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Assay Detail

CHEMBL4182207

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

Binding
Inhibition of HCV genotype 1b Con1 NS3 protease infected in human HuH7 replicon cells assessed as reduction in viral replication after 4 days by luciferase reporter gene assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus (isolate Con1)
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

NS3 (CHEMBL1293269)
Type SINGLE PROTEIN
Organism Hepatitis C virus

Publication

The discovery and optimization of naphthalene-linked P2-P4 Macrocycles as inhibitors of HCV NS3 protease.
Bowsher M, Hiebert S, Li R, Wang AX, Friborg J, Yu F, Hernandez D, Wang YK, Klei H, Rajamani R, Mosure K, Knipe JO, Meanwell NA, McPhee F, Scola PM.
Bioorg Med Chem Lett (2018) 28 : 43 -48
PubMed 29162454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 8.03 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215698 1 9.70
CHEMBL4202696 1 9.52
CHEMBL4205832 1 9.22
CHEMBL4210795 1 9.00
CHEMBL2105735 ASUNAPREVIR 4.0 1 8.92
CHEMBL4204453 1 8.74
CHEMBL4210743 1 8.52
CHEMBL3933212 1 8.35
CHEMBL4209552 1 8.30
CHEMBL4211655 1 8.15
CHEMBL4213684 1 8.10
CHEMBL4207524 1 7.82
CHEMBL4216353 1 7.80
CHEMBL4211245 1 7.75
CHEMBL4212349 1 7.47
CHEMBL4211385 1 7.46
CHEMBL4216640 1 7.46
CHEMBL4215939 1 7.30
CHEMBL4217267 1 7.16
CHEMBL4207303 1 6.89
CHEMBL4217305 1 6.60
CHEMBL4212654 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215698 EC50 = 0.2 nM 9.70
CHEMBL4202696 EC50 = 0.3 nM 9.52
CHEMBL4205832 EC50 = 0.6 nM 9.22
CHEMBL4210795 EC50 = 1.0 nM 9.00
CHEMBL2105735 ASUNAPREVIR EC50 = 1.2 nM 8.92
CHEMBL4204453 EC50 = 1.8 nM 8.74
CHEMBL4210743 EC50 = 3.0 nM 8.52
CHEMBL3933212 EC50 = 4.5 nM 8.35
CHEMBL4209552 EC50 = 5.0 nM 8.30
CHEMBL4211655 EC50 = 7.0 nM 8.15
CHEMBL4213684 EC50 = 8.0 nM 8.10
CHEMBL4207524 EC50 = 15.0 nM 7.82
CHEMBL4216353 EC50 = 16.0 nM 7.80
CHEMBL4211245 EC50 = 18.0 nM 7.75
CHEMBL4212349 EC50 = 34.0 nM 7.47
CHEMBL4211385 EC50 = 35.0 nM 7.46
CHEMBL4216640 EC50 = 35.0 nM 7.46
CHEMBL4215939 EC50 = 50.0 nM 7.30
CHEMBL4217267 EC50 = 69.0 nM 7.16
CHEMBL4207303 EC50 = 130.0 nM 6.89
CHEMBL4217305 EC50 = 253.0 nM 6.60
CHEMBL4212654 EC50 = 302.0 nM 6.52