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Assay Detail

CHEMBL5133363

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

Binding
Inhibition of Escherichia coli DNA gyrase by fluorescence based microtiter plate reader assay
5
Total Activities
5
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

Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors.
Flagstad T, Pedersen MT, Jakobsen TH, Felding J, Tolker-Nielsen T, Givskov M, Qvortrup K, Nielsen TE.
Bioorg Med Chem Lett (2022) 57 : 128499 -128499
PubMed 34906671 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.45 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8 CIPROFLOXACIN 4.0 1 6.64
CHEMBL2158050 1 5.41
CHEMBL5176134 1 5.27
CHEMBL5178214 1 5.19
CHEMBL5183842 1 4.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8 CIPROFLOXACIN IC50 = 230.0 nM 6.64
CHEMBL2158050 IC50 = 3900.0 nM 5.41
CHEMBL5176134 IC50 = 5400.0 nM 5.27
CHEMBL5178214 IC50 = 6460.0 nM 5.19
CHEMBL5183842 IC50 = 18420.0 nM 4.74