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Assay Detail

CHEMBL4386710

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Binding
Inhibition of NS5A in HCV genotype 1b Con1 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 1b
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 10.55 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4588138 — — 1 11.00
CHEMBL4587426 — — 1 10.96
CHEMBL4449384 — — 1 10.92
CHEMBL4466693 — — 1 10.89
CHEMBL3545062 VELPATASVIR 4.0 1 10.80
CHEMBL4588741 — — 1 10.80
CHEMBL4583723 — — 1 10.77
CHEMBL4536960 — — 1 10.77
CHEMBL4453135 — — 1 10.77
CHEMBL4557789 — — 1 10.77
CHEMBL4542363 — — 1 10.74
CHEMBL4450375 — — 1 10.74
CHEMBL4519639 — — 1 10.74
CHEMBL4469219 — — 1 10.74
CHEMBL4562949 — — 1 10.72
CHEMBL4467926 — — 1 10.72
CHEMBL4576714 — — 1 10.72
CHEMBL4574152 — — 1 10.70
CHEMBL4457264 — — 1 10.70
CHEMBL4547877 — — 1 10.70
CHEMBL4458486 — — 1 10.70
CHEMBL4516340 — — 1 10.68
CHEMBL4533239 — — 1 10.68
CHEMBL3914296 — — 1 10.68
CHEMBL4588951 — — 1 10.66
CHEMBL4436929 — — 1 10.66
CHEMBL4580476 — — 1 10.66
CHEMBL4565239 — — 1 10.59
CHEMBL4466791 — — 1 10.55
CHEMBL4473265 — — 1 10.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4588138 — EC50 = 0.01 nM 11.00
CHEMBL4587426 — EC50 = 0.011 nM 10.96
CHEMBL4449384 — EC50 = 0.012 nM 10.92
CHEMBL4466693 — EC50 = 0.013 nM 10.89
CHEMBL3545062 VELPATASVIR EC50 = 0.016 nM 10.80
CHEMBL4588741 — EC50 = 0.016 nM 10.80
CHEMBL4583723 — EC50 = 0.017 nM 10.77
CHEMBL4536960 — EC50 = 0.017 nM 10.77
CHEMBL4453135 — EC50 = 0.017 nM 10.77
CHEMBL4557789 — EC50 = 0.017 nM 10.77
CHEMBL4450375 — EC50 = 0.018 nM 10.74
CHEMBL4469219 — EC50 = 0.018 nM 10.74
CHEMBL4519639 — EC50 = 0.018 nM 10.74
CHEMBL4542363 — EC50 = 0.018 nM 10.74
CHEMBL4576714 — EC50 = 0.019 nM 10.72
CHEMBL4562949 — EC50 = 0.019 nM 10.72
CHEMBL4467926 — EC50 = 0.019 nM 10.72
CHEMBL4574152 — EC50 = 0.02 nM 10.70
CHEMBL4457264 — EC50 = 0.02 nM 10.70
CHEMBL4547877 — EC50 = 0.02 nM 10.70
CHEMBL4458486 — EC50 = 0.02 nM 10.70
CHEMBL4516340 — EC50 = 0.021 nM 10.68
CHEMBL3914296 — EC50 = 0.021 nM 10.68
CHEMBL4533239 — EC50 = 0.021 nM 10.68
CHEMBL4588951 — EC50 = 0.022 nM 10.66
CHEMBL4436929 — EC50 = 0.022 nM 10.66
CHEMBL4580476 — EC50 = 0.022 nM 10.66
CHEMBL4565239 — EC50 = 0.026 nM 10.59
CHEMBL4466791 — EC50 = 0.028 nM 10.55
CHEMBL4473265 — EC50 = 0.03 nM 10.52
CHEMBL4543321 — EC50 = 0.031 nM 10.51
CHEMBL4468617 — EC50 = 0.033 nM 10.48
CHEMBL4440405 — EC50 = 0.034 nM 10.47
CHEMBL4466184 — EC50 = 0.048 nM 10.32
CHEMBL4575259 — EC50 = 0.079 nM 10.10
CHEMBL4579101 — EC50 = 0.172 nM 9.76
CHEMBL4437973 — EC50 = 0.315 nM 9.50
CHEMBL4442040 — EC50 = 0.58 nM 9.24
CHEMBL4542747 — EC50 = 0.8 nM 9.10
CHEMBL4550389 — EC50 = 0.005 nM -
CHEMBL4437858 — EC50 = 0.005 nM -
CHEMBL2374220 LEDIPASVIR EC50 = 0.004 nM -