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Assay Detail

CHEMBL5133362

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

Binding
Inhibition of Staphylococcus aureus topoisomerase 4 using pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence based microtiter plate reader assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Staphylococcus aureus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Topoisomerase IV (CHEMBL3038508)
Type PROTEIN COMPLEX
Organism Staphylococcus aureus

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 11 5.27 5.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5176331 1 5.74
CHEMBL5178214 1 5.62
CHEMBL5206355 1 5.61
CHEMBL5199813 1 5.47
CHEMBL5176348 1 5.42
CHEMBL5176134 1 5.12
CHEMBL2158050 1 5.06
CHEMBL8 CIPROFLOXACIN 4.0 1 5.04
CHEMBL5207657 1 5.00
CHEMBL5176046 1 4.99
CHEMBL5204986 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5176331 IC50 = 1810.0 nM 5.74
CHEMBL5178214 IC50 = 2410.0 nM 5.62
CHEMBL5206355 IC50 = 2470.0 nM 5.61
CHEMBL5199813 IC50 = 3360.0 nM 5.47
CHEMBL5176348 IC50 = 3820.0 nM 5.42
CHEMBL5176134 IC50 = 7640.0 nM 5.12
CHEMBL2158050 IC50 = 8800.0 nM 5.06
CHEMBL8 CIPROFLOXACIN IC50 = 9160.0 nM 5.04
CHEMBL5207657 IC50 = 9920.0 nM 5.00
CHEMBL5176046 IC50 = 10160.0 nM 4.99
CHEMBL5204986 IC50 = 12550.0 nM 4.90