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Assay Detail

CHEMBL651103

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

Binding
Inhibitory activity against serine beta-lactamase, PC1 (class A) derived from Staphylococcus aureus
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Staphylococcus aureus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Beta-lactamase (CHEMBL4114)
Type SINGLE PROTEIN
Organism Staphylococcus aureus

Publication

The synthesis and evaluation of 6-alkylidene-2'beta-substituted penam sulfones as beta-lactamase inhibitors.
Buynak JD, Rao AS, Doppalapudi VR, Adam G, Petersen PJ, Nidamarthy SD.
Bioorg Med Chem Lett (1999) 9 : 1997 -2002
PubMed 10450969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.61 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294608 1 6.41
CHEMBL294203 1 6.18
CHEMBL303053 1 6.16
CHEMBL304709 1 5.66
CHEMBL1439 TAZOBACTAM SODIUM 4.0 1 5.59
CHEMBL64793 1 5.14
CHEMBL61762 1 4.12
CHEMBL60220 1 -
CHEMBL59053 1 -
CHEMBL61760 1 -
CHEMBL292147 1 -
CHEMBL292093 1 -
CHEMBL59227 1 -
CHEMBL60491 1 -
CHEMBL305361 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294608 IC50 = 390.0 nM 6.41
CHEMBL294203 IC50 = 660.0 nM 6.18
CHEMBL303053 IC50 = 700.0 nM 6.16
CHEMBL304709 IC50 = 2210.0 nM 5.66
CHEMBL1439 TAZOBACTAM SODIUM IC50 = 2570.0 nM 5.59
CHEMBL64793 IC50 = 7200.0 nM 5.14
CHEMBL61762 IC50 = 76530.0 nM 4.12
CHEMBL60220 IC50 = 504000.0 nM -
CHEMBL59053 IC50 = 939700.0 nM -
CHEMBL61760 IC50 = 173000.0 nM -
CHEMBL292147 IC50 = 432000.0 nM -
CHEMBL292093 IC50 = 579000.0 nM -
CHEMBL59227 IC50 = 2100000.0 nM -
CHEMBL60491 IC50 = 108000.0 nM -
CHEMBL305361 IC50 = 116000.0 nM -