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Assay Detail

CHEMBL4375022

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Binding
Inhibition of Staphylococcus aureus DNA gyrase
4
Total Activities
4
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

DNA gyrase (CHEMBL3038482)
Type PROTEIN COMPLEX
Organism Staphylococcus aureus

Publication

Virtual Screening Approach and Investigation of Structure-Activity Relationships To Discover Novel Bacterial Topoisomerase Inhibitors Targeting Gram-Positive and Gram-Negative Pathogens.
Magarò G, Prati F, Garofalo B, Corso G, Furlotti G, Apicella C, Mangano G, D'Atanasio N, Robinson D, Di Giorgio FP, Ombrato R.
J Med Chem (2019) 62 : 7445 -7472
PubMed 31276392 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.34 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4448131 1 8.10
CHEMBL1235773 1 7.85
CHEMBL3317856 GEPOTIDACIN 3.0 1 7.33
CHEMBL4531538 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4448131 IC50 = 8.0 nM 8.10
CHEMBL1235773 IC50 = 14.0 nM 7.85
CHEMBL3317856 GEPOTIDACIN IC50 = 47.0 nM 7.33
CHEMBL4531538 IC50 = 830.0 nM 6.08