308 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 7308 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 7308 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 10738 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 10738 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 10738 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 10738 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 10738 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 67859 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 67859 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 68113 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 68113 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 9671 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 9671 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 9671 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 10738 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 10738 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 10738 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 10738 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 10738 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 123925 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 123925 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 155154 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 155154 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 10738 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 10738 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 10738 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 10738 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 10738 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 17131 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 17131 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 68122 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 68122 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 8220 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 8220 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 8220 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 8220 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 8220 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 97490 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 97490 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 97490 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 97490 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 97490 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 97490 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 9982 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 9982 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 9982 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 17136 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 17136 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 10738 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 10738 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 10738 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 10738 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 10738 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 117692 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 117692 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 117692 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 117692 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 17109 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 17109 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 17110 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 17110 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 98050 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 98050 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 8149 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 8149 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 8149 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 8149 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 191141 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 191141 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 195538 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 195538 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 10738 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 10738 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 10738 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 10738 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 10738 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 194146 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 194146 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 90285 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 90285 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 8220 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 8220 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 8220 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 8220 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 8220 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 123925 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 123925 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 199374 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 199374 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 17114 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 17114 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 17137 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 17137 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 98616 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 98616 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 208462 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 208462 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 208462 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 208462 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 78084 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 78084 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 68120 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 68120 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 69697 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 69697 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 17106 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 17106 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 171247 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 171247 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 10738 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 10738 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 10738 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 10738 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 10738 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 152534 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 152534 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 13524 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 13524 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 10738 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 10738 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 10738 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 10738 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 10738 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 199501 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 199501 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 191107 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 191107 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 10694 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 10694 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 10694 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 10694 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 10694 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 123925 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 123925 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 117691 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 117691 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 10738 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 10738 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 10738 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 10738 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 10738 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 123925 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 123925 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 20961 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 20961 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 20961 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 20961 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 20961 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 20961 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 20961 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 20961 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 191077 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 191077 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 191077 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 191077 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 116204 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 116204 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 28520 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 28520 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 28520 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 28520 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 191108 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 191108 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 98614 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 98614 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 8220 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 8220 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 8220 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 8220 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 8220 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 7308 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 7308 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 7308 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 7308 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 7308 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 90212 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 90212 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 67860 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 67860 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 67857 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 67857 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 7308 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 7308 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 7308 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 7308 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 7308 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 123925 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 123925 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 117684 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 117684 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 117684 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 117684 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 190927 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 190927 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 179374 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 179374 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 166593 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 166593 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 186923 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 186923 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 186923 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 186923 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 69695 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 69695 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 117680 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 117680 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 117680 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 117680 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 96298 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 96298 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 17115 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 17115 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 96299 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 96299 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 10738 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 10738 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 10738 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 10738 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 10738 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 8149 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 8149 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 8149 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 8149 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 152083 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 152083 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 207663 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 207663 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 206158 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 206158 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 6918 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 6918 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 6918 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 8220 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 78085 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 78085 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 13387 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 13387 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 20973 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 20973 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 20973 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 20973 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 20973 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 20973 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 20973 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 20973 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 117678 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 117678 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 8220 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 8220 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 8220 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 8220 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 8220 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 98743 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 98743 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 6918 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 6918 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 6918 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 8149 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 8149 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 8149 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 8149 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 17136 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 17136 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 98611 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 98611 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 195234 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 195234 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 195234 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 195234 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 20966 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 20966 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 20966 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 6847 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 6847 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 6847 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 8220 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 8220 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 8220 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 8220 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 8220 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 10739 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 10739 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 10739 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 17146 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 17146 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 215927 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 116199 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 116199 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 119414 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 119414 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 119414 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 198581 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 198581 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 198581 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 198581 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 198581 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 198581 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 215926 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 161237 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 161237 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 6913 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 6913 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 6913 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 191010 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 191010 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 171461 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 171461 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 69632 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 69632 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 8149 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 8149 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 8149 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 8149 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 186923 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 186923 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 69693 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 69693 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 20968 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 20968 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 20968 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 20968 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 20968 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 20968 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 20971 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 20971 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 20971 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 117689 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 117689 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 68119 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 68119 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 116205 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 116205 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 171545 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 171545 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 7308 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 7308 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 7308 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 7308 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 7308 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 117677 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 117677 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 98746 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 98746 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 173176 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 173176 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 97900 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 97900 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 195453 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 195453 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 10738 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 10738 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 10738 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 10738 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 10738 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 7308 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 7308 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 7308 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 7308 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 7308 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 194988 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 194988 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 194988 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 194988 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 194988 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 194988 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 207764 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 207764 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 215919 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 17111 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 17111 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 154365 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 154365 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 171200 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 171200 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 78087 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 78087 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 117683 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 117683 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 117688 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 117688 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 116202 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 116202 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 195115 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 195115 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 69702 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 69702 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 123925 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 123925 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 21629 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 21629 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 21629 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 117679 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 117679 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 195574 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 195574 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 123925 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 123925 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 6918 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 6918 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 6918 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 98615 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 98615 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 173551 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 173551 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 6878 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 6878 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 6878 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 6878 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 6878 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 6878 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 6878 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 6878 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 6878 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 17107 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 17107 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 117682 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 117682 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 21006 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 21006 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 21006 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 89211 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 89211 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 180769 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 180769 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 205806 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 205806 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 205806 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 205806 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 205806 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 87261 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 87261 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 10738 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 10738 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 10738 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 10738 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 10738 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 211594 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 211594 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 211594 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 69692 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 69692 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 8000 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 8000 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 8000 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 8000 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 116207 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 116207 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 97999 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 97999 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 191010 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 191010 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 116203 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 116203 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 8220 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 8220 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 8220 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 8220 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 8220 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 198675 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 198675 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 97744 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 97744 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 78086 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 78086 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 78366 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 78366 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 78366 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 198675 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 198675 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 191054 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 191054 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 8220 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 8220 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 8220 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 8220 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 8220 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 97420 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 97420 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 123925 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 123925 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 10738 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 10738 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 10738 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 10738 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 10738 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 17141 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 17141 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 10738 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 10738 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 10738 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 10738 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 10738 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 117685 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 117685 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 117686 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 117686 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 117687 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 117687 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 117687 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 117687 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 91031 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 91031 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 91006 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 91006 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 68121 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 68121 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 176765 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 176765 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 69701 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 69701 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 10738 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 10738 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 10738 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 10738 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 10738 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 69703 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 69703 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 67858 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 67858 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 161231 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 161231 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 161231 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 161231 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 10738 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 10738 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 10738 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 10738 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 10738 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 6878 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 6878 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 6878 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 20968 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 20968 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 20968 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 10738 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 10738 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 10738 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 10738 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 10738 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 78090 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 78090 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 69633 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 69633 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 69694 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 69694 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 199501 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 199501 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 17119 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 17119 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 116200 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 116200 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 68112 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 68112 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 98618 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 98618 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 68115 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 68115 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 17128 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 17128 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 117681 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 117681 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 17126 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 17126 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 97899 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 97899 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 10738 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 10738 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 10738 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 10738 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 10738 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 154368 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 154368 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 90239 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 90239 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 85973 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 85973 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 87930 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 87930 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 190896 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 190896 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 8220 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 8220 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 8220 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 8220 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 8220 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 119584 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 119584 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 119584 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 186925 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 186925 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 10738 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 10738 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 10738 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 10738 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 10738 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 97076 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 97076 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 8220 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 8220 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 8220 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 8220 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 8220 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 190863 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 190863 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 68658 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 68658 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 68117 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 68117 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 67855 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 67855 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 148383 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 148383 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 148383 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 148383 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 69634 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 69634 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 69698 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 69698 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 69698 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 69698 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 68114 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 68114 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 116198 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 116198 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 7308 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 7308 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 7308 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 7308 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 7308 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 9443 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 9443 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 9443 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 215922 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 215926 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 97743 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 97743 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 144756 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 144756 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 9444 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 9444 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 9444 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 69699 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 69699 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 123925 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 123925 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 17106 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 17106 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 154367 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 154367 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 154195 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 154195 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 199370 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 199370 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 10738 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 10738 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 10738 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 10738 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 10738 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 97998 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 97998 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 78089 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 78089 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 6913 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 6913 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 6913 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 69704 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 69704 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 17144 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 17144 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 123925 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 123925 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 6918 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 6918 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 6918 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 68118 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 68118 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 98617 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 98617 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 69691 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 69691 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 187884 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 187884 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 10738 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 10738 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 10738 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 10738 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 10738 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 198581 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 198581 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 9434 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 9434 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 9434 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 98745 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 98745 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 9434 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 9434 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 9434 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 9434 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 9434 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 9434 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 9434 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 9434 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 9434 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 208462 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 208462 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 195826 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 195826 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 20964 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 20964 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 20964 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 9989 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 9989 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 9989 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 10738 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 10738 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 10738 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 10738 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 10738 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 20952 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 20952 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 20952 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 123925 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 123925 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 69696 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 69696 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 67856 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 67856 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 90316 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 90316 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 171586 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 171586 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 69700 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 69700 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 96301 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 96301 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 85969 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 85969 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 151677 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 151677 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 85204 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 85204 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 211594 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 211594 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 211594 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 194147 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 194147 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 97982 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 97982 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 68116 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 68116 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 108847 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 108847 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 85204 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 85204 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 190862 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 190862 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 10738 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 10738 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 10738 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 10738 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 10738 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 117693 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 117693 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 17117 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 17117 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 8220 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 8220 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 8220 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 8220 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 8220 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 176765 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 176765 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 17112 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 17112 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 7308 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 7308 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 7308 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 7308 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 7308 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 67855 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 67855 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 17145 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 17145 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 86037 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 86037 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 68123 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 68123 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 208390 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 208390 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 10738 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 10738 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 10738 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 10738 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 10738 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 195421 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 195421 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 10069 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 10069 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 10069 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 10069 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 21659 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 21659 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 21659 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 67024 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 67024 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 67024 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 67036 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 67036 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 67036 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 67037 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 67037 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 67037 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 21736 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 21736 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 21736 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 186294 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 186294 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 21504 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 21504 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 21504 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 9985 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 9985 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 9985 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 10069 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 10069 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 10069 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 10069 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 21497 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 21497 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 21497 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 21497 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 21497 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 21497 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 21497 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 21497 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 21497 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 9989 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 9989 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 9989 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 21525 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 21525 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 21525 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 10069 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 10069 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 10069 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 10069 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 21524 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 21524 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 21524 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 21690 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 21690 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 21690 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 167856 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 167856 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 167856 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 21608 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 21608 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 21608 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 187203 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 187203 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 21613 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 21613 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 21613 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 10738 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 10738 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 10738 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 10738 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 10738 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 21504 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 21504 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 21504 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 167892 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 167892 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 167892 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 9989 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 9989 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 9989 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 21502 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 21502 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 21502 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 21613 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 21613 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 21613 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 21497 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 21497 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 21497 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 9989 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 9989 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 9989 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 10069 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 21523 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 21523 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 21523 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 9989 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 9989 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 9989 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 9989 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 9989 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 9989 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 9989 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 9989 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 9989 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 21659 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 21659 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 21659 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 9989 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 9989 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 9989 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 21607 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 21607 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 21607 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 21708 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 21708 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 21708 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 67030 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 67030 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 67030 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 21522 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 21522 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 21522 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 9989 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 9989 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 9989 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 21623 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 21623 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 21623 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 9989 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 9989 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 9989 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 21623 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 21623 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 21623 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 21732 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 21732 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 21732 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 67031 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 67031 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 67031 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 21606 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 21606 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 21606 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 186437 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 186437 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 21502 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 21502 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 21502 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 21659 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 21659 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 21659 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 187330 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 187330 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 21703 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 21703 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 21703 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 188816 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 188816 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 9989 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 9989 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 9989 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 21606 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 21606 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 21606 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 21688 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 21688 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 21688 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 21688 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 21688 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 21688 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 10069 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 10069 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 10069 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 10069 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 21523 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 21523 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 21523 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 21501 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 21501 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 21501 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 186329 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 186329 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 21497 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 21497 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 21497 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 7248 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 7248 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 7248 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 186456 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 186456 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 21524 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 21524 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 21524 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 167866 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 167866 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 167866 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 21698 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 21698 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 21698 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 21625 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 21625 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 21625 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 21608 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 21608 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 21608 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 167809 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 167809 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 167809 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 21501 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 21501 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 21501 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 21509 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 21509 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 21509 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 21525 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 21525 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 21525 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 204660 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 204660 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 21607 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 21607 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 21607 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 10069 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 10069 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 10069 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 10069 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 21509 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 21509 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 21509 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 167884 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 167884 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 167884 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 166550 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 166550 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 167756 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 167756 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 167756 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 167943 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 167943 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 167943 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 163273 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 163273 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 7248 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 7248 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 7248 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 167977 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 167977 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 167977 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 165791 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 165791 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 167984 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 167984 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 167984 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 164387 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 164387 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 163283 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 163283 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 165056 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 165056 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 164196 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 164196 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 165104 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 165104 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 164486 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 164486 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 163510 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 163510 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 164943 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 164943 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 168006 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 168006 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 168006 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 163314 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 163314 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 166103 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 166103 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 165659 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 165659 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 166560 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 166560 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 164188 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 164188 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 167847 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 167847 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 167847 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 164425 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 164425 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 167864 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 167864 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 167864 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 165881 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 165881 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 167826 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 167826 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 167826 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 7308 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 7308 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 7308 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 7308 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 7308 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 8220 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 8220 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 8220 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 8220 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 8220 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 10738 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 10738 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 10738 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 10738 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 10738 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 9435 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 9435 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 10739 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 10739 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 10739 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 7249 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 7249 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 7238 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 7238 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 7238 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 7238 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 8149 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 8149 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 8149 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 8149 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 8149 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 8149 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 8149 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 8149 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 8149 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 8149 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 8149 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 8149 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 7308 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 9982 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 9982 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 9982 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 9982 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 9982 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 9982 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 9982 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 9982 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 9982 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 8220 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 8220 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 8220 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 8220 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 8220 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 6878 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 6878 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 6878 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 9434 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 9434 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 9434 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 10738 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 6918 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 6918 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 6918 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 6913 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 6913 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 6913 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 10482 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 9989 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 9989 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 9989 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 10069 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 10069 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 10069 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 10069 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 7248 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 7248 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 7248 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 10738 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 10738 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 10738 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 10738 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 10738 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 8149 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 8149 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 8149 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 8149 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 7308 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 7308 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 7308 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 7308 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 7308 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 117695 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 117695 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 211467 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 211467 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 168391 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 168391 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 168314 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 168314 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 168217 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 168217 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 168300 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 168300 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 168199 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 168199 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 168277 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 168277 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 168355 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 168355 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 168187 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 168187 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 168365 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 168365 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 168125 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 168125 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 168132 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 168132 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 168269 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 168269 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 168121 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 168121 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 168285 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 168285 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 168277 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 168277 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 168272 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 168272 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 7248 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 7248 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 7248 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 94238 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 94238 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 168292 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 168292 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 10739 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 10739 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 10739 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 7248 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 7248 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 7248 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 168300 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 168300 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 7248 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 7248 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 7248 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 7248 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 7248 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 7248 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 168280 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 168280 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 94242 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 94242 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 167884 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 167884 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 167884 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