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ChEMBL ligand: CHEMBL2419490 |
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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] | ||||||||
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]