ChEMBL ligand: CHEMBL3728620
PAR4/Proteinase activated receptor 4 in Human [ChEMBL: CHEMBL4691] [GtoPdb: 350] [UniProtKB: Q96RI0] There should be some charts here, you may need to enable JavaScript!

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	Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes	B	8.52	pKd	3	nM	Kd	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]
ChEMBL	Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes measured after 2 hrs	B	8.85	pKd	1.4	nM	Kd	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]
ChEMBL	Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin	B	7.6	pIC50	25	nM	IC50	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]
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	7.61	pIC50	24.74	nM	IC50	WO-2013163244-A1. Imidazothiadiazole derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation (2013)
ChEMBL	Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin	B	8.1	pIC50	8	nM	IC50	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]
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 before agonist addition by FLIPR assay	F	8.62	pIC50	2.42	nM	IC50	WO-2013163244-A1. Imidazothiadiazole derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation (2013)
ChEMBL	Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay	F	8.62	pIC50	2.4	nM	IC50	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]
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	8.62	pIC50	2.4	nM	IC50	J Med Chem (2022) 65: 8843-8854 [PMID:35729784]
GtoPdb	Measuring inhibition of PAR4 agonist-induced intracellular calcium mobilization in HEK293-PAR4 cells by FLIPR assay.	-	8.62	pIC50	2.4	nM	IC50	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]

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]