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Assay Detail

CHEMBL867030

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

Functional
Inhibition of HCV RNA replication in Huh7 cells
ChEMBL ↗
36
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Hepacivirus hominis
Cell Type Huh-7
Confidence 9 — Direct single protein target
Curated By Expert

Target

RNA-directed RNA polymerase (CHEMBL4296320) ↗
Type SINGLE PROTEIN
Organism Hepacivirus hominis

Publication

3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase.
Tedesco R, Shaw AN, Bambal R, Chai D, Concha NO, Darcy MG, Dhanak D, Fitch DM, Gates A, Gerhardt WG, Halegoua DL, Han C, Hofmann GA, Johnston VK, Kaura AC, Liu N, Keenan RM, Lin-Goerke J, Sarisky RT, Wiggall KJ, Zimmerman MN, Duffy KJ.
J Med Chem (2006) 49 : 971 -983
PubMed 16451063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 6.48 7.42
EC90 18 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372357 — — 2 7.42
CHEMBL202319 — — 2 6.82
CHEMBL203426 — — 2 6.80
CHEMBL201769 — — 2 6.75
CHEMBL201385 — — 2 6.62
CHEMBL202310 — — 2 6.58
CHEMBL202317 — — 2 6.58
CHEMBL426302 — — 2 6.56
CHEMBL201690 — — 2 6.53
CHEMBL202595 — — 2 6.43
CHEMBL202513 — — 2 6.42
CHEMBL370203 — — 2 6.41
CHEMBL176058 — — 2 6.38
CHEMBL180974 — — 2 6.35
CHEMBL380686 — — 2 6.29
CHEMBL377075 — — 2 6.11
CHEMBL201406 — — 2 5.92
CHEMBL425221 — — 2 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372357 — EC50 = 38.0 nM 7.42
CHEMBL202319 — EC50 = 152.0 nM 6.82
CHEMBL203426 — EC50 = 157.0 nM 6.80
CHEMBL201769 — EC50 = 180.0 nM 6.75
CHEMBL201385 — EC50 = 241.0 nM 6.62
CHEMBL202317 — EC50 = 261.0 nM 6.58
CHEMBL202310 — EC50 = 265.0 nM 6.58
CHEMBL426302 — EC50 = 274.0 nM 6.56
CHEMBL201690 — EC50 = 298.0 nM 6.53
CHEMBL202595 — EC50 = 370.0 nM 6.43
CHEMBL202513 — EC50 = 381.0 nM 6.42
CHEMBL370203 — EC50 = 389.0 nM 6.41
CHEMBL176058 — EC50 = 417.0 nM 6.38
CHEMBL180974 — EC50 = 444.0 nM 6.35
CHEMBL380686 — EC50 = 511.0 nM 6.29
CHEMBL377075 — EC50 = 774.0 nM 6.11
CHEMBL201406 — EC50 = 1204.0 nM 5.92
CHEMBL425221 — EC50 = 2492.0 nM 5.60
CHEMBL180974 — EC90 = 3760.0 nM -
CHEMBL372357 — EC90 = 207.0 nM -
CHEMBL203426 — EC90 = 593.0 nM -
CHEMBL202595 — EC90 = 1442.0 nM -
CHEMBL202310 — EC90 = 998.0 nM -
CHEMBL425221 — EC90 = 9610.0 nM -
CHEMBL380686 — EC90 = 2411.0 nM -
CHEMBL201690 — EC90 = 1613.0 nM -
CHEMBL426302 — EC90 = 1197.0 nM -
CHEMBL201769 — EC90 = 831.0 nM -
CHEMBL201406 — EC90 = 3832.0 nM -
CHEMBL202317 — EC90 = 4953.0 nM -
CHEMBL176058 — EC90 = 1423.0 nM -
CHEMBL202319 — EC90 = 808.0 nM -
CHEMBL202513 — EC90 = 2073.0 nM -
CHEMBL201385 — EC90 = 1194.0 nM -
CHEMBL370203 — EC90 = 2529.0 nM -
CHEMBL377075 — EC90 = 1872.0 nM -