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Assay Detail

CHEMBL4015579

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

Binding
Inhibition of HCV genotype 1b NS5B replicase C316N mutant infected in human HuH7 cells assessed as reduction of viral replication after 3 days by luciferase reporter assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 1b
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.
Yeung KS, Beno BR, Parcella K, Bender JA, Grant-Young KA, Nickel A, Gunaga P, Anjanappa P, Bora RO, Selvakumar K, Rigat K, Wang YK, Liu M, Lemm J, Mosure K, Sheriff S, Wan C, Witmer M, Kish K, Hanumegowda U, Zhuo X, Shu YZ, Parker D, Haskell R, Ng A, Gao Q, Colston E, Raybon J, Grasela DM, Santone K, Gao M, Meanwell NA, Sinz M, Soars MG, Knipe JO, Roberts SB, Kadow JF.
J Med Chem (2017) 60 : 4369 -4385
PubMed 28430437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.14 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4093031 BMS-929075 1.0 1 7.75
CHEMBL4067259 1 7.50
CHEMBL4088517 1 7.46
CHEMBL4063673 1 7.34
CHEMBL4104000 1 7.29
CHEMBL4078188 1 7.26
CHEMBL4086080 1 7.20
CHEMBL4080649 1 7.20
CHEMBL4091857 1 6.96
CHEMBL4085288 1 6.86
CHEMBL4104880 1 6.82
CHEMBL4096241 1 6.71
CHEMBL4071017 1 6.51
CHEMBL4072654 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4093031 BMS-929075 EC50 = 18.0 nM 7.75
CHEMBL4067259 EC50 = 32.0 nM 7.50
CHEMBL4088517 EC50 = 35.0 nM 7.46
CHEMBL4063673 EC50 = 46.0 nM 7.34
CHEMBL4104000 EC50 = 51.0 nM 7.29
CHEMBL4078188 EC50 = 55.0 nM 7.26
CHEMBL4086080 EC50 = 63.0 nM 7.20
CHEMBL4080649 EC50 = 63.0 nM 7.20
CHEMBL4091857 EC50 = 109.0 nM 6.96
CHEMBL4085288 EC50 = 139.0 nM 6.86
CHEMBL4104880 EC50 = 150.0 nM 6.82
CHEMBL4096241 EC50 = 193.0 nM 6.71
CHEMBL4071017 EC50 = 308.0 nM 6.51
CHEMBL4072654 EC50 - -