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Assay Detail

CHEMBL4602773

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

Binding
Inhibition of HCV NS3/4a protease using Ac-DE-Dap(QXL520)-EE-Abu-shi-[COO]AS-C(5-FAMsp)-NH2 as substrate after 15 mins
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Hepatitis C virus serine protease, NS3/NS4A (CHEMBL2095231)
Type PROTEIN COMPLEX
Organism Hepatitis C virus

Publication

A review on HCV inhibitors: Significance of non-structural polyproteins.
Ganta NM, Gedda G, Rathnakar B, Satyanarayana M, Yamajala B, Ahsan MJ, Jadav SS, Balaraju T.
Eur J Med Chem (2019) 164 : 576 -601
PubMed 30639895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.97 9.70
Ki 1 8.22 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL258734 DANOPREVIR 3.0 1 9.70
CHEMBL2063090 GRAZOPREVIR ANHYDROUS 4.0 1 8.70
CHEMBL4287268 1 8.52
CHEMBL1255891 NARLAPREVIR 3.0 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL258734 DANOPREVIR IC50 = 0.2 nM 9.70
CHEMBL2063090 GRAZOPREVIR ANHYDROUS IC50 = 2.0 nM 8.70
CHEMBL4287268 IC50 = 3.0 nM 8.52
CHEMBL1255891 NARLAPREVIR Ki = 6.0 nM 8.22