ATP [Ligand Id: 1713] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL14249 (Adenosine 5'-triphosphoric acid, Adenosine triphosphate) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Adenylate kinase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2376] [UniProtKB: P29410] | ||||||||
| ChEMBL | Inhibitory activity against rat adenylate kinase II was determined in the presence of ATP, non competitive inhibition | B | 4.05 | pKi | 90000 | nM | Ki | J Med Chem (1982) 25: 1179-1184 [PMID:6292418] |
| CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45] | ||||||||
| ChEMBL | Binding affinity to mitoNEET (unknown origin) by ITC method | B | 5.72 | pKd | 1920 | nM | Kd | Bioorg Med Chem Lett (2023) 89: 129310-129310 [PMID:37137430] |
| TNF receptor associated protein 1/Heat shock protein 75 kDa, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075132] [GtoPdb: 2909] [UniProtKB: Q12931] | ||||||||
| ChEMBL | Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from recombinant human Trap-1 after 24 hrs by fluorescence polarization assay | B | 4.5 | pIC50 | 31303 | nM | IC50 | J Med Chem (2013) 56: 6803-6818 [PMID:23965125] |
| Heat shock protein 90 beta in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4748] [UniProtKB: P41148] | ||||||||
| ChEMBL | Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from dog Grp94 after 24 hrs by fluorescence polarization assay | B | 5.49 | pIC50 | 3241 | nM | IC50 | J Med Chem (2013) 56: 6803-6818 [PMID:23965125] |
| ChEMBL | Inhibition of BODIPY-AG binding to dog Grp94 | B | 4.72 | pEC50 | 19000 | nM | EC50 | J Med Chem (2006) 49: 4606-4615 [PMID:16854066] |
| Kinesin-like protein KIFC1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3351200] [UniProtKB: Q9BW19] | ||||||||
| ChEMBL | Displacement of FP-Probe from N-terminal His-tagged full length recombinant human HSET incubated for 2 hrs by fluorescence polarization based competitive binding assay | B | 6.36 | pKd | 436 | nM | Kd | J Med Chem (2023) 66: 2622-2645 [PMID:36749938] |
| MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
| ChEMBL | Displacement of [8-3H]ATP from human recombinant MK2 (41-364) by scintillation proximity assay | B | 4.92 | pIC50 | 12000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 330-333 [PMID:19919896] |
| ChEMBL | Displacement of [8-3H]ATP from human recombinant MK2 (36-400) by scintillation proximity assay | B | 5.2 | pIC50 | 6300 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 330-333 [PMID:19919896] |
| ChEMBL | Inhibition of human recombinant phospho-MK2 (36-400) by HTRF assay | B | 5.55 | pIC50 | 2800 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 330-333 [PMID:19919896] |
| mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318] | ||||||||
| ChEMBL | Binding affinity to recombinant human biotinylated N-terminal GST-tagged autophosphorylated TAK1 (1 to 303 residues) fused with TAB1 (437 to 504 residues) expressed in baculovirus infected sf9 cells by SPR assay | B | 5.55 | pKd | 2800 | nM | Kd | Bioorg Med Chem Lett (2017) 27: 1031-1036 [PMID:28109791] |
| P2X1/P2X purinoceptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2094] [GtoPdb: 478] [UniProtKB: P51575] | ||||||||
| GtoPdb | - | - | 7.25 | pEC50 | 56 | nM | EC50 | J Med Chem (2002) 45: 4057-93 [PMID:12213051] |
| ChEMBL | Antagonist activity against recombinant human P2X purinoceptor 1 (P2X1 ) | F | 7.25 | pEC50 | 56 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X2/P2X purinoceptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2135] [GtoPdb: 479] [UniProtKB: P49653] | ||||||||
| GtoPdb | - | - | 5.85 | pEC50 | 1400 | nM | EC50 | Purinergic Signal (2009) 5: 75-89 [PMID:18600475] |
| ChEMBL | Antagonist activity against recombinant rat receptor P2X purinoceptor 2 (P2X2) at 10 uM, expressed in Xenopus oocytes | F | 5.85 | pEC50 | 1400 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X3/P2X purinoceptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2998] [GtoPdb: 480] [UniProtKB: P56373] | ||||||||
| ChEMBL | Antagonist activity against recombinant human P2X purinoceptor 3 (P2X3 ) | F | 6.47 | pEC50 | 340 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| GtoPdb | - | - | 6.47 | pEC50 | 340 | nM | EC50 | J Med Chem (2002) 45: 4057-93 [PMID:12213051] |
| P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571] | ||||||||
| GtoPdb | - | - | 5.9 | pEC50 | 1259 | nM | EC50 | Br J Pharmacol (2000) 129: 388-94 [PMID:10694247] |
| ChEMBL | Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2012) 55: 9576-9588 [PMID:23075067] |
| GtoPdb | - | - | 6.3 | pEC50 | 500 | nM | EC50 | J Med Chem (2002) 45: 4057-93 [PMID:12213051] |
| ChEMBL | Antagonist activity against recombinant human P2X purinoceptor 4 (P2X4) | F | 6.3 | pEC50 | 500 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X4/P2X purinoceptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176849] [GtoPdb: 481] [UniProtKB: Q9JJX6] | ||||||||
| GtoPdb | - | - | 5.6 | pEC50 | 2511 | nM | EC50 | Br J Pharmacol (2000) 129: 388-94 [PMID:10694247] |
| GtoPdb | - | - | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2002) 45: 4057-93 [PMID:12213051] |
| ChEMBL | Antagonist activity at mouse P2X4 receptor by cell-based calcium influx assay | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2012) 55: 9576-9588 [PMID:23075067] |
| P2X4/P2X purinoceptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577] | ||||||||
| GtoPdb | - | - | 5.3 | pEC50 | 5011 | nM | EC50 | Br J Pharmacol (2000) 129: 388-94 [PMID:10694247] |
| ChEMBL | Antagonist activity against recombinant rat P2X purinoceptor 4 (P2X4) at 30 uM, expressed in Xenopus oocytes | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| ChEMBL | Antagonist activity at rat P2X4 receptor by cell-based calcium influx assay | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2012) 55: 9576-9588 [PMID:23075067] |
| P2X5/P2X purinoceptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2495] [GtoPdb: 482] [UniProtKB: P51578] | ||||||||
| GtoPdb | - | - | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2002) 45: 4057-93 [PMID:12213051] |
| ChEMBL | Antagonist activity against recombinant rat P2X purinoceptor 5 (P2X5) | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X6/P2X purinoceptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2122] [GtoPdb: 483] [UniProtKB: P51579] | ||||||||
| GtoPdb | - | - | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2002) 45: 4057-93 [PMID:12213051] |
| ChEMBL | Antagonist activity against recombinant rat P2X purinoceptor 6 (P2X6 ) | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2Y purinoceptor 1 in Turkey (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5720] [UniProtKB: P49652] | ||||||||
| ChEMBL | Agonistic activity for P2Y purinoceptor 1 of turkey erythrocyte membranes | F | 5.2 | pEC50 | 6353 | nM | EC50 | J Med Chem (1999) 42: 3636-3646 [PMID:10479295] |
| ChEMBL | Evaluated for agonist activity against phospholipase C coupled P2Y purinoceptor 1 (P2Y1) of turkey erythrocytes | F | 5.55 | pEC50 | 2800 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| ChEMBL | Activation of Purinoceptor P2Y1-mediated phospholipase C in turkey erythrocyte membranes | B | 5.55 | pEC50 | 2800 | nM | EC50 | J Med Chem (2002) 45: 2090-2100 [PMID:11985476] |
| P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900] | ||||||||
| GtoPdb | - | - | 4.8 | pKi | - | - | - | Mol Pharmacol (1998) 53: 727-33 [PMID:9547364] |
| GtoPdb | - | - | 7.8 | pIC50 | - | - | - |
Br J Pharmacol (1997) 121: 338-44 [PMID:9154346]; Mol Pharmacol (2002) 62: 1249-57 [PMID:12391289] |
| ChEMBL | Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor | B | 5.82 | pEC50 | 1500 | nM | EC50 | J Med Chem (2002) 45: 2090-2100 [PMID:11985476] |
| ChEMBL | Agonist activity at human GFP-tagged P2Y1R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay | F | 6.07 | pEC50 | 850 | nM | EC50 | J Med Chem (2013) 56: 4938-4952 [PMID:23751098] |
| ChEMBL | Agonist activity at human P2Y1 receptor expressed in human 1321N1 cells assessed as increase of intracellular calcium level after 30 mins using fura-2 AM by fluorescence assay | F | 6.07 | pEC50 | 850 | nM | EC50 | J Med Chem (2014) 57: 4677-4691 [PMID:24846781] |
| 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 | 6.07 | pEC50 | 850 | nM | EC50 | J Med Chem (2015) 58: 8427-8443 [PMID:26447940] |
| ChEMBL | Agonist activity at P2Y1 receptor expressed in human HEK293 cells | F | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (2010) 53: 2472-2481 [PMID:20175517] |
| ChEMBL | Agonist activity at GFP tagged-human P2Y1 receptor expressed in human 1321N1 cells assessed as elevation in calcium level after 30 mins by fluorescence spectrophotometric analysis | F | 6.82 | pEC50 | 150 | nM | EC50 | J Med Chem (2010) 53: 8485-8497 [PMID:21090681] |
| P2Y1 receptor/Purinergic receptor P2Y1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2497] [GtoPdb: 323] [UniProtKB: P49651] | ||||||||
| ChEMBL | Concentration required for calcium mobilization at rat purinergic 2Y1 receptor expressed in HEK 293 cells | F | 6.23 | pEC50 | 590 | nM | EC50 | J Med Chem (2004) 47: 4405-4416 [PMID:15317453] |
| ChEMBL | Agonist activity at rat P2Y1R expressed in HEK293 cells assessed as release of intracellular calcium by fluorescence based assay | F | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (2012) 55: 7623-7635 [PMID:22873688] |
| P2Y11 receptor/Purinergic receptor P2Y11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91] | ||||||||
| ChEMBL | Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 11 | F | 4.76 | pEC50 | 17300 | nM | EC50 | J Med Chem (2002) 45: 2090-2100 [PMID:11985476] |
| ChEMBL | Agonist activity against phospholipase C coupled human P2Y purinoceptor 11 (P2Y11) | F | 4.77 | pEC50 | 17000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| ChEMBL | Agonist activity at human GFP-tagged P2Y11R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay | F | 5.17 | pEC50 | 6700 | nM | EC50 | J Med Chem (2013) 56: 4938-4952 [PMID:23751098] |
| ChEMBL | Agonist activity at GFP-tagged human P2Y11R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay | F | 5.17 | pEC50 | 6700 | nM | EC50 | J Med Chem (2015) 58: 8427-8443 [PMID:26447940] |
| ChEMBL | Agonist activity at GFP tagged-human P2Y11 receptor expressed in human 1321N1 cells assessed as elevation in calcium level after 30 mins by fluorescence spectrophotometric analysis | F | 5.48 | pEC50 | 3300 | nM | EC50 | J Med Chem (2010) 53: 8485-8497 [PMID:21090681] |
| GtoPdb | - | - | 5.6 | pEC50 | - | - | EC50 |
Br J Pharmacol (1999) 128: 1199-206 [PMID:10578132]; Mol Pharmacol (2003) 63: 1356-63 [PMID:12761346]; J Med Chem (2002) 45: 4057-93 [PMID:12213051] |
| P2Y12 receptor/Purinergic receptor P2Y12 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4] | ||||||||
| ChEMBL | Antagonist activity against phospholipase C coupled rat P2Y purinoceptor 12 (P2Y12) | F | 5.5 | pEC50 | 3190 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231] | ||||||||
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 4.93 | pEC50 | 11700 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.52 | pEC50 | 299 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | 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 level | F | 6.62 | pEC50 | 239 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.63 | pEC50 | 237 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at human P2Y2 transfected in human 1321N1 cells | B | 6.64 | pEC50 | 230 | nM | EC50 | J Med Chem (2016) 59: 9981-10005 [PMID:27413802] |
| ChEMBL | Agonist activity at P2Y2 receptor (unknown origin) | F | 6.64 | pEC50 | 230 | nM | EC50 | Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895] |
| ChEMBL | Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2) | F | 6.64 | pEC50 | 230 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| ChEMBL | Agonist activity at P2Y2 receptor in human CF/T43 cells | F | 6.7 | pEC50 | 200 | nM | EC50 | Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895] |
| ChEMBL | Agonist activity at P2Y2 receptor in BEA cells (unknown origin) | F | 6.7 | pEC50 | 200 | nM | EC50 | Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.74 | pEC50 | 183 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin) | F | 6.74 | pEC50 | 180 | nM | EC50 | Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.95 | pEC50 | 111 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | 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 level | F | 7.02 | pEC50 | 95.8 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | 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 assay | F | 7.07 | pEC50 | 85 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 3002-3005 [PMID:19419868] |
| ChEMBL | Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C | F | 7.07 | pEC50 | 85 | nM | EC50 | J Med Chem (2007) 50: 1166-1176 [PMID:17302398] |
| ChEMBL | Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2 | F | 7.07 | pEC50 | 85 | nM | EC50 | J Med Chem (2002) 45: 2090-2100 [PMID:11985476] |
| GtoPdb | - | - | 7.1 | pEC50 | - | - | EC50 |
Br J Pharmacol (1995) 116: 1619-27 [PMID:8564228]; J Med Chem (2002) 45: 208-18 [PMID:11754592]; J Med Chem (2002) 45: 4057-93 [PMID:12213051] |
| ChEMBL | 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 level | F | 7.2 | pEC50 | 63.1 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 7.52 | pEC50 | 30.1 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582] | ||||||||
| GtoPdb | - | - | 6.2 | pKd | - | - | - | Mol Pharmacol (2000) 57: 926-31 [PMID:10779375] |
| ChEMBL | The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4) | F | 4.37 | pEC50 | 43000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| ChEMBL | Antagonist activity at human P2Y4 | B | 5.21 | pEC50 | 6200 | nM | EC50 | J Med Chem (2016) 59: 9981-10005 [PMID:27413802] |
| GtoPdb | - | - | 5.37 | pEC50 | 4300 | nM | EC50 | Biochim Biophys Acta (2011) 1812: 982-94 [PMID:21193033] |
| P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2124] [GtoPdb: 325] [UniProtKB: O35811] | ||||||||
| ChEMBL | The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4) | F | 5.74 | pEC50 | 1800 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| ChEMBL | Antagonist activity at rat P2Y4 | B | 5.93 | pEC50 | 1170 | nM | EC50 | J Med Chem (2016) 59: 9981-10005 [PMID:27413802] |
| GtoPdb | - | - | 6.3 | pEC50 | - | - | EC50 |
Br J Pharmacol (1998) 124: 428-30 [PMID:9647463]; Mol Pharmacol (2000) 57: 926-31 [PMID:10779375]; J Med Chem (2002) 45: 4057-93 [PMID:12213051] |
| P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077] | ||||||||
| ChEMBL | The compound was evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 6 (P2Y6) | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| Serine/threonine protein phosphatase 2A, 56 kDa regulatory subunit, alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4763] [UniProtKB: Q15172] | ||||||||
| ChEMBL | Binding affinity against Purine Nucleoside Phosphatase | B | 7.16 | pKd | -7.16 | - | Log Kd | J Med Chem (2002) 45: 2770-2780 [PMID:12061879] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Binding affinity to wild type 6XHis-tagged human JAK2 JH2 domain (513 to 827 residues) expressed in baculovirus infected Sf9 cells by MANT-ATP binding assay | B | 5.89 | pKd | 1300 | nM | Kd | J Med Chem (2020) 63: 5324-5340 [PMID:32329617] |
| ChEMBL | Binding affinity to 6XHis-tagged human JAK2 JH2 domain V617F mutant (513 to 827 residues) expressed in baculovirus infected Sf9 cells by MANT-ATP binding assay | B | 5.89 | pKd | 1300 | nM | Kd | J Med Chem (2020) 63: 5324-5340 [PMID:32329617] |
| GPR17 in Human [GtoPdb: 88] [UniProtKB: Q13304] | ||||||||
| GtoPdb | - | - | 7.43 | pEC50 | 37 | nM | EC50 | Purinergic Signal (2011) 7: 463-8 [PMID:21773766] |
| P2Y13 receptor in Human [GtoPdb: 329] [UniProtKB: Q9BPV8] | ||||||||
| GtoPdb | - | - | 5.4 | pIC50 | - | - | - | Mol Pharmacol (2003) 64: 104-12 [PMID:12815166] |
| P2X7 in Human [GtoPdb: 484] [UniProtKB: Q99572] | ||||||||
| GtoPdb | - | - | 3.11 | pEC50 | 780000 | nM | EC50 | J Med Chem (2002) 45: 4057-93 [PMID:12213051] |
| TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43] | ||||||||
| GtoPdb | - | - | 4.9 | pIC50 | - | - | - | Pflugers Arch (2004) 448: 70-5 [PMID:14758478] |
| GtoPdb | - | - | 5.8 | pIC50 | - | - | - | Pflugers Arch (2004) 448: 70-5 [PMID:14758478] |
| TRPM4 in Mouse [GtoPdb: 496] [UniProtKB: Q7TN37] | ||||||||
| GtoPdb | - | - | 6.1 | pIC50 | - | - | - | Cell Calcium (2005) 37: 267-78 [PMID:15670874] |
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]
