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 platelet rich plasma F 5.44 pIC50 3600 nM IC50 Bioorg Med Chem (2022) 56: 116614-116614 [PMID:35033884]
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 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 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 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]