Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL864372

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

Binding
Inhibitory activity against wild type Staphylococcus aureus topoisomerase 4
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Staphylococcus aureus
Confidence 9 — Direct single protein target
Curated By Expert

Target

DNA topoisomerase 4 subunit A (CHEMBL4088)
Type SINGLE PROTEIN
Organism Staphylococcus aureus

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 5.56 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL380520 1 6.70
CHEMBL430 GEMIFLOXACIN 4.0 1 6.52
CHEMBL202864 1 6.30
CHEMBL32 MOXIFLOXACIN 4.0 1 6.10
CHEMBL8 CIPROFLOXACIN 4.0 1 6.00
CHEMBL31 GATIFLOXACIN 4.0 1 5.92
CHEMBL383497 1 5.82
CHEMBL204271 1 5.80
CHEMBL382817 1 5.58
CHEMBL438444 1 5.57
CHEMBL380696 1 5.14
CHEMBL205011 1 5.09
CHEMBL382560 1 5.00
CHEMBL205729 1 5.00
CHEMBL380505 1 4.92
CHEMBL381395 1 4.60
CHEMBL203002 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL380520 IC50 = 200.0 nM 6.70
CHEMBL430 GEMIFLOXACIN IC50 = 300.0 nM 6.52
CHEMBL202864 IC50 = 500.0 nM 6.30
CHEMBL32 MOXIFLOXACIN IC50 = 800.0 nM 6.10
CHEMBL8 CIPROFLOXACIN IC50 = 1000.0 nM 6.00
CHEMBL31 GATIFLOXACIN IC50 = 1200.0 nM 5.92
CHEMBL383497 IC50 = 1500.0 nM 5.82
CHEMBL204271 IC50 = 1600.0 nM 5.80
CHEMBL382817 IC50 = 2600.0 nM 5.58
CHEMBL438444 IC50 = 2700.0 nM 5.57
CHEMBL380696 IC50 = 7200.0 nM 5.14
CHEMBL205011 IC50 = 8200.0 nM 5.09
CHEMBL382560 IC50 = 10000.0 nM 5.00
CHEMBL205729 IC50 = 10000.0 nM 5.00
CHEMBL380505 IC50 = 12000.0 nM 4.92
CHEMBL381395 IC50 = 25000.0 nM 4.60
CHEMBL203002 IC50 = 41000.0 nM 4.39