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Assay Detail

CHEMBL3131503

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

Binding
Inhibition of full-length HCV NS3 protease D168V mutant
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NS3 protease (CHEMBL4296313)
Type SINGLE PROTEIN
Organism Hepacivirus C

Publication

Achiral pyrazinone-based inhibitors of the hepatitis C virus NS3 protease and drug-resistant variants with elongated substituents directed toward the S2 pocket.
Gising J, Belfrage AK, Alogheli H, Ehrenberg A, Åkerblom E, Svensson R, Artursson P, Karlén A, Danielson UH, Larhed M, Sandström A.
J Med Chem (2014) 57 : 1790 -1801
PubMed 23517538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.67 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231813 TELAPREVIR 4.0 1 8.41
CHEMBL297884 CILUPREVIR 2.0 1 6.70
CHEMBL3125634 1 6.50
CHEMBL3125635 1 5.90
CHEMBL3125620 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231813 TELAPREVIR Ki = 3.9 nM 8.41
CHEMBL297884 CILUPREVIR Ki = 200.0 nM 6.70
CHEMBL3125634 Ki = 320.0 nM 6.50
CHEMBL3125635 Ki = 1260.0 nM 5.90
CHEMBL3125620 Ki = 1520.0 nM 5.82