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Assay Detail

CHEMBL809537

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Functional
In vitro antagonist activity against Thrombin induced gel-filtered platelet (GFP) aggregation at 0.15 nM.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
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
IC50 9 5.68 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275003 1 6.47
CHEMBL7642 RWJ-58259 1 6.43
CHEMBL428311 1 6.24
CHEMBL7610 RWJ-54003 1 6.05
CHEMBL267059 1 5.97
CHEMBL269345 1 5.63
CHEMBL275946 1 4.88
CHEMBL7627 1 4.75
CHEMBL268328 1 4.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275003 IC50 = 340.0 nM 6.47
CHEMBL7642 RWJ-58259 IC50 = 370.0 nM 6.43
CHEMBL428311 IC50 = 570.0 nM 6.24
CHEMBL7610 RWJ-54003 IC50 = 900.0 nM 6.05
CHEMBL267059 IC50 = 1060.0 nM 5.97
CHEMBL269345 IC50 = 2320.0 nM 5.63
CHEMBL275946 IC50 = 13300.0 nM 4.88
CHEMBL7627 IC50 = 17800.0 nM 4.75
CHEMBL268328 IC50 = 18200.0 nM 4.74