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Assay Detail

CHEMBL759579

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

Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 7 8.97 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267059 1 10.40
CHEMBL275946 1 9.15
CHEMBL428311 1 9.09
CHEMBL7610 RWJ-54003 1 8.89
CHEMBL269345 1 8.66
CHEMBL268328 1 8.62
CHEMBL7627 1 7.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267059 Kd = 0.04 nM 10.40
CHEMBL275946 Kd = 0.7 nM 9.15
CHEMBL428311 Kd = 0.82 nM 9.09
CHEMBL7610 RWJ-54003 Kd = 1.3 nM 8.89
CHEMBL269345 Kd = 2.2 nM 8.66
CHEMBL268328 Kd = 2.4 nM 8.62
CHEMBL7627 Kd = 10.7 nM 7.97