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Assay Detail

CHEMBL650684

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Binding
Inhibitory activity against class A Beta-lactamase TEM isolated from Enterobacter coli
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Enterobacter cloacae
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Beta-lactamase TEM (CHEMBL3652)
Type SINGLE PROTEIN
Organism Enterobacter cloacae

Publication

The synthesis and SAR of rhodanines as novel class C beta-lactamase inhibitors.
Grant EB, Guiadeen D, Baum EZ, Foleno BD, Jin H, Montenegro DA, Nelson EA, Bush K, Hlasta DJ.
Bioorg Med Chem Lett (2000) 10 : 2179 -2182
PubMed 11012024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 4.80 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL404 TAZOBACTAM 4.0 1 7.22
CHEMBL305404 1 5.06
CHEMBL69368 1 4.50
CHEMBL69612 1 4.00
CHEMBL68217 1 4.00
CHEMBL68939 1 4.00
CHEMBL68042 1 -
CHEMBL303602 1 -
CHEMBL307557 1 -
CHEMBL66070 1 -
CHEMBL302252 1 -
CHEMBL306881 1 -
CHEMBL431550 1 -
CHEMBL67876 1 -
CHEMBL66064 1 -
CHEMBL308010 1 -
CHEMBL305763 1 -
CHEMBL68578 1 -
CHEMBL69428 1 -
CHEMBL303038 1 -
CHEMBL69676 1 -
CHEMBL304529 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL404 TAZOBACTAM IC50 = 60.0 nM 7.22
CHEMBL305404 IC50 = 8700.0 nM 5.06
CHEMBL69368 IC50 = 32000.0 nM 4.50
CHEMBL69612 IC50 = 100000.0 nM 4.00
CHEMBL68217 IC50 = 100000.0 nM 4.00
CHEMBL68939 IC50 = 100000.0 nM 4.00
CHEMBL68042 IC50 > 700000.0 nM -
CHEMBL303602 IC50 = 138000.0 nM -
CHEMBL307557 IC50 = 432000.0 nM -
CHEMBL66070 IC50 > 700000.0 nM -
CHEMBL302252 IC50 > 700000.0 nM -
CHEMBL306881 IC50 > 50000.0 nM -
CHEMBL431550 IC50 > 700000.0 nM -
CHEMBL67876 IC50 > 700000.0 nM -
CHEMBL66064 IC50 > 700000.0 nM -
CHEMBL308010 IC50 = 190000.0 nM -
CHEMBL305763 IC50 > 700000.0 nM -
CHEMBL68578 IC50 > 700000.0 nM -
CHEMBL69428 IC50 > 700000.0 nM -
CHEMBL303038 IC50 > 700000.0 nM -
CHEMBL69676 IC50 > 100000.0 nM -
CHEMBL304529 IC50 > 700000.0 nM -