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Assay Detail

CHEMBL3863832

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

Binding
Antagonist activity at PAR4 (unknown origin) assessed as inhibition of activating peptide-induced receptor activation
2
Total Activities
2
Compounds Tested
1
Activity Types
0
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

Identification of the minimum PAR4 inhibitor pharmacophore and optimization of a series of 2-methoxy-6-arylimidazo[2,1-b][1,3,4]thiadiazoles.
Temple KJ, Duvernay MT, Maeng JG, Blobaum AL, Stauffer SR, Hamm HE, Lindsley CW.
Bioorg Med Chem Lett (2016) 26 : 5481 -5486
PubMed 27777004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.77 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3931873 1 8.77
CHEMBL3715848 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3931873 IC50 = 1.69 nM 8.77
CHEMBL3715848 IC50 = 0.0043 nM -