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Assay Detail

CHEMBL3131502

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

Binding
Inhibition of full-length HCV NS3 protease R155K mutant
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

NS3 protease (CHEMBL4296325)
Type SINGLE PROTEIN
Organism Hepatitis C virus subtype 1b

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 6.53 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297884 CILUPREVIR 2.0 1 7.62
CHEMBL231813 TELAPREVIR 4.0 1 7.09
CHEMBL3125634 1 6.38
CHEMBL3125635 1 5.81
CHEMBL3125620 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297884 CILUPREVIR Ki = 24.0 nM 7.62
CHEMBL231813 TELAPREVIR Ki = 82.0 nM 7.09
CHEMBL3125634 Ki = 420.0 nM 6.38
CHEMBL3125635 Ki = 1550.0 nM 5.81
CHEMBL3125620 Ki = 1800.0 nM 5.75