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Assay Detail

CHEMBL5041012

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

Binding
Inhibition of Escherichia coli DNA gyrase supercoiling activity using pBR322 as substrate incubated for 30 mins by fluorimetric assay
20
Total Activities
20
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

Design and synthesis of ciprofloxacin-sulfonamide hybrids to manipulate ciprofloxacin pharmacological qualities: Potency and side effects.
Ibrahim NM, Fahim SH, Hassan M, Farag AE, Georgey HH.
Eur J Med Chem (2022) 228 : 114021 -114021
PubMed 34871841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.71 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5090088 1 6.37
CHEMBL5086095 1 6.26
CHEMBL5084320 1 6.11
CHEMBL8 CIPROFLOXACIN 4.0 1 6.08
CHEMBL5086519 1 6.05
CHEMBL5092701 1 5.96
CHEMBL5075535 1 5.91
CHEMBL5087299 1 5.90
CHEMBL5089465 1 5.88
CHEMBL5085647 1 5.88
CHEMBL5087899 1 5.84
CHEMBL5084570 1 5.71
CHEMBL5093987 1 5.70
CHEMBL5078898 1 5.54
CHEMBL5092628 1 5.45
CHEMBL5076830 1 5.25
CHEMBL5090251 1 5.23
CHEMBL5076468 1 5.20
CHEMBL5080786 1 4.89
CHEMBL5072607 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5090088 IC50 = 430.0 nM 6.37
CHEMBL5086095 IC50 = 550.0 nM 6.26
CHEMBL5084320 IC50 = 770.0 nM 6.11
CHEMBL8 CIPROFLOXACIN IC50 = 830.0 nM 6.08
CHEMBL5086519 IC50 = 900.0 nM 6.05
CHEMBL5092701 IC50 = 1100.0 nM 5.96
CHEMBL5075535 IC50 = 1240.0 nM 5.91
CHEMBL5087299 IC50 = 1270.0 nM 5.90
CHEMBL5089465 IC50 = 1320.0 nM 5.88
CHEMBL5085647 IC50 = 1330.0 nM 5.88
CHEMBL5087899 IC50 = 1440.0 nM 5.84
CHEMBL5084570 IC50 = 1950.0 nM 5.71
CHEMBL5093987 IC50 = 1990.0 nM 5.70
CHEMBL5078898 IC50 = 2870.0 nM 5.54
CHEMBL5092628 IC50 = 3560.0 nM 5.45
CHEMBL5076830 IC50 = 5650.0 nM 5.25
CHEMBL5090251 IC50 = 5860.0 nM 5.23
CHEMBL5076468 IC50 = 6310.0 nM 5.20
CHEMBL5080786 IC50 = 13000.0 nM 4.89
CHEMBL5072607 IC50 = 12800.0 nM 4.89