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Assay Detail

CHEMBL3380749

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

Binding
Inhibition of aureus Escherichia coli DNA gyrase A2B2 using pBR322 plasmid DNA as substrate by coupled enzyme reaction assay
3
Total Activities
3
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

Second-generation antibacterial benzimidazole ureas: discovery of a preclinical candidate with reduced metabolic liability.
Grillot AL, Le Tiran A, Shannon D, Krueger E, Liao Y, O'Dowd H, Tang Q, Ronkin S, Wang T, Waal N, Li P, Lauffer D, Sizensky E, Tanoury J, Perola E, Grossman TH, Doyle T, Hanzelka B, Jones S, Dixit V, Ewing N, Liao S, Boucher B, Jacobs M, Bennani Y, Charifson PS.
J Med Chem (2014) 57 : 8792 -8816
PubMed 25317480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.26 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356986 1 8.30
CHEMBL222333 1 8.22
CHEMBL3264033 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356986 Ki = 5.0 nM 8.30
CHEMBL222333 Ki = 6.0 nM 8.22
CHEMBL3264033 Ki < 4.0 nM -