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Assay Detail

CHEMBL804369

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

Binding
Beta-Lactamase inhibitory activity against representative class A (TEM-1) serine enzyme
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Penicillin-derived inhibitors that simultaneously target both metallo- and serine-beta-lactamases.
Buynak JD, Chen H, Vogeti L, Gadhachanda VR, Buchanan CA, Palzkill T, Shaw RW, Spencer J, Walsh TR.
Bioorg Med Chem Lett (2004) 14 : 1299 -1304
PubMed 14980686 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.26 6.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1439 TAZOBACTAM SODIUM 4.0 1 6.91
CHEMBL416561 1 6.19
CHEMBL25766 1 5.17
CHEMBL24878 1 4.84
CHEMBL24235 1 4.29
CHEMBL26275 1 4.16
CHEMBL25644 1 -
CHEMBL24275 1 -
CHEMBL277857 1 -
CHEMBL277225 1 -
CHEMBL25613 1 -
CHEMBL24351 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1439 TAZOBACTAM SODIUM IC50 = 122.0 nM 6.91
CHEMBL416561 IC50 = 650.0 nM 6.19
CHEMBL25766 IC50 = 6800.0 nM 5.17
CHEMBL24878 IC50 = 14600.0 nM 4.84
CHEMBL24235 IC50 = 51700.0 nM 4.29
CHEMBL26275 IC50 = 69200.0 nM 4.16
CHEMBL25644 IC50 = 601000.0 nM -
CHEMBL24275 IC50 = 988000.0 nM -
CHEMBL277857 IC50 = 275000.0 nM -
CHEMBL277225 IC50 = 648000.0 nM -
CHEMBL25613 IC50 = 752000.0 nM -
CHEMBL24351 IC50 > 1000000.0 nM -