Home
Drugs
Targets
Pathways
Ontologies
Cyp450s
Adv.search
Help/FAQ

Drug-Target Interaction

Drug

show drug details
PubChem ID:124093
Structure:
Synonyms:
1-Cyclopropyl-8-(difluoromethoxy)-7-[(1R)-(1-methyl-2,3-dihydro-1H-5-isoin
1-Cyclopropyl-8-(difluoromethoxy)-7-[(1R)-(1-methyl-2,3-dihydro-1H-5-isoindolyl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid
194804-75-6
223652-82-2
223652-82-2 (MESYLATE SALT)
AC1L3XUP
AIDS-080974
AIDS080974
BMS 284756 (*Mesylate salt*)
BMS-284756 (*Mesylate salt*)
CHEMBL215303
Garenoxacin
NCGC00181770-01
T 3811
T-3811
T-3811MEa
UNII-V72H9867WB
ATC-Codes:

Target

show target details
Uniprot ID:Q7VFP2_HELHP
Synonyms:
DNA gyrase
EC-Numbers:5.99.1.3
Organism:Helicobacter hepaticus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

12384338
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of garenoxacin (BMS-284756, T-3811ME), a new desfluoroquinolone.. Dilek Ince; Xiamei Zhang; L Christine Silver; David C Hooper (2002) Antimicrobial agents and chemotherapy display abstract
We determined the target enzyme interactions of garenoxacin (BMS-284756, T-3811ME), a novel desfluoroquinolone, in Staphylococcus aureus by genetic and biochemical studies. We found garenoxacin to be four- to eightfold more active than ciprofloxacin against wild-type S. aureus. A single topoisomerase IV or gyrase mutation caused only a 2- to 4-fold increase in the MIC of garenoxacin, whereas a combination of mutations in both loci caused a substantial increase (128-fold). Overexpression of the NorA efflux pump had minimal effect on resistance to garenoxacin. With garenoxacin at twice the MIC, selection of resistant mutants (