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Assay Detail

CHEMBL834775

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

Functional
Inhibitory concentration against gel filtered platelet aggregation induced by alpha thrombin
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 1 — Organism
Curated By Intermediate

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
Costanzo MJ, Almond HR, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Corcoran TW, Giardino EC, Kauffman JA, Lewis JM, de Garavilla L, Haertlein BJ, Maryanoff BE.
J Med Chem (2005) 48 : 1984 -2008
PubMed 15771442 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.40 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL257898 1 7.80
CHEMBL363003 1 7.77
CHEMBL175620 1 7.66
CHEMBL361379 1 7.47
CHEMBL401737 1 7.43
CHEMBL176348 1 7.33
CHEMBL175612 1 7.12
CHEMBL273196 EFEGATRAN 2.0 1 7.08
CHEMBL367973 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL257898 IC50 = 16.0 nM 7.80
CHEMBL363003 IC50 = 17.0 nM 7.77
CHEMBL175620 IC50 = 22.0 nM 7.66
CHEMBL361379 IC50 = 34.0 nM 7.47
CHEMBL401737 IC50 = 37.0 nM 7.43
CHEMBL176348 IC50 = 47.0 nM 7.33
CHEMBL175612 IC50 = 76.0 nM 7.12
CHEMBL273196 EFEGATRAN IC50 = 83.0 nM 7.08
CHEMBL367973 IC50 = 120.0 nM 6.92