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Assay Detail

CHEMBL973586

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

Functional
Antiviral activity against HCV 1b Con1 isolate in human Huh7.5 cells assessed as renilla luciferase activity after 3 days by RNA replicon assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Hepacivirus hominis
Cell Type Huh-7
Confidence 1 — Organism
Curated By Autocuration

Target

Hepatitis C virus (CHEMBL379)
Type ORGANISM
Organism Hepacivirus hominis

Publication

Discovery of (R)-6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a potent and orally available hepatitis C virus polymerase inhibitor.
Li H, Tatlock J, Linton A, Gonzalez J, Jewell T, Patel L, Ludlum S, Drowns M, Rahavendran SV, Skor H, Hunter R, Shi ST, Herlihy KJ, Parge H, Hickey M, Yu X, Chau F, Nonomiya J, Lewis C.
J Med Chem (2009) 52 : 1255 -1258
PubMed 19209845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.02 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL230744 1 7.82
CHEMBL509746 1 7.80
CHEMBL515872 1 7.60
CHEMBL514640 1 7.55
CHEMBL490672 FILIBUVIR 3.0 1 7.39
CHEMBL489476 1 7.37
CHEMBL516051 1 7.23
CHEMBL490671 1 7.17
CHEMBL230743 1 7.13
CHEMBL522458 1 7.00
CHEMBL472913 1 6.82
CHEMBL522658 1 6.72
CHEMBL489295 1 6.51
CHEMBL524103 1 6.48
CHEMBL474322 1 6.23
CHEMBL472914 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL230744 EC50 = 15.0 nM 7.82
CHEMBL509746 EC50 = 16.0 nM 7.80
CHEMBL515872 EC50 = 25.0 nM 7.60
CHEMBL514640 EC50 = 28.0 nM 7.55
CHEMBL490672 FILIBUVIR EC50 = 41.0 nM 7.39
CHEMBL489476 EC50 = 43.0 nM 7.37
CHEMBL516051 EC50 = 59.0 nM 7.23
CHEMBL490671 EC50 = 67.0 nM 7.17
CHEMBL230743 EC50 = 74.0 nM 7.13
CHEMBL522458 EC50 = 100.0 nM 7.00
CHEMBL472913 EC50 = 150.0 nM 6.82
CHEMBL522658 EC50 = 190.0 nM 6.72
CHEMBL489295 EC50 = 310.0 nM 6.51
CHEMBL524103 EC50 = 330.0 nM 6.48
CHEMBL474322 EC50 = 590.0 nM 6.23
CHEMBL472914 EC50 = 2900.0 nM 5.54