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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  • PAR4/Proteinase activated receptor 4 in Human [ChEMBL: CHEMBL4691] [GtoPdb: 350] [UniProtKB: Q96RI0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL Agonist activity at PXR (unknown origin) B 4.82 pEC50 >15000 nM EC50 J Med Chem (2022) 65: 8843-8854 [PMID:35729784]
PAR4/Proteinase activated receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4691] [GtoPdb: 350] [UniProtKB: Q96RI0]
ChEMBL Binding affinity to PAR4 (unknown origin) assessed as saturation binding B 10 pKd 0.1 nM Kd J Med Chem (2022) 65: 8843-8854 [PMID:35729784]
ChEMBL Binding affinity to PAR4 (unknown origin) assessed as association constant B 10.07 pKd 0.09 nM Kd J Med Chem (2022) 65: 8843-8854 [PMID:35729784]
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 at full length 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 pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method F 9.4 pIC50 0.4 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 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]