[3H]2MeSADP [Ligand Id: 1763] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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] | ||||||||
| 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 | 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 | 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
