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ChEMBL ligand: CHEMBL2172275 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244] | ||||||||
ChEMBL | Displacement of [33P]2-MeS-ADP from human recombinant P2Y12 receptor expressed in CHO cell membranes by scintillation counting method | B | 7.07 | pKi | 86 | nM | Ki | J Med Chem (2012) 55: 8615-8629 [PMID:22984835] |
ChEMBL | Antagonist activity at P2Y12 receptor in human washed platelets assessed as inhibition of ADP-induced platelet aggregation measured for 5 mins by light transmission analysis | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2739-2754 [PMID:27133596] |
ChEMBL | Antagonist activity at human P2Y12 | B | 6.89 | pIC50 | 129.9 | nM | IC50 | J Med Chem (2016) 59: 9981-10005 [PMID:27413802] |
GtoPdb | - | - | 7 | pIC50 | - | - | - | Thromb Res (2008) 122: 533-40 [PMID:18539312] |
ChEMBL | Displacement of [3H]-2-Mes-ADP from human P2Y12 receptor | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2739-2754 [PMID:27133596] |
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]