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Assay Detail

CHEMBL972700

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

Binding
Inhibition of HCV 1b BK delta21 NS5B delta21 polymerase
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 1b
Confidence 1 — Organism
Curated By Autocuration

Target

Hepatitis C virus (CHEMBL379)
Type ORGANISM
Organism Hepacivirus hominis

Publication

4-(1,1-Dioxo-1,4-dihydro-1lambda6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase.
Ellis DA, Blazel JK, Webber SE, Tran CV, Dragovich PS, Sun Z, Ruebsam F, McGuire HM, Xiang AX, Zhao J, Li LS, Zhou Y, Han Q, Kissinger CR, Showalter RE, Lardy M, Shah AM, Tsan M, Patel R, LeBrun LA, Kamran R, Bartkowski DM, Nolan TG, Norris DA, Sergeeva MV, Kirkovsky L.
Bioorg Med Chem Lett (2008) 18 : 4628 -4632
PubMed 18662878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.50 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL457611 1 7.82
CHEMBL455908 1 7.75
CHEMBL401595 1 7.64
CHEMBL524461 1 7.57
CHEMBL457176 1 7.41
CHEMBL456132 1 6.60
CHEMBL525739 1 6.36
CHEMBL513932 1 5.80
CHEMBL456343 1 5.80
CHEMBL401931 1 5.31
CHEMBL505717 1 5.05
CHEMBL498308 1 4.92
CHEMBL457175 1 -
CHEMBL456104 1 -
CHEMBL401974 1 -
CHEMBL497491 1 -
CHEMBL401825 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL457611 IC50 = 15.0 nM 7.82
CHEMBL455908 IC50 = 18.0 nM 7.75
CHEMBL401595 IC50 = 23.0 nM 7.64
CHEMBL524461 IC50 = 27.0 nM 7.57
CHEMBL457176 IC50 = 39.0 nM 7.41
CHEMBL456132 IC50 = 250.0 nM 6.60
CHEMBL525739 IC50 = 440.0 nM 6.36
CHEMBL513932 IC50 = 1600.0 nM 5.80
CHEMBL456343 IC50 = 1600.0 nM 5.80
CHEMBL401931 IC50 = 4900.0 nM 5.31
CHEMBL505717 IC50 = 9000.0 nM 5.05
CHEMBL498308 IC50 = 12000.0 nM 4.92
CHEMBL457175 IC50 < 10.0 nM -
CHEMBL456104 IC50 < 10.0 nM -
CHEMBL401974 IC50 < 10.0 nM -
CHEMBL497491 IC50 < 10.0 nM -
CHEMBL401825 IC50 < 10.0 nM -