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Assay Detail

CHEMBL652842

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Binding
Inhibitory activity against TEM-1 (class A) beta-lactamase
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

6-(1-Hydroxyalkyl)penam sulfone derivatives as inhibitors of class A and class C beta-lactamases I.
Bitha P, Li Z, Francisco GD, Rasmussen BA, Lin YI.
Bioorg Med Chem Lett (1999) 9 : 991 -996
PubMed 10230626 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.98 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416561 1 8.10
CHEMBL1206880 1 7.46
CHEMBL1439 TAZOBACTAM SODIUM 4.0 1 7.22
CHEMBL366664 1 7.04
CHEMBL403 SULBACTAM 4.0 1 5.85
CHEMBL24878 1 5.10
CHEMBL265722 1 4.51
CHEMBL177912 1 4.32
CHEMBL177463 1 4.23
CHEMBL177772 1 -
CHEMBL175189 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416561 IC50 = 8.0 nM 8.10
CHEMBL1206880 IC50 = 35.0 nM 7.46
CHEMBL1439 TAZOBACTAM SODIUM IC50 = 60.0 nM 7.22
CHEMBL366664 IC50 = 91.0 nM 7.04
CHEMBL403 SULBACTAM IC50 = 1400.0 nM 5.85
CHEMBL24878 IC50 = 8000.0 nM 5.10
CHEMBL265722 IC50 = 31000.0 nM 4.51
CHEMBL177912 IC50 = 47900.0 nM 4.32
CHEMBL177463 IC50 = 59000.0 nM 4.23
CHEMBL177772 IC50 > 334000.0 nM -
CHEMBL175189 IC50 = 204000.0 nM -