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Assay Detail

CHEMBL3362860

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

Binding
Inhibition of full length Hepatitis C virus genotype 1b Con1 NS3/4A by FRET assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus (isolate Con1)
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Structure-based design of a novel series of azetidine inhibitors of the hepatitis C virus NS3/4A serine protease.
Parsy C, Alexandre FR, Brandt G, Caillet C, Cappelle S, Chaves D, Convard T, Derock M, Gloux D, Griffon Y, Lallos L, Leroy F, Liuzzi M, Loi AG, Moulat L, Musiu C, Rahali H, Roques V, Seifer M, Standring D, Surleraux D.
Bioorg Med Chem Lett (2014) 24 : 4444 -4449
PubMed 25155387 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.85 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297884 CILUPREVIR 2.0 1 9.10
CHEMBL3326826 1 8.89
CHEMBL3326830 1 8.68
CHEMBL3326539 1 8.46
CHEMBL3326829 1 8.18
CHEMBL3326540 1 7.78
CHEMBL3326538 1 7.35
CHEMBL3326537 1 6.56
CHEMBL3326536 1 5.62
CHEMBL3326827 1 -
CHEMBL3326828 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297884 CILUPREVIR IC50 = 0.8 nM 9.10
CHEMBL3326826 IC50 = 1.3 nM 8.89
CHEMBL3326830 IC50 = 2.1 nM 8.68
CHEMBL3326539 IC50 = 3.5 nM 8.46
CHEMBL3326829 IC50 = 6.6 nM 8.18
CHEMBL3326540 IC50 = 16.8 nM 7.78
CHEMBL3326538 IC50 = 45.0 nM 7.35
CHEMBL3326537 IC50 = 278.0 nM 6.56
CHEMBL3326536 IC50 = 2400.0 nM 5.62
CHEMBL3326827 IC50 < 1000.0 nM -
CHEMBL3326828 IC50 < 1000.0 nM -