AZD1283 [Ligand Id: 7360] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2419490
  • P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
GtoPdb - - 8 pKi - - - Nature (2014) 509: 115-8 [PMID:24670650];
Future Med Chem (2013) 5: 2037-56 [PMID:24215345]
ChEMBL Antagonist activity at P2Y12 receptor in human whole blood assessed as inhibition of ADP-induced platelet aggregation after 5 mins by residual platelet count assay B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2013) 56: 7015-7024 [PMID:23899349]
ChEMBL Antagonist activity P2Y12 receptor in human blood assessed as inhibition of ADP-induced platelet aggregation measured as residual platelet count after 5 mins by flow cytometric analysis B 5.49 pIC50 3200 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 10 seconds B 7.36 pIC50 44 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL Antagonist activity at P2Y12 receptor (unknown origin) expressed in CHO cell membrane by [35S]GTPgammaS binding assay F 7.6 pIC50 25 nM IC50 J. Med. Chem. (2013) 56: 7015-7024 [PMID:23899349]
ChEMBL Antagonist activity at P2Y12 receptor (unknown origin) assessed as inhibition of ADP-induced [35S]GTPgammaS binding after 45 mins by scintillation counting analysis F 7.6 pIC50 25 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 30 seconds B 7.66 pIC50 22 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 seconds B 7.85 pIC50 14 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL Displacement of [125I]-AZ11931285 from P2Y12 receptor (unknown origin) expressed in CHO cell membrane after 1 hr by scintillation counting analysis B 7.96 pIC50 11 nM IC50 J. Med. Chem. (2013) 56: 7015-7024 [PMID:23899349]
ChEMBL Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 mins B 8.05 pIC50 9 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL Antagonist activity P2Y12 receptor in human washed platelets assessed as inhibition of ADP-induced platelet aggregation after 5 to 90 mins by spectrophotometric analysis B 8.05 pIC50 9 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2963-2968 [PMID:24835983]

ChEMBL data shown on this page come from version 28:

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