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Assay Detail

CHEMBL3580247

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

Binding
Inhibition of Escherichia coli recombinant TEM-10 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
Hecker SJ, Reddy KR, Totrov M, Hirst GC, Lomovskaya O, Griffith DC, King P, Tsivkovski R, Sun D, Sabet M, Tarazi Z, Clifton MC, Atkins K, Raymond A, Potts KT, Abendroth J, Boyer SH, Loutit JS, Morgan EE, Durso S, Dudley MN.
J Med Chem (2015) 58 : 3682 -3692
PubMed 25782055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.65 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL404 TAZOBACTAM 4.0 1 8.30
CHEMBL777 CLAVULANIC ACID 4.0 1 7.70
CHEMBL3317857 VABORBACTAM 4.0 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL404 TAZOBACTAM Ki = 5.0 nM 8.30
CHEMBL777 CLAVULANIC ACID Ki = 20.0 nM 7.70
CHEMBL3317857 VABORBACTAM Ki = 110.0 nM 6.96