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Assay Detail

CHEMBL863775

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

Binding
Inhibitory activity against wild type Escherichia coli gyrase
17
Total Activities
17
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

Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
Wiles JA, Wang Q, Lucien E, Hashimoto A, Song Y, Cheng J, Marlor CW, Ou Y, Podos SD, Thanassi JA, Thoma CL, Deshpande M, Pucci MJ, Bradbury BJ.
Bioorg Med Chem Lett (2006) 16 : 1272 -1276
PubMed 16337791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.38 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL202864 1 7.00
CHEMBL380520 1 7.00
CHEMBL383497 1 7.00
CHEMBL204271 1 6.70
CHEMBL8 CIPROFLOXACIN 4.0 1 6.52
CHEMBL205729 1 6.52
CHEMBL380505 1 6.52
CHEMBL32 MOXIFLOXACIN 4.0 1 6.52
CHEMBL205011 1 6.30
CHEMBL31 GATIFLOXACIN 4.0 1 6.30
CHEMBL430 GEMIFLOXACIN 4.0 1 6.30
CHEMBL438444 1 6.16
CHEMBL381395 1 6.10
CHEMBL203002 1 6.05
CHEMBL382817 1 6.00
CHEMBL380696 1 6.00
CHEMBL382560 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL202864 IC50 = 100.0 nM 7.00
CHEMBL380520 IC50 = 100.0 nM 7.00
CHEMBL383497 IC50 = 100.0 nM 7.00
CHEMBL204271 IC50 = 200.0 nM 6.70
CHEMBL8 CIPROFLOXACIN IC50 = 300.0 nM 6.52
CHEMBL205729 IC50 = 300.0 nM 6.52
CHEMBL380505 IC50 = 300.0 nM 6.52
CHEMBL32 MOXIFLOXACIN IC50 = 300.0 nM 6.52
CHEMBL205011 IC50 = 500.0 nM 6.30
CHEMBL31 GATIFLOXACIN IC50 = 500.0 nM 6.30
CHEMBL430 GEMIFLOXACIN IC50 = 500.0 nM 6.30
CHEMBL438444 IC50 = 700.0 nM 6.16
CHEMBL381395 IC50 = 800.0 nM 6.10
CHEMBL203002 IC50 = 900.0 nM 6.05
CHEMBL382817 IC50 = 1000.0 nM 6.00
CHEMBL380696 IC50 = 1000.0 nM 6.00
CHEMBL382560 IC50 = 3100.0 nM 5.51