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Assay Detail

CHEMBL652843

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

Binding
Inhibitory activity against TEM-1 (class A) beta-lactamase
7
Total Activities
7
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 II.
Bitha P, Li Z, Francisco GD, Yang Y, Petersen PJ, Lenoy E, Lin YI.
Bioorg Med Chem Lett (1999) 9 : 997 -1002
PubMed 10230627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.24 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6533 1 8.22
CHEMBL6469 1 7.72
CHEMBL6461 Ro-481220 1 7.38
CHEMBL1439 TAZOBACTAM SODIUM 4.0 1 7.22
CHEMBL6678 1 7.19
CHEMBL269471 1 7.13
CHEMBL403 SULBACTAM 4.0 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6533 IC50 = 6.0 nM 8.22
CHEMBL6469 IC50 = 19.0 nM 7.72
CHEMBL6461 Ro-481220 IC50 = 42.0 nM 7.38
CHEMBL1439 TAZOBACTAM SODIUM IC50 = 60.0 nM 7.22
CHEMBL6678 IC50 = 64.0 nM 7.19
CHEMBL269471 IC50 = 74.0 nM 7.13
CHEMBL403 SULBACTAM IC50 = 1400.0 nM 5.85