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Assay Detail

CHEMBL4386709

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

Binding
Inhibition of NS5A in HCV genotype 1a H77 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay
ChEMBL ↗
42
Total Activities
42
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

Discovery of velpatasvir (GS-5816): A potent pan-genotypic HCV NS5A inhibitor in the single-tablet regimens Vosevi<sup>®</sup> and Epclusa<sup>®</sup>.
Link JO, Taylor JG, Trejo-Martin A, Kato D, Katana AA, Krygowski ES, Yang ZY, Zipfel S, Cottell JJ, Bacon EM, Tran CV, Yang CY, Wang Y, Wang KW, Zhao G, Cheng G, Tian Y, Gong R, Lee YJ, Yu M, Gorman E, Mogalian E, Perry JK.
Bioorg Med Chem Lett (2019) 29 : 2415 -2427
PubMed 31230974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 10.30 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4587426 — — 1 11.00
CHEMBL4467926 — — 1 10.96
CHEMBL4583723 — — 1 10.96
CHEMBL4450375 — — 1 10.96
CHEMBL4519639 — — 1 10.96
CHEMBL4547877 — — 1 10.89
CHEMBL4557789 — — 1 10.89
CHEMBL3545062 VELPATASVIR 4.0 1 10.85
CHEMBL4576714 — — 1 10.85
CHEMBL4542363 — — 1 10.82
CHEMBL4588741 — — 1 10.80
CHEMBL4536960 — — 1 10.80
CHEMBL4565239 — — 1 10.68
CHEMBL4516340 — — 1 10.66
CHEMBL4440405 — — 1 10.62
CHEMBL4436929 — — 1 10.54
CHEMBL2374220 LEDIPASVIR 4.0 1 10.51
CHEMBL4574152 — — 1 10.51
CHEMBL4562949 — — 1 10.51
CHEMBL4473265 — — 1 10.48
CHEMBL4468617 — — 1 10.46
CHEMBL4453135 — — 1 10.39
CHEMBL4543321 — — 1 10.30
CHEMBL4458486 — — 1 10.28
CHEMBL4588951 — — 1 10.26
CHEMBL4580476 — — 1 10.20
CHEMBL4466791 — — 1 10.19
CHEMBL4575259 — — 1 10.06
CHEMBL4533239 — — 1 10.06
CHEMBL4550389 — — 1 10.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4587426 — EC50 = 0.01 nM 11.00
CHEMBL4467926 — EC50 = 0.011 nM 10.96
CHEMBL4519639 — EC50 = 0.011 nM 10.96
CHEMBL4583723 — EC50 = 0.011 nM 10.96
CHEMBL4450375 — EC50 = 0.011 nM 10.96
CHEMBL4547877 — EC50 = 0.013 nM 10.89
CHEMBL4557789 — EC50 = 0.013 nM 10.89
CHEMBL3545062 VELPATASVIR EC50 = 0.014 nM 10.85
CHEMBL4576714 — EC50 = 0.014 nM 10.85
CHEMBL4542363 — EC50 = 0.015 nM 10.82
CHEMBL4588741 — EC50 = 0.016 nM 10.80
CHEMBL4536960 — EC50 = 0.016 nM 10.80
CHEMBL4565239 — EC50 = 0.021 nM 10.68
CHEMBL4516340 — EC50 = 0.022 nM 10.66
CHEMBL4440405 — EC50 = 0.024 nM 10.62
CHEMBL4436929 — EC50 = 0.029 nM 10.54
CHEMBL2374220 LEDIPASVIR EC50 = 0.031 nM 10.51
CHEMBL4574152 — EC50 = 0.031 nM 10.51
CHEMBL4562949 — EC50 = 0.031 nM 10.51
CHEMBL4473265 — EC50 = 0.033 nM 10.48
CHEMBL4468617 — EC50 = 0.035 nM 10.46
CHEMBL4453135 — EC50 = 0.041 nM 10.39
CHEMBL4543321 — EC50 = 0.05 nM 10.30
CHEMBL4458486 — EC50 = 0.053 nM 10.28
CHEMBL4588951 — EC50 = 0.055 nM 10.26
CHEMBL4580476 — EC50 = 0.063 nM 10.20
CHEMBL4466791 — EC50 = 0.065 nM 10.19
CHEMBL4575259 — EC50 = 0.087 nM 10.06
CHEMBL4533239 — EC50 = 0.087 nM 10.06
CHEMBL4550389 — EC50 = 0.092 nM 10.04
CHEMBL4466184 — EC50 = 0.093 nM 10.03
CHEMBL4457264 — EC50 = 0.15 nM 9.82
CHEMBL3914296 — EC50 = 0.156 nM 9.81
CHEMBL4579101 — EC50 = 0.185 nM 9.73
CHEMBL4466693 — EC50 = 0.22 nM 9.66
CHEMBL4437973 — EC50 = 0.32 nM 9.49
CHEMBL4542747 — EC50 = 0.38 nM 9.42
CHEMBL4469219 — EC50 = 0.528 nM 9.28
CHEMBL4442040 — EC50 = 0.75 nM 9.12
CHEMBL4588138 — EC50 = 5.99 nM 8.22
CHEMBL4437858 — EC50 = 0.008 nM -
CHEMBL4449384 — EC50 = 0.008 nM -