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Assay Detail

CHEMBL657999

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Binding
Inhibitory activity against DNA gyrase enzyme was determined by supercoiling assay with Escherichia coli DNA gyrase
5
Total Activities
5
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

Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
Hubschwerlen C, Specklin JL, Baeschlin DK, Borer Y, Haefeli S, Sigwalt C, Schroeder S, Locher HH.
Bioorg Med Chem Lett (2003) 13 : 4229 -4233
PubMed 14623007 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.12 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8 CIPROFLOXACIN 4.0 1 6.30
CHEMBL134293 1 5.70
CHEMBL336059 1 5.00
CHEMBL131858 1 4.30
CHEMBL335513 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8 CIPROFLOXACIN IC50 = 500.0 nM 6.30
CHEMBL134293 IC50 = 2000.0 nM 5.70
CHEMBL336059 IC50 = 10000.0 nM 5.00
CHEMBL131858 IC50 = 50000.0 nM 4.30
CHEMBL335513 IC50 = 50000.0 nM 4.30