PSB-0739 [Ligand Id: 5904] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL455536 (PSB-0739) |
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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] | ||||||||
| ChEMBL | Competitive antagonist activity at human P2Y12 receptor expressed in CHO cells assessed as forskolin/ 2-methylthio-ADP-induced cAMP production preincubated for 10 mins followed 2-methylthio-ADP addition measured after 3.5 hrs by luciferase reporter gene assay | F | 9.8 | pKd | 0.16 | nM | Kd | J Med Chem (2017) 60: 3020-3038 [PMID:28306255] |
| GtoPdb | - | - | 7.6 | pKi | 24.9 | nM | Ki | J Med Chem (2009) 52: 3784-93 [PMID:19463000] |
| ChEMBL | Binding affinity to P2Y12 (unknown origin) assessed as inhibition constant | B | 7.6 | pKi | 25 | nM | Ki | Bioorg Med Chem Lett (2022) 71: 128837-128837 [PMID:35640763] |
| ChEMBL | Displacement of [3H]PSB0413 from human platelet P2Y12 receptor | B | 7.6 | pKi | 24.9 | nM | Ki | J Med Chem (2009) 52: 3784-3793 [PMID:19463000] |
| GtoPdb | - | - | 9.8 | pA2 | - | - | - | J Pharmacol Exp Ther (2009) 331: 648-55 [PMID:19690189] |
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]
