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Assay Detail

CHEMBL4359198

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

Binding
Inhibition of NS5A in HCV genotype 1a infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 1a
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Nonstructural protein 5A (CHEMBL3307224)
Type SINGLE PROTEIN
Organism Hepatitis C virus

Publication

GSK2818713, a Novel Biphenylene Scaffold-Based Hepatitis C NS5A Replication Complex Inhibitor with Broad Genotype Coverage.
Kazmierski WM, Baskaran S, Walker JT, Miriyala N, Meesala R, Beesu M, Adjabeng G, Grimes RM, Hamatake R, Leivers MR, Crosby R, Xia B, Remlinger K.
J Med Chem (2020) 63 : 4155 -4170
PubMed 32202782 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 10.43 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4563742 1 10.96
CHEMBL4471986 1 10.93
CHEMBL4533823 1 10.89
CHEMBL4531684 1 10.87
CHEMBL4436027 1 10.78
CHEMBL4567354 1 10.70
CHEMBL4483702 1 10.70
CHEMBL4440257 1 10.53
CHEMBL4561734 1 10.53
CHEMBL2023898 DACLATASVIR 4.0 1 10.49
CHEMBL4548808 1 10.38
CHEMBL3360467 1 10.36
CHEMBL4549709 1 10.27
CHEMBL4448604 1 10.26
CHEMBL4472037 1 10.09
CHEMBL4466702 1 9.83
CHEMBL4446161 1 9.61
CHEMBL4579455 1 9.52
CHEMBL4465921 1 -
CHEMBL4444885 1 -
CHEMBL4476378 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4563742 EC50 = 0.011 nM 10.96
CHEMBL4471986 EC50 = 0.0117 nM 10.93
CHEMBL4533823 EC50 = 0.0129 nM 10.89
CHEMBL4531684 EC50 = 0.0135 nM 10.87
CHEMBL4436027 EC50 = 0.0167 nM 10.78
CHEMBL4567354 EC50 = 0.02 nM 10.70
CHEMBL4483702 EC50 = 0.0201 nM 10.70
CHEMBL4440257 EC50 = 0.0293 nM 10.53
CHEMBL4561734 EC50 = 0.0297 nM 10.53
CHEMBL2023898 DACLATASVIR EC50 = 0.0324 nM 10.49
CHEMBL4548808 EC50 = 0.0414 nM 10.38
CHEMBL3360467 EC50 = 0.044 nM 10.36
CHEMBL4549709 EC50 = 0.0531 nM 10.27
CHEMBL4448604 EC50 = 0.055 nM 10.26
CHEMBL4472037 EC50 = 0.0807 nM 10.09
CHEMBL4466702 EC50 = 0.1479 nM 9.83
CHEMBL4446161 EC50 = 0.2483 nM 9.61
CHEMBL4579455 EC50 = 0.302 nM 9.52
CHEMBL4465921 EC50 = 0.0099 nM -
CHEMBL4444885 EC50 = 0.0091 nM -
CHEMBL4476378 EC50 = 0.0099 nM -