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Assay Detail

CHEMBL2213722

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

Functional
Antiviral activity against HCV genotype 1b Con1 infected in human Huh7 cells assessed as inhibition of viral replication in presence of 50% NHS by HCV bicistronic replicon assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Hepacivirus hominis
Cell Type Huh-7
Confidence 1 — Organism
Curated By Autocuration

Target

Hepatitis C virus (CHEMBL379)
Type ORGANISM
Organism Hepacivirus hominis

Publication

Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.
Rudd MT, McIntyre CJ, Romano JJ, Butcher JW, Holloway MK, Bush K, Nguyen KT, Gilbert KF, Lyle TA, Liverton NJ, Wan BL, Summa V, Harper S, Rowley M, Vacca JP, Carroll SS, Burlein C, DiMuzio JM, Gates A, Graham DJ, Huang Q, Ludmerer SW, McClain S, McHale C, Stahlhut M, Fandozzi C, Taylor A, Trainor N, Olsen DB, McCauley JA.
Bioorg Med Chem Lett (2012) 22 : 7207 -7213
PubMed 23084906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.62 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203293 1 8.30
CHEMBL2203887 1 8.05
CHEMBL2203882 1 7.96
CHEMBL2203881 1 7.80
CHEMBL2203874 1 7.77
CHEMBL2203890 1 7.75
CHEMBL2203879 1 7.75
CHEMBL2203886 1 7.64
CHEMBL2203878 1 7.62
CHEMBL2203883 1 7.60
CHEMBL2203876 1 7.60
CHEMBL2203885 1 7.54
CHEMBL2203893 1 7.51
CHEMBL2203892 1 7.50
CHEMBL2203888 1 7.50
CHEMBL2203877 1 7.42
CHEMBL2203884 1 7.37
CHEMBL2203875 1 7.26
CHEMBL2203891 1 7.24
CHEMBL2203889 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203293 IC50 = 5.0 nM 8.30
CHEMBL2203887 IC50 = 9.0 nM 8.05
CHEMBL2203882 IC50 = 11.0 nM 7.96
CHEMBL2203881 IC50 = 16.0 nM 7.80
CHEMBL2203874 IC50 = 17.0 nM 7.77
CHEMBL2203890 IC50 = 18.0 nM 7.75
CHEMBL2203879 IC50 = 18.0 nM 7.75
CHEMBL2203886 IC50 = 23.0 nM 7.64
CHEMBL2203878 IC50 = 24.0 nM 7.62
CHEMBL2203883 IC50 = 25.0 nM 7.60
CHEMBL2203876 IC50 = 25.0 nM 7.60
CHEMBL2203885 IC50 = 29.0 nM 7.54
CHEMBL2203893 IC50 = 31.0 nM 7.51
CHEMBL2203892 IC50 = 32.0 nM 7.50
CHEMBL2203888 IC50 = 32.0 nM 7.50
CHEMBL2203877 IC50 = 38.0 nM 7.42
CHEMBL2203884 IC50 = 43.0 nM 7.37
CHEMBL2203875 IC50 = 55.0 nM 7.26
CHEMBL2203891 IC50 = 58.0 nM 7.24
CHEMBL2203889 IC50 = 64.0 nM 7.19