ATP [Ligand Id: 1713] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL14249 (Adenosine triphosphate)
  • Adenylate kinase 2 in Rat [ChEMBL: CHEMBL2376] [UniProtKB: P29410]
  • This target only has 1 pki data point
  • 4.05
1 CHEMBL14249_lig_chart_1 Adenylate kinase 2 Rat
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  • TNF receptor associated protein 1/Heat shock protein 75 kDa, mitochondrial in Human [ChEMBL: CHEMBL1075132] [GtoPdb: 2909] [UniProtKB: Q12931]
  • This target only has 0 pki data point
  • 0
2 CHEMBL14249_lig_chart_2 Heat shock protein 75 kDa, mitochondrial Human
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  • Heat shock protein 90 beta in Dog [ChEMBL: CHEMBL4748] [UniProtKB: P41148]
  • This target only has 0 pki data point
  • 0
3 CHEMBL14249_lig_chart_3 Heat shock protein 90 beta Dog
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  • MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
  • This target only has 0 pki data point
  • 0
4 CHEMBL14249_lig_chart_4 MAP kinase-activated protein kinase 2 Human
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  • mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318]
  • This target only has 0 pki data point
  • 0
5 CHEMBL14249_lig_chart_5 Mitogen-activated protein kinase kinase kinase 7 Human
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  • P2X1/P2X purinoceptor 1 in Human [ChEMBL: CHEMBL2094] [GtoPdb: 478] [UniProtKB: P51575]
  • This target only has 0 pki data point
  • 0
6 CHEMBL14249_lig_chart_6 P2X purinoceptor 1 Human
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  • P2X2/P2X purinoceptor 2 in Rat [ChEMBL: CHEMBL2135] [GtoPdb: 479] [UniProtKB: P49653]
  • This target only has 0 pki data point
  • 0
7 CHEMBL14249_lig_chart_7 P2X purinoceptor 2 Rat
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  • P2X3/P2X purinoceptor 3 in Human [ChEMBL: CHEMBL2998] [GtoPdb: 480] [UniProtKB: P56373]
  • This target only has 0 pki data point
  • 0
8 CHEMBL14249_lig_chart_8 P2X purinoceptor 3 Human
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  • P2X4/P2X purinoceptor 4 in Human [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571]
  • P2X4/P2X purinoceptor 4 in Mouse [ChEMBL: CHEMBL2176849] [GtoPdb: 481] [UniProtKB: Q9JJX6]
  • P2X4/P2X purinoceptor 4 in Rat [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577]
  • This target only has 0 pki data point
  • 0
9 CHEMBL14249_lig_chart_9 P2X purinoceptor 4 HumanMouseRat
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  • P2X5/P2X purinoceptor 5 in Rat [ChEMBL: CHEMBL2495] [GtoPdb: 482] [UniProtKB: P51578]
  • This target only has 0 pki data point
  • 0
10 CHEMBL14249_lig_chart_10 P2X purinoceptor 5 Rat
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  • P2X6/P2X purinoceptor 6 in Rat [ChEMBL: CHEMBL2122] [GtoPdb: 483] [UniProtKB: P51579]
  • This target only has 0 pki data point
  • 0
11 CHEMBL14249_lig_chart_11 P2X purinoceptor 6 Rat
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  • P2Y purinoceptor 1 in Turkey [ChEMBL: CHEMBL5720] [UniProtKB: P49652]
  • This target only has 0 pki data point
  • 0
12 CHEMBL14249_lig_chart_12 P2Y purinoceptor 1 Turkey
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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]
  • This target only has 1 pki data point
  • 0
13 CHEMBL14249_lig_chart_13 Purinergic receptor P2Y1 HumanRat
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  • P2Y11 receptor/Purinergic receptor P2Y11 in Human [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91]
  • This target only has 0 pki data point
  • 0
14 CHEMBL14249_lig_chart_14 Purinergic receptor P2Y11 Human
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  • P2Y12 receptor/Purinergic receptor P2Y12 in Rat [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4]
  • This target only has 0 pki data point
  • 0
15 CHEMBL14249_lig_chart_15 Purinergic receptor P2Y12 Rat
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  • P2Y2 receptor/Purinergic receptor P2Y2 in Human [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
  • This target only has 0 pki data point
  • 0
16 CHEMBL14249_lig_chart_16 Purinergic receptor P2Y2 Human
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  • P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582]
  • P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Rat [ChEMBL: CHEMBL2124] [GtoPdb: 325] [UniProtKB: O35811]
  • This target only has 0 pki data point
  • 0
17 CHEMBL14249_lig_chart_17 Pyrimidinergic receptor P2Y4 HumanRat
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  • P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
  • This target only has 0 pki data point
  • 0
18 CHEMBL14249_lig_chart_18 Pyrimidinergic receptor P2Y6 Human
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  • Serine/threonine protein phosphatase 2A, 56 kDa regulatory subunit, alpha isoform in Human [ChEMBL: CHEMBL4763] [UniProtKB: Q15172]
  • This target only has 0 pki data point
  • 0
19 CHEMBL14249_lig_chart_19 Serine/threonine protein phosphatase 2A, 56 kDa regulatory subunit, alpha isoform Human
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
  • This target only has 0 pki data point
  • 0
20 CHEMBL14249_lig_chart_20 Tyrosine-protein kinase JAK2 Human
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  • GPR17 in Human [GtoPdb: 88] [UniProtKB: Q13304]
  • This target only has 0 pki data point
  • 0
21 CHEMBL14249_lig_chart_21 GPR17 Human
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  • P2Y13 receptor in Human [GtoPdb: 329] [UniProtKB: Q9BPV8]
  • This target only has 0 pki data point
  • 0
22 CHEMBL14249_lig_chart_22 P2Y13 receptor Human
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  • P2X7 in Human [GtoPdb: 484] [UniProtKB: Q99572]
  • This target only has 0 pki data point
  • 0
23 CHEMBL14249_lig_chart_23 P2X7 Human
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  • TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43]
  • TRPM4 in Mouse [GtoPdb: 496] [UniProtKB: Q7TN37]
  • This target only has 0 pki data point
  • 0
24 CHEMBL14249_lig_chart_24 TRPM4 HumanMouse
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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]
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]
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 B 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 B 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 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 (unknown origin) F 6.64 pEC50 230 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 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 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 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]
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]
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]
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]
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]