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Assay Detail

CHEMBL4359200

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

Binding
Inhibition of NS5A in HCV genotype 2a con infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 2a
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 14 8.59 9.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4476378 1 9.94
CHEMBL4563742 1 9.85
CHEMBL4531684 1 9.72
CHEMBL4446161 1 9.48
CHEMBL4533823 1 9.01
CHEMBL4549709 1 8.83
CHEMBL4483702 1 8.48
CHEMBL4567354 1 8.36
CHEMBL4465921 1 8.35
CHEMBL4448604 1 8.05
CHEMBL4444885 1 7.92
CHEMBL3360467 1 7.50
CHEMBL4579455 1 7.46
CHEMBL2023898 DACLATASVIR 4.0 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4476378 EC50 = 0.1145 nM 9.94
CHEMBL4563742 EC50 = 0.1406 nM 9.85
CHEMBL4531684 EC50 = 0.1884 nM 9.72
CHEMBL4446161 EC50 = 0.3273 nM 9.48
CHEMBL4533823 EC50 = 0.9698 nM 9.01
CHEMBL4549709 EC50 = 1.471 nM 8.83
CHEMBL4483702 EC50 = 3.33 nM 8.48
CHEMBL4567354 EC50 = 4.365 nM 8.36
CHEMBL4465921 EC50 = 4.519 nM 8.35
CHEMBL4448604 EC50 = 8.912 nM 8.05
CHEMBL4444885 EC50 = 12.16 nM 7.92
CHEMBL3360467 EC50 = 31.99 nM 7.50
CHEMBL4579455 EC50 = 35.08 nM 7.46
CHEMBL2023898 DACLATASVIR EC50 = 52.85 nM 7.28