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Assay Detail

CHEMBL5148580

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
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
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
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
IC50 53 9.02 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3716230 — — 1 9.70
CHEMBL3715848 — — 1 9.52
CHEMBL3717235 — — 1 9.52
CHEMBL3718639 — — 1 9.52
CHEMBL3717937 — — 1 9.52
CHEMBL5189522 — — 1 9.40
CHEMBL5206065 — — 1 9.40
CHEMBL3716552 BMS-986141 2.0 1 9.40
CHEMBL3715840 — — 1 9.40
CHEMBL3718059 — — 1 9.40
CHEMBL3716726 — — 1 9.40
CHEMBL3718313 — — 1 9.30
CHEMBL3715722 — — 1 9.30
CHEMBL3719106 — — 1 9.30
CHEMBL3716066 — — 1 9.30
CHEMBL3718564 — — 1 9.30
CHEMBL3716636 — — 1 9.22
CHEMBL3716064 — — 1 9.22
CHEMBL3718360 — — 1 9.22
CHEMBL5177223 — — 1 9.22
CHEMBL3714821 — — 1 9.22
CHEMBL3715632 — — 1 9.22
CHEMBL3715852 — — 1 9.22
CHEMBL3719215 — — 1 9.22
CHEMBL5184586 — — 1 9.20
CHEMBL5171201 — — 1 9.15
CHEMBL3717535 — — 1 9.15
CHEMBL3717597 — — 1 9.15
CHEMBL3715516 — — 1 9.10
CHEMBL3715093 — — 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3716230 — IC50 = 0.2 nM 9.70
CHEMBL3715848 — IC50 = 0.3 nM 9.52
CHEMBL3717235 — IC50 = 0.3 nM 9.52
CHEMBL3718639 — IC50 = 0.3 nM 9.52
CHEMBL3717937 — IC50 = 0.3 nM 9.52
CHEMBL5189522 — IC50 = 0.4 nM 9.40
CHEMBL5206065 — IC50 = 0.4 nM 9.40
CHEMBL3716552 BMS-986141 IC50 = 0.4 nM 9.40
CHEMBL3715840 — IC50 = 0.4 nM 9.40
CHEMBL3718059 — IC50 = 0.4 nM 9.40
CHEMBL3716726 — IC50 = 0.4 nM 9.40
CHEMBL3718564 — IC50 = 0.5 nM 9.30
CHEMBL3718313 — IC50 = 0.5 nM 9.30
CHEMBL3715722 — IC50 = 0.5 nM 9.30
CHEMBL3719106 — IC50 = 0.5 nM 9.30
CHEMBL3716066 — IC50 = 0.5 nM 9.30
CHEMBL3719215 — IC50 = 0.6 nM 9.22
CHEMBL3715852 — IC50 = 0.6 nM 9.22
CHEMBL3715632 — IC50 = 0.6 nM 9.22
CHEMBL3714821 — IC50 = 0.6 nM 9.22
CHEMBL5177223 — IC50 = 0.6 nM 9.22
CHEMBL3716636 — IC50 = 0.6 nM 9.22
CHEMBL3718360 — IC50 = 0.6 nM 9.22
CHEMBL3716064 — IC50 = 0.6 nM 9.22
CHEMBL5184586 — IC50 = 0.63 nM 9.20
CHEMBL5171201 — IC50 = 0.7 nM 9.15
CHEMBL3717597 — IC50 = 0.7 nM 9.15
CHEMBL3717535 — IC50 = 0.7 nM 9.15
CHEMBL3715516 — IC50 = 0.8 nM 9.10
CHEMBL3715093 — IC50 = 0.8 nM 9.10
CHEMBL5173906 — IC50 = 0.8 nM 9.10
CHEMBL3717040 — IC50 = 0.8 nM 9.10
CHEMBL3719264 — IC50 = 0.9 nM 9.05
CHEMBL3719331 — IC50 = 1.1 nM 8.96
CHEMBL5205126 — IC50 = 1.1 nM 8.96
CHEMBL3715264 — IC50 = 1.1 nM 8.96
CHEMBL3719069 — IC50 = 1.3 nM 8.89
CHEMBL3718231 — IC50 = 1.3 nM 8.89
CHEMBL3717275 — IC50 = 1.5 nM 8.82
CHEMBL3717580 — IC50 = 1.5 nM 8.82
CHEMBL5188943 — IC50 = 1.7 nM 8.77
CHEMBL3715642 — IC50 = 1.8 nM 8.74
CHEMBL3717195 — IC50 = 2.4 nM 8.62
CHEMBL3728620 — IC50 = 2.4 nM 8.62
CHEMBL5194507 — IC50 = 2.8 nM 8.55
CHEMBL3719133 — IC50 = 3.9 nM 8.41
CHEMBL5193311 — IC50 = 4.0 nM 8.40
CHEMBL3732490 — IC50 = 4.2 nM 8.38
CHEMBL3717423 — IC50 = 4.4 nM 8.36
CHEMBL3718606 — IC50 = 6.3 nM 8.20