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Assay Detail

CHEMBL1282385

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

Binding
Inhibition of DNA supercoiling activity of Escherichia coli DNA gyrase gyrA G81C mutant
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

DNA gyrase subunit A (CHEMBL1858)
Type SINGLE PROTEIN
Organism Escherichia coli K-12

Publication

Comparison of in vitro activities of fluoroquinolone-like 2,4- and 1,3-diones.
Oppegard LM, Streck KR, Rosen JD, Schwanz HA, Drlica K, Kerns RJ, Hiasa H.
Antimicrob Agents Chemother (2010) 54 : 3011 -3014
PubMed 20404126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.22 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276635 1 5.92
CHEMBL1276667 1 5.77
CHEMBL1276666 1 5.37
CHEMBL8 CIPROFLOXACIN 4.0 1 4.55
CHEMBL1276697 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276635 IC50 = 1200.0 nM 5.92
CHEMBL1276667 IC50 = 1700.0 nM 5.77
CHEMBL1276666 IC50 = 4300.0 nM 5.37
CHEMBL8 CIPROFLOXACIN IC50 = 28000.0 nM 4.55
CHEMBL1276697 IC50 = 31000.0 nM 4.51