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Assay Detail

CHEMBL964675

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

Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proteinase-activated receptor 1 (CHEMBL3974)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.
Chackalamannil S, Wang Y, Greenlee WJ, Hu Z, Xia Y, Ahn HS, Boykow G, Hsieh Y, Palamanda J, Agans-Fantuzzi J, Kurowski S, Graziano M, Chintala M.
J Med Chem (2008) 51 : 3061 -3064
PubMed 18447380 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.96 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL493982 VORAPAXAR 4.0 1 8.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL493982 VORAPAXAR Ki = 1.1 nM 8.96