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Assay Detail

CHEMBL4353048

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

Binding
Inhibition of thrombin (unknown origin) using Boc-Val-Pro-Arg-AMC as substrate preincubated with enzyme for 15 mins followed by addition of substrate by fluorescence plate reader analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of small-molecular di-basic esters, amides and carbamates as flaviviral protease inhibitors.
Sundermann TR, Benzin CV, Dražić T, Klein CD.
Eur J Med Chem (2019) 176 : 187 -194
PubMed 31103899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.73 6.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4561509 1 6.28
CHEMBL590799 CAMOSTAT 3.0 1 6.11
CHEMBL4451902 1 6.10
CHEMBL3344303 1 5.39
CHEMBL4586045 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4561509 IC50 = 530.0 nM 6.28
CHEMBL590799 CAMOSTAT IC50 = 780.0 nM 6.11
CHEMBL4451902 IC50 = 800.0 nM 6.10
CHEMBL3344303 IC50 = 4080.0 nM 5.39
CHEMBL4586045 IC50 = 17600.0 nM 4.75