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Assay Detail

CHEMBL936680

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Functional
Antiviral activity against HCV 1b in human Huh7/C24 cells after 72 hrs by replicon cell assay
ChEMBL ↗
62
Total Activities
62
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

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 3: Further optimization of the 2-, 6-, and 7'-substituents and initial pharmacokinetic assessments.
Li LS, Zhou Y, Murphy DE, Stankovic N, Zhao J, Dragovich PS, Bertolini T, Sun Z, Ayida B, Tran CV, Ruebsam F, Webber SE, Shah AM, Tsan M, Showalter RE, Patel R, Lebrun LA, Bartkowski DM, Nolan TG, Norris DA, Kamran R, Brooks J, Sergeeva MV, Kirkovsky L, Zhao Q, Kissinger CR.
Bioorg Med Chem Lett (2008) 18 : 3446 -3455
PubMed 18457949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 62 6.95 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL409248 — — 1 8.40
CHEMBL259995 — — 1 8.30
CHEMBL401825 — — 1 8.30
CHEMBL256918 — — 1 8.30
CHEMBL261300 — — 1 8.30
CHEMBL259781 — — 1 8.15
CHEMBL402234 — — 1 8.15
CHEMBL403189 — — 1 8.15
CHEMBL255901 — — 1 8.10
CHEMBL259741 — — 1 8.10
CHEMBL411407 — — 1 8.05
CHEMBL257195 — — 1 7.82
CHEMBL258459 — — 1 7.80
CHEMBL257408 — — 1 7.80
CHEMBL261298 — — 1 7.72
CHEMBL265924 — — 1 7.70
CHEMBL408675 — — 1 7.64
CHEMBL411288 — — 1 7.62
CHEMBL261698 — — 1 7.52
CHEMBL256948 — — 1 7.50
CHEMBL403641 — — 1 7.47
CHEMBL258236 — — 1 7.40
CHEMBL255239 — — 1 7.39
CHEMBL257409 — — 1 7.37
CHEMBL253963 — — 1 7.34
CHEMBL261697 — — 1 7.22
CHEMBL256949 — — 1 7.16
CHEMBL256741 — — 1 7.10
CHEMBL410687 — — 1 7.00
CHEMBL254164 — — 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL409248 — EC50 = 4.0 nM 8.40
CHEMBL259995 — EC50 = 5.0 nM 8.30
CHEMBL261300 — EC50 = 5.0 nM 8.30
CHEMBL401825 — EC50 = 5.0 nM 8.30
CHEMBL256918 — EC50 = 5.0 nM 8.30
CHEMBL259781 — EC50 = 7.0 nM 8.15
CHEMBL402234 — EC50 = 7.0 nM 8.15
CHEMBL403189 — EC50 = 7.0 nM 8.15
CHEMBL255901 — EC50 = 8.0 nM 8.10
CHEMBL259741 — EC50 = 8.0 nM 8.10
CHEMBL411407 — EC50 = 9.0 nM 8.05
CHEMBL257195 — EC50 = 15.0 nM 7.82
CHEMBL258459 — EC50 = 16.0 nM 7.80
CHEMBL257408 — EC50 = 16.0 nM 7.80
CHEMBL261298 — EC50 = 19.0 nM 7.72
CHEMBL265924 — EC50 = 20.0 nM 7.70
CHEMBL408675 — EC50 = 23.0 nM 7.64
CHEMBL411288 — EC50 = 24.0 nM 7.62
CHEMBL261698 — EC50 = 30.0 nM 7.52
CHEMBL256948 — EC50 = 32.0 nM 7.50
CHEMBL403641 — EC50 = 34.0 nM 7.47
CHEMBL258236 — EC50 = 40.0 nM 7.40
CHEMBL255239 — EC50 = 41.0 nM 7.39
CHEMBL257409 — EC50 = 43.0 nM 7.37
CHEMBL253963 — EC50 = 46.0 nM 7.34
CHEMBL261697 — EC50 = 60.0 nM 7.22
CHEMBL256949 — EC50 = 69.0 nM 7.16
CHEMBL256741 — EC50 = 80.0 nM 7.10
CHEMBL410687 — EC50 = 100.0 nM 7.00
CHEMBL254164 — EC50 = 110.0 nM 6.96
CHEMBL259349 — EC50 = 120.0 nM 6.92
CHEMBL401595 — EC50 = 130.0 nM 6.89
CHEMBL254163 — EC50 = 140.0 nM 6.85
CHEMBL402125 — EC50 = 150.0 nM 6.82
CHEMBL410688 — EC50 = 160.0 nM 6.80
CHEMBL258027 — EC50 = 190.0 nM 6.72
CHEMBL259335 — EC50 = 210.0 nM 6.68
CHEMBL403642 — EC50 = 250.0 nM 6.60
CHEMBL256323 — EC50 = 260.0 nM 6.58
CHEMBL262327 — EC50 = 360.0 nM 6.44
CHEMBL399631 — EC50 = 400.0 nM 6.40
CHEMBL409672 — EC50 = 410.0 nM 6.39
CHEMBL402906 — EC50 = 420.0 nM 6.38
CHEMBL265190 — EC50 = 530.0 nM 6.28
CHEMBL262065 — EC50 = 560.0 nM 6.25
CHEMBL256324 — EC50 = 750.0 nM 6.12
CHEMBL258237 — EC50 = 760.0 nM 6.12
CHEMBL260084 — EC50 = 800.0 nM 6.10
CHEMBL258899 — EC50 = 810.0 nM 6.09
CHEMBL260083 — EC50 = 1040.0 nM 5.98