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Assay Detail

CHEMBL957239

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

Binding
Inhibition of Staphylococcus aureus DNA gyrase gyrA S84L mutant supercoiling activity assessed as effect on conversion of relaxed pBR322 DNA to supercoiled form
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

DNA gyrase subunit A (CHEMBL2424506)
Type SINGLE PROTEIN
Organism Staphylococcus aureus

Publication

Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
Cheng J, Thanassi JA, Thoma CL, Bradbury BJ, Deshpande M, Pucci MJ.
Antimicrob Agents Chemother (2007) 51 : 2445 -2453
PubMed 17502409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.48 4.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220656 1 4.67
CHEMBL219534 1 4.28
CHEMBL8 CIPROFLOXACIN 4.0 1 -
CHEMBL430 GEMIFLOXACIN 4.0 1 -
CHEMBL32 MOXIFLOXACIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220656 IC50 = 21500.0 nM 4.67
CHEMBL219534 IC50 = 52300.0 nM 4.28
CHEMBL8 CIPROFLOXACIN IC50 > 300000.0 nM -
CHEMBL430 GEMIFLOXACIN IC50 > 300000.0 nM -
CHEMBL32 MOXIFLOXACIN IC50 = 227000.0 nM -