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Assay Detail

CHEMBL4357008

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

Binding
Inhibition of bacterial SHV-5 using cefotaxime as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bacteria
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
Liu B, Trout REL, Chu GH, McGarry D, Jackson RW, Hamrick JC, Daigle DM, Cusick SM, Pozzi C, De Luca F, Benvenuti M, Mangani S, Docquier JD, Weiss WJ, Pevear DC, Xerri L, Burns CJ.
J Med Chem (2020) 63 : 2789 -2801
PubMed 31765155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.88 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4463697 1 9.40
CHEMBL777 CLAVULANIC ACID 4.0 1 7.92
CHEMBL1689063 AVIBACTAM 4.0 1 7.89
CHEMBL404 TAZOBACTAM 4.0 1 7.82
CHEMBL3317857 VABORBACTAM 4.0 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4463697 IC50 = 0.4 nM 9.40
CHEMBL777 CLAVULANIC ACID IC50 = 12.0 nM 7.92
CHEMBL1689063 AVIBACTAM IC50 = 13.0 nM 7.89
CHEMBL404 TAZOBACTAM IC50 = 15.0 nM 7.82
CHEMBL3317857 VABORBACTAM IC50 = 440.0 nM 6.36