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Assay Detail

CHEMBL869436

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

Binding
Inhibition of DNA gyrase supercoiling in Escherichia coli ATCC 25922
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

DNA gyrase (CHEMBL2094139)
Type PROTEIN COMPLEX
Organism Escherichia coli

Publication

Isothiazolopyridones: synthesis, structure, and biological activity of a new class of antibacterial agents.
Wiles JA, Hashimoto A, Thanassi JA, Cheng J, Incarvito CD, Deshpande M, Pucci MJ, Bradbury BJ.
J Med Chem (2006) 49 : 39 -42
PubMed 16392790 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.89 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200962 1 6.70
CHEMBL8 CIPROFLOXACIN 4.0 1 6.52
CHEMBL201369 1 6.40
CHEMBL9 NORFLOXACIN 4.0 1 6.22
CHEMBL201439 1 4.85
CHEMBL199517 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200962 IC50 = 200.0 nM 6.70
CHEMBL8 CIPROFLOXACIN IC50 = 300.0 nM 6.52
CHEMBL201369 IC50 = 400.0 nM 6.40
CHEMBL9 NORFLOXACIN IC50 = 600.0 nM 6.22
CHEMBL201439 IC50 = 14000.0 nM 4.85
CHEMBL199517 IC50 = 24000.0 nM 4.62