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ChEMBL ligand: CHEMBL435402 (2-MeS-ADP, 2-MeSADP, 2-(Methylthio)-Adenosinediphosphate) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 [PMID:30108800] |
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 [PMID:30108800] |
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 [PMID:30108800] |
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 [PMID:30108800] |
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] | ||||||||
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] |
GtoPdb | - | - | 7 | pIC50 | - | - | - |
Br J Pharmacol (1997) 121: 338-44 [PMID:9154346]; Mol Pharmacol (2002) 62: 1249-57 [PMID:12391289] |
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 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 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 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 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 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 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 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 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 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 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 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 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 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 | F | 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 | F | 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 | Agonist activity at human P2Y1R in human 1321N1 cells | B | 8.19 | pEC50 | 6.4 | nM | EC50 | RSC Med Chem (2021) 12: 1808-1825 [PMID:34825182] |
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 | 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 | 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 | 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] |
P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244] | ||||||||
ChEMBL | Displacement of [3H]-2MesADP from recombinant human P2Y12 transfected in HEK cell membrane assessed as inhibition constant | B | 7.49 | pKi | 32.1 | nM | Ki | Bioorg Med Chem Lett (2022) 71: 128837-128837 [PMID:35640763] |
GtoPdb | - | - | 9.2 | pKi | - | - | - | Nature (2001) 409: 202-7 [PMID:11196645] |
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] |
P2Y13 receptor in Human [GtoPdb: 329] [UniProtKB: Q9BPV8] | ||||||||
GtoPdb | - | - | 9 | pIC50 | - | - | - | Mol Pharmacol (2003) 64: 104-12 [PMID:12815166] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]