Assay Detail

CHEMBL5148591

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Binding

Binding affinity to PAR4 (unknown origin) assessed as association constant

ChEMBL ↗

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Target

Proteinase-activated receptor 4 (CHEMBL4691) ↗

Open DB target context

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Proteinase-activated receptor 4 (CHEMBL4691) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Proteinase-activated receptor 4

CHEMBL4691

Anchored from Assay target.

Protein identity Proteinase-activated receptor 4

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Proteinase-activated receptor 4 (CHEMBL4691) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.

Priestley ES, Banville J, Deon D, Dubé L, Gagnon M, Guy J, Lapointe P, Lavallée JF, Martel A, Plamondon S, Rémillard R, Ruediger E, Tremblay F, Posy SL, Guarino VR, Richter JM, Li J, Gupta A, Vetrichelvan M, Balapragalathan TJ, Mathur A, Hua J, Callejo M, Guay J, Sum CS, Cvijic ME, Watson C, Wong P, Yang J, Bouvier M, Gordon DA, Wexler RR, Marinier A.
J Med Chem (2022) 65 : 8843 -8854
PubMed 35729784 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	2	10.11	10.15

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3716726	—	—	1	10.15
CHEMBL3716552	BMS-986141	2.0	1	10.07

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3716726	—	Kd	=	0.07	nM	10.15
CHEMBL3716552	BMS-986141	Kd	=	0.086	nM	10.07