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Assay Detail

CHEMBL4042365

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

Functional
Antiviral activity against HCV genotype 1b infected in human HuH5.2 cells with persistent I389luc-ubi-neo/NS3-3'/5.1 replicon after 72 hrs by luciferase reporter gene assay
101
Total Activities
68
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Hepacivirus hominis
Confidence 1 — Organism
Curated By Autocuration

Target

Hepatitis C virus (CHEMBL379)
Type ORGANISM
Organism Hepacivirus hominis

Publication

In silico identification, design and synthesis of novel piperazine-based antiviral agents targeting the hepatitis C virus helicase.
Bassetto M, Leyssen P, Neyts J, Yerukhimovich MM, Frick DN, Courtney-Smith M, Brancale A.
Eur J Med Chem (2017) 125 : 1115 -1131
PubMed 27810598 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 68 4.87 6.10
EC90 33 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231813 TELAPREVIR 4.0 1 6.10
CHEMBL4073039 1 5.92
CHEMBL4066868 2 5.89
CHEMBL4078074 1 5.77
CHEMBL4103386 1 5.70
CHEMBL4059548 1 5.67
CHEMBL4075921 2 5.66
CHEMBL4086891 1 5.52
CHEMBL4076316 2 5.46
CHEMBL4082636 1 5.43
CHEMBL4104767 1 5.42
CHEMBL4093709 1 5.40
CHEMBL4063334 1 5.31
CHEMBL4072741 1 5.19
CHEMBL4089207 2 5.18
CHEMBL4085961 1 5.18
CHEMBL4104740 2 5.06
CHEMBL4102345 2 5.03
CHEMBL4087121 2 5.00
CHEMBL4091436 2 5.00
CHEMBL4066918 1 4.98
CHEMBL4076772 1 4.97
CHEMBL4095027 1 4.92
CHEMBL4073008 1 4.92
CHEMBL4070921 1 4.92
CHEMBL4095326 1 4.89
CHEMBL590023 1 4.88
CHEMBL4077120 1 4.76
CHEMBL4076162 2 4.74
CHEMBL4077147 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231813 TELAPREVIR EC50 = 800.0 nM 6.10
CHEMBL4073039 EC50 = 1200.0 nM 5.92
CHEMBL4066868 EC50 = 1300.0 nM 5.89
CHEMBL4078074 EC50 = 1700.0 nM 5.77
CHEMBL4103386 EC50 = 1980.0 nM 5.70
CHEMBL4059548 EC50 = 2120.0 nM 5.67
CHEMBL4075921 EC50 = 2210.0 nM 5.66
CHEMBL4086891 EC50 = 3030.0 nM 5.52
CHEMBL4076316 EC50 = 3500.0 nM 5.46
CHEMBL4082636 EC50 = 3740.0 nM 5.43
CHEMBL4104767 EC50 = 3840.0 nM 5.42
CHEMBL4093709 EC50 = 4000.0 nM 5.40
CHEMBL4063334 EC50 = 4900.0 nM 5.31
CHEMBL4072741 EC50 = 6500.0 nM 5.19
CHEMBL4089207 EC50 = 6620.0 nM 5.18
CHEMBL4085961 EC50 = 6590.0 nM 5.18
CHEMBL4104740 EC50 = 8700.0 nM 5.06
CHEMBL4102345 EC50 = 9320.0 nM 5.03
CHEMBL4087121 EC50 = 10100.0 nM 5.00
CHEMBL4091436 EC50 = 9930.0 nM 5.00
CHEMBL4066918 EC50 = 10400.0 nM 4.98
CHEMBL4076772 EC50 = 10600.0 nM 4.97
CHEMBL4095027 EC50 = 12100.0 nM 4.92
CHEMBL4070921 EC50 = 12000.0 nM 4.92
CHEMBL4073008 EC50 = 12100.0 nM 4.92
CHEMBL4095326 EC50 = 13000.0 nM 4.89
CHEMBL590023 EC50 = 13200.0 nM 4.88
CHEMBL4077120 EC50 = 17400.0 nM 4.76
CHEMBL4076162 EC50 = 18100.0 nM 4.74
CHEMBL4077147 EC50 = 19200.0 nM 4.72
CHEMBL4067609 EC50 = 19900.0 nM 4.70
CHEMBL4076613 EC50 = 26300.0 nM 4.58
CHEMBL4076214 EC50 = 26400.0 nM 4.58
CHEMBL1444743 EC50 = 30600.0 nM 4.51
CHEMBL4078821 EC50 = 35800.0 nM 4.45
CHEMBL4075563 EC50 = 39600.0 nM 4.40
CHEMBL4086670 EC50 = 41800.0 nM 4.38
CHEMBL4068187 EC50 = 42500.0 nM 4.37
CHEMBL4073174 EC50 = 56200.0 nM 4.25
CHEMBL4102358 EC50 = 57200.0 nM 4.24
CHEMBL4068770 EC50 = 58300.0 nM 4.23
CHEMBL4076373 EC50 = 62000.0 nM 4.21
CHEMBL4097200 EC50 = 61900.0 nM 4.21
CHEMBL4094601 EC50 = 64300.0 nM 4.19
CHEMBL4077360 EC50 = 66700.0 nM 4.18
CHEMBL4064427 EC50 = 69200.0 nM 4.16
CHEMBL4076812 EC50 = 76900.0 nM 4.11
CHEMBL4087856 EC50 = 82000.0 nM 4.09
CHEMBL4063262 EC50 = 81700.0 nM 4.09
CHEMBL4089629 EC50 = 85800.0 nM 4.07