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Assay Detail

CHEMBL759580

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

Functional
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.
Zhang HC, Derian CK, Andrade-Gordon P, Hoekstra WJ, McComsey DF, White KB, Poulter BL, Addo MF, Cheung WM, Damiano BP, Oksenberg D, Reynolds EE, Pandey A, Scarborough RM, Maryanoff BE.
J Med Chem (2001) 44 : 1021 -1024
PubMed 11297447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 9.36 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275003 1 9.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275003 Kd = 0.44 nM 9.36