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Assay Detail

CHEMBL652838

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

Binding
In vitro inhibitory activity against Class B (CCRA) beta-Lactamases
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bacteroides fragilis
Confidence 9 — Direct single protein target
Curated By Expert

Target

Metallo-beta-lactamase type 2 (CHEMBL4840)
Type SINGLE PROTEIN
Organism Bacteroides fragilis

Publication

Mechanism of inactivation of beta-lactamases by novel 6-methylidene penems elucidated using electrospray ionization mass spectrometry.
Tabei K, Feng X, Venkatesan AM, Abe T, Hideki U, Mansour TS, Siegel MM.
J Med Chem (2004) 47 : 3674 -3688
PubMed 15214794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.04 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL124416 1 7.85
CHEMBL263746 1 7.18
CHEMBL122450 1 6.62
CHEMBL331090 1 6.50
CHEMBL404 TAZOBACTAM 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124416 IC50 = 14.0 nM 7.85
CHEMBL263746 IC50 = 66.0 nM 7.18
CHEMBL122450 IC50 = 240.0 nM 6.62
CHEMBL331090 IC50 = 320.0 nM 6.50
CHEMBL404 TAZOBACTAM IC50 = 400000.0 nM -