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Assay Detail

CHEMBL894371

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

Binding
Inhibition of Escherichia coli TEM1
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Beta-lactamase TEM (CHEMBL2065)
Type SINGLE PROTEIN
Organism Escherichia coli

Publication

4-Substituted trinems as broad spectrum beta-lactamase inhibitors: structure-based design, synthesis, and biological activity.
Plantan I, Selic L, Mesar T, Anderluh PS, Oblak M, Prezelj A, Hesse L, Andrejasic M, Vilar M, Turk D, Kocijan A, Prevec T, Vilfan G, Kocjan D, Copar A, Urleb U, Solmajer T.
J Med Chem (2007) 50 : 4113 -4121
PubMed 17665896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.57 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396998 1 7.92
CHEMBL404 TAZOBACTAM 4.0 1 7.77
CHEMBL397438 1 7.75
CHEMBL395017 1 7.68
CHEMBL230859 1 7.66
CHEMBL777 CLAVULANIC ACID 4.0 1 7.52
CHEMBL230332 1 7.50
CHEMBL396753 1 7.41
CHEMBL396509 1 7.26
CHEMBL230226 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396998 IC50 = 12.0 nM 7.92
CHEMBL404 TAZOBACTAM IC50 = 17.0 nM 7.77
CHEMBL397438 IC50 = 18.0 nM 7.75
CHEMBL395017 IC50 = 21.0 nM 7.68
CHEMBL230859 IC50 = 22.0 nM 7.66
CHEMBL777 CLAVULANIC ACID IC50 = 30.0 nM 7.52
CHEMBL230332 IC50 = 32.0 nM 7.50
CHEMBL396753 IC50 = 39.0 nM 7.41
CHEMBL396509 IC50 = 55.0 nM 7.26
CHEMBL230226 IC50 = 57.0 nM 7.24