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Assay Detail

CHEMBL1280255

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Binding
Inhibition of Escherichia coli DNA gyrase GyrA/GyrB
4
Total Activities
4
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

Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
Matrat S, Aubry A, Mayer C, Jarlier V, Cambau E.
Antimicrob Agents Chemother (2008) 52 : 2909 -2914
PubMed 18426901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.42 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4 OFLOXACIN 4.0 1 5.82
CHEMBL32 MOXIFLOXACIN 4.0 1 5.60
CHEMBL826 ENOXACIN 4.0 1 4.85
CHEMBL5 NALIDIXIC ACID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4 OFLOXACIN IC50 = 1500.0 nM 5.82
CHEMBL32 MOXIFLOXACIN IC50 = 2500.0 nM 5.60
CHEMBL826 ENOXACIN IC50 = 14000.0 nM 4.85
CHEMBL5 NALIDIXIC ACID IC50 = 215000.0 nM -