[3H]2MeSADP [Ligand Id: 1763] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL435402 (2-MeSADP, 2-MeS-ADP, 2-(Methylthio)-Adenosinediphosphate)
  • Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Human [ChEMBL: CHEMBL5925] [UniProtKB: P22413]
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  • P2Y1 receptor/Purinergic receptor P2Y1 in Human [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
  • P2Y1 receptor/Purinergic receptor P2Y1 in Rat [ChEMBL: CHEMBL2497] [GtoPdb: 323] [UniProtKB: P49651]
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  • P2Y2 receptor/Purinergic receptor P2Y2 in Human [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
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  • P2Y12 receptor in Human [GtoPdb: 328] [UniProtKB: Q9H244]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5925] [UniProtKB: P22413]
ChEMBL Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using p-Nph-5'-AMP as substrate after 30 mins by capillary electrophoresis method B 4.45 pKi 35400 nM Ki MedChemComm (2017) 8: 823-840
ChEMBL Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using ATP as substrate by capillary electrophoresis method B 4.48 pKi 32800 nM Ki MedChemComm (2017) 8: 823-840
ChEMBL Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using ATP as substrate after 30 mins by capillary electrophoresis method B 4.63 pKi 23700 nM Ki MedChemComm (2017) 8: 823-840
ChEMBL Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using p-Nph-5'-TMP as substrate after 15 mins by capillary electrophoresis method B 5.66 pKi 2180 nM Ki MedChemComm (2017) 8: 823-840
P2Y purinoceptor 1 in Turkey (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5720] [UniProtKB: P49652]
ChEMBL Evaluated for agonist activity against phospholipase C coupled P2Y purinoceptor 1 (P2Y1) of turkey erythrocytes F 8.22 pEC50 6 nM EC50 J. Med. Chem. (2002) 45: 4057-4093 [PMID:12213051]
ChEMBL Activation of Purinoceptor P2Y1-mediated phospholipase C in turkey erythrocyte membranes B 8.22 pEC50 6 nM EC50 J. Med. Chem. (2002) 45: 2090-2100 [PMID:11985476]
ChEMBL Agonist activity at turkey P2Y1 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis F 8.4 pEC50 4 nM EC50 Eur. J. Med. Chem. (2009) 44: 1525-1536 [PMID:18760862]
ChEMBL Agonist activity at turkey P2Y purinoceptor 1 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry F 8.4 pEC50 4 nM EC50 J. Med. Chem. (2012) 55: 437-448 [PMID:22107038]
ChEMBL Agonist activity at turkey P2Y1 receptor expressed in human 132N1 receptor assessed as induction of intracellular calcium mobilization F 8.6 pEC50 2.5 nM EC50 J. Med. Chem. (2010) 53: 3305-3319 [PMID:20337495]
ChEMBL Agonist activity at turkey P2Y1R expressed in 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry F 8.6 pEC50 2.5 nM EC50 J. Med. Chem. (2012) 55: 7623-7635 [PMID:22873688]
P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
GtoPdb - - 7.3 pKd 49 nM Kd Mol Pharmacol (2001) 60: 432-439 [PMID:11502873]
ChEMBL Inhibition concentration required against human Y203A (EL2) mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Inhibition concentration required against human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand B 6.44 pIC50 360 nM IC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Inhibition concentration required against human Y203F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand B 6.59 pIC50 260 nM IC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Inhibition concentration required against human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand B 6.82 pIC50 150 nM IC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Inhibition concentration required against human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand B 7.4 pIC50 40 nM IC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Inhibition concentration required against wild type strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]-MRS2279 as radioligand B 7.62 pIC50 24 nM IC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Inhibition concentration required against human Y273A mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]-MRS2279 as radioligand B 7.66 pIC50 22 nM IC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human C202A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R287E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human S314A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human C124A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R128A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R310A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human E209A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 4.76 pEC50 17200 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R287A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 4.83 pEC50 14800 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration to activate human Y203A (EL2) mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate B 5 pEC50 >10000 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration to activate human Y273A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate B 5 pEC50 >10000 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R287Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 5.28 pEC50 5290 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human C296A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 5.29 pEC50 5160 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(R310K) human P2Y1 receptor in presence of MRS2179 F 5.64 pEC50 2270 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration required for the activation of human K280A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 5.75 pEC50 1790 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(K280A) human P2Y1 receptor in presence of MRS2179 F 5.8 pEC50 1580 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(K280A) human P2Y1 receptor. F 5.82 pEC50 1520 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(H277A) human P2Y1 receptor in presence of MRS2179 F 6.13 pEC50 738 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration required for the activation of human D204N mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 6.23 pEC50 595 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human Q307A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 6.34 pEC50 455 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R310K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 6.38 pEC50 418 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(Q307A) human P2Y1 receptor in presence of MRS2179 F 6.42 pEC50 378 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(R310K) human P2Y1 receptor. F 6.49 pEC50 324 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(Q307A) human P2Y1 receptor. F 6.49 pEC50 323 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration required for the activation of human D204E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 6.84 pEC50 145 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(H277A) human P2Y1 receptor. F 6.94 pEC50 115 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(F131A) human P2Y1 receptor in presence of MRS2179 (P<0.05) F 6.99 pEC50 103 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration required for the activation of human H277A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7 pEC50 100 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R287K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7.13 pEC50 74.9 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human D204A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7.18 pEC50 66.5 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(H132A) human P2Y1 receptor in presence of MRS2179 (P<0.005) F 7.28 pEC50 53 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(Y136A) human P2Y1 receptor in presence of MRS2179 (P<0.005) F 7.44 pEC50 36 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(S314T) human P2Y1 receptor in presence of MRS2179 F 7.51 pEC50 30.9 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(F226A) human P2Y1 receptor in presence of MRS2179. F 7.57 pEC50 27 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(T222A) human P2Y1 receptor in presence of MRS2179 (P<0.005) F 7.6 pEC50 25 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration required for the activation of human F226A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7.68 pEC50 20.7 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(F226A) human P2Y1 receptor. F 7.71 pEC50 19.5 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(F131A) human P2Y1 receptor. F 7.72 pEC50 19.2 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration to activate human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate B 7.72 pEC50 19 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human F131A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7.74 pEC50 18.2 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(H132A) human P2Y1 receptor. F 7.75 pEC50 17.7 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration required for the activation of human K198A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7.76 pEC50 17.5 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration to activate human Y203F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate B 7.8 pEC50 16 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human H132A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7.8 pEC50 15.9 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human T221A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7.8 pEC50 15.9 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration to activate human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate B 7.82 pEC50 15 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Agonist activity at GFP-tagged human P2Y1R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay B 7.89 pEC50 13 nM EC50 J. Med. Chem. (2015) 58: 8427-8443 [PMID:26447940]
ChEMBL Agonist activity at human GFP-tagged P2Y1R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay F 7.89 pEC50 13 nM EC50 J. Med. Chem. (2013) 56: 4938-4952 [PMID:23751098]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(WT) human P2Y1 receptor in presence of MRS2179 (P<0.005) F 7.89 pEC50 12.9 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration required for the activation of human Y136A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7.9 pEC50 12.6 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(T221A) human P2Y1 receptor in presence of MRS2179 (P<0.005) F 7.91 pEC50 12.4 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Agonist activity at P2Y1 receptor expressed in 1321N1 cells assessed as cytosolic calcium level F 7.91 pEC50 12.3 nM EC50 J. Med. Chem. (2007) 50: 5600-5607 [PMID:17941622]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(Y136A) human P2Y1 receptor. F 7.91 pEC50 12.3 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(S317A) human P2Y1 receptor in presence of MRS2179 F 7.92 pEC50 12.1 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration required for the activation of human S314T mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7.93 pEC50 11.7 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human T222A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 7.95 pEC50 11.2 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Activity against human P2Y1-GFP expressed in 1321N1 cells by intracellular calcium increase F 7.96 pEC50 11 nM EC50 J. Med. Chem. (2006) 49: 1980-1990 [PMID:16539385]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(T222A) human P2Y1 receptor. F 7.96 pEC50 10.9 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(S314T) human P2Y1 receptor. F 7.98 pEC50 10.4 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Activation of human P2Y1 receptor expressed in human 1321N1 cells assessed as induction of calcium flux by FLIPR assay B 7.99 pEC50 10.3 nM EC50 J. Med. Chem. (2010) 53: 2562-2576 [PMID:20192270]
ChEMBL Effective concentration required for the activation of human D300A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.01 pEC50 9.8 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R285A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.04 pEC50 9.2 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human E209Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.07 pEC50 8.6 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R212A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.11 pEC50 7.8 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor B 8.19 pEC50 6.4 nM EC50 J. Med. Chem. (2002) 45: 2090-2100 [PMID:11985476]
ChEMBL Effective concentration to activate human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate B 8.22 pEC50 6 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human K125A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.23 pEC50 5.9 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human E209R mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.31 pEC50 4.9 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R195A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.33 pEC50 4.7 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human D289A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.41 pEC50 3.9 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human D208A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.44 pEC50 3.6 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human E209D mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.49 pEC50 3.2 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration to activate wild-type P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate B 8.52 pEC50 3 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human R301A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.59 pEC50 2.6 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of human K196A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.6 pEC50 2.5 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Agonist activity at G-protein coupled P2Y1 receptor expressed in human 1321N1 cells assessed as increase in calcium by Fura2 assay F 8.6 pEC50 2.5 nM EC50 J. Med. Chem. (2010) 53: 2472-2481 [PMID:20175517]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(T221A) human P2Y1 receptor. F 8.61 pEC50 2.45 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate is determined in separate experiment B 8.66 pEC50 2.2 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(WT) human P2Y1 receptor. F 8.71 pEC50 1.94 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Compound was measured for the antagonism of the activation of phospholipase C in mutant(S317A) human P2Y1 receptor. F 8.73 pEC50 1.88 nM EC50 J. Med. Chem. (1998) 41: 1456-1466 [PMID:9554879]
ChEMBL Effective concentration required for the activation of human S317A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.8 pEC50 1.58 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
ChEMBL Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate B 8.9 pEC50 1.27 nM EC50 J. Med. Chem. (2004) 47: 5393-5404 [PMID:15481977]
P2Y1 receptor/Purinergic receptor P2Y1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2497] [GtoPdb: 323] [UniProtKB: P49651]
ChEMBL Activity against rat P2Y1-GFP transfected in HEK293 cells by intracellular calcium increase F 7 pEC50 100 nM EC50 J. Med. Chem. (2006) 49: 1980-1990 [PMID:16539385]
P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
ChEMBL Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2) F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2002) 45: 4057-4093 [PMID:12213051]
P2Y12 receptor in Human [GtoPdb: 328] [UniProtKB: Q9H244]
GtoPdb - - 9.6 pIC50 0.25 nM IC50 Mol Pharmacol (2001) 60: 432-439 [PMID:11502873]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]