BMS-986141 [Ligand Id: 12038] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3716552 (Bms-986141, BMS-986141, UDM-003183) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| PAR4/Proteinase activated receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4691] [GtoPdb: 350] [UniProtKB: Q96RI0] | ||||||||
| ChEMBL | Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay | F | 8.47 | pIC50 | 3.35 | nM | IC50 | Eur J Med Chem (2021) 225: 113764-113764 [PMID:34391031] |
| ChEMBL | Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay | F | 8.68 | pIC50 | 2.1 | nM | IC50 | US-20150094297-A1. Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation (2015) |
| GtoPdb | Affinity determined by saturation binding assay. | - | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2022) 65: 8843-8854 [PMID:35729784] |
| ChEMBL | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay | F | 9.35 | pEC50 | 0.45 | nM | EC50 | US-20150094297-A1. Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation (2015) |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
