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Assay Detail

CHEMBL856671

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Functional
Inhibition of Escherichia coli gyrase
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Escherichia coli
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

DNA gyrase (CHEMBL2094139)
Type PROTEIN COMPLEX
Organism Escherichia coli

Publication

3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
Ellsworth EL, Tran TP, Showalter HD, Sanchez JP, Watson BM, Stier MA, Domagala JM, Gracheck SJ, Joannides ET, Shapiro MA, Dunham SA, Hanna DL, Huband MD, Gage JW, Bronstein JC, Liu JY, Nguyen DQ, Singh R.
J Med Chem (2006) 49 : 6435 -6438
PubMed 17064062 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.48 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8 CIPROFLOXACIN 4.0 1 6.70
CHEMBL383917 1 6.70
CHEMBL31 GATIFLOXACIN 4.0 1 6.30
CHEMBL217592 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8 CIPROFLOXACIN IC50 = 200.0 nM 6.70
CHEMBL383917 IC50 = 200.0 nM 6.70
CHEMBL31 GATIFLOXACIN IC50 = 500.0 nM 6.30
CHEMBL217592 IC50 = 600.0 nM 6.22