Assay Detail

CHEMBL1280251

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Binding

Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB R447K mutant gene

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Mycobacterium tuberculosis
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

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	5.27	6.00

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL32	MOXIFLOXACIN	4.0	1	6.00
CHEMBL4	OFLOXACIN	4.0	1	5.16
CHEMBL826	ENOXACIN	4.0	1	4.64
CHEMBL5	NALIDIXIC ACID	4.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL32	MOXIFLOXACIN	IC50	=	1000.0	nM	6.00
CHEMBL4	OFLOXACIN	IC50	=	7000.0	nM	5.16
CHEMBL826	ENOXACIN	IC50	=	23000.0	nM	4.64
CHEMBL5	NALIDIXIC ACID	IC50	=	1080000.0	nM	-