Assay Detail

CHEMBL5148596

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Functional

Antiplatelet activity against PAR4 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

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Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

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	Functional
Organism	Homo sapiens
Cell Type	Platelet
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

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
IC50	2	8.21	8.66

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3716552	BMS-986141	2.0	1	8.66
CHEMBL3716726	—	—	1	7.76

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3716552	BMS-986141	IC50	=	2.2	nM	8.66
CHEMBL3716726	—	IC50	=	17.5	nM	7.76