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Assay Detail

CHEMBL5318755

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

Binding
Inhibition of Escherichia coli DNA gyrase incubated for 30 mins by fluorescence based assay
2
Total Activities
2
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

Discovery and Hit-to-Lead Optimization of Benzothiazole Scaffold-Based DNA Gyrase Inhibitors with Potent Activity against <i>Acinetobacter baumannii</i> and <i>Pseudomonas aeruginosa</i>.
Cotman AE, Durcik M, Benedetto Tiz D, Fulgheri F, Secci D, Sterle M, Možina Š, Skok Ž, Zidar N, Zega A, Ilaš J, Peterlin Mašič L, Tomašič T, Hughes D, Huseby DL, Cao S, Garoff L, Berruga Fernández T, Giachou P, Crone L, Simoff I, Svensson R, Birnir B, Korol SV, Jin Z, Vicente F, Ramos MC, de la Cruz M, Glinghammar B, Lenhammar L, Henderson SR, Mundy JEA, Maxwell A, Stevenson CEM, Lawson DM, Janssen GV, Sterk GJ, Kikelj D.
J Med Chem (2023) 66 : 1380 -1425
PubMed 36634346 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.79 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4854181 1 9.10
CHEMBL4873935 1 8.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4854181 IC50 = 0.8 nM 9.10
CHEMBL4873935 IC50 = 3.3 nM 8.48