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Assay Detail

CHEMBL834790

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
13
Total Activities
13
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 13 7.24 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361822 1 8.00
CHEMBL368894 1 7.80
CHEMBL368960 1 7.77
CHEMBL368937 1 7.55
CHEMBL179210 1 7.54
CHEMBL270437 1 7.50
CHEMBL367890 1 7.41
CHEMBL176385 1 7.37
CHEMBL435514 1 7.34
CHEMBL368900 1 7.23
CHEMBL176063 1 6.75
CHEMBL272931 1 6.64
CHEMBL180163 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361822 IC50 = 10.0 nM 8.00
CHEMBL368894 IC50 = 16.0 nM 7.80
CHEMBL368960 IC50 = 17.0 nM 7.77
CHEMBL368937 IC50 = 28.0 nM 7.55
CHEMBL179210 IC50 = 29.0 nM 7.54
CHEMBL270437 IC50 = 32.0 nM 7.50
CHEMBL367890 IC50 = 39.0 nM 7.41
CHEMBL176385 IC50 = 43.0 nM 7.37
CHEMBL435514 IC50 = 46.0 nM 7.34
CHEMBL368900 IC50 = 59.0 nM 7.23
CHEMBL176063 IC50 = 180.0 nM 6.75
CHEMBL272931 IC50 = 230.0 nM 6.64
CHEMBL180163 IC50 = 5200.0 nM 5.28