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Assay Detail

CHEMBL4617686

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

Binding
Inhibition of Acinetobacter baumannii OXA-23 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Acinetobacter baumannii
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-lactamase OXA-23 (CHEMBL3885669)
Type SINGLE PROTEIN
Organism Acinetobacter baumannii

Publication

Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
Hecker SJ, Reddy KR, Lomovskaya O, Griffith DC, Rubio-Aparicio D, Nelson K, Tsivkovski R, Sun D, Sabet M, Tarazi Z, Parkinson J, Totrov M, Boyer SH, Glinka TW, Pemberton OA, Chen Y, Dudley MN.
J Med Chem (2020) 63 : 7491 -7507
PubMed 32150407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.45 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4633785 XERUBORBACTAM 1.0 1 9.13
CHEMBL1689063 AVIBACTAM 4.0 1 5.77
CHEMBL3317857 VABORBACTAM 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4633785 XERUBORBACTAM Ki = 0.74 nM 9.13
CHEMBL1689063 AVIBACTAM Ki = 1700.0 nM 5.77
CHEMBL3317857 VABORBACTAM Ki > 40000.0 nM -