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Assay Detail

CHEMBL660942

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

Binding
Inhibition of GC1 extended spectrum class C beta-lactamase
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Enterobacter cloacae GC1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Beta-lactamase class C (CHEMBL3499)
Type SINGLE PROTEIN
Organism Enterobacter cloacae

Publication

The synthesis and evaluation of 3-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors.
Buynak JD, Doppalapudi VR, Adam G.
Bioorg Med Chem Lett (2000) 10 : 853 -857
PubMed 10853646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.57 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL353613 1 8.00
CHEMBL354754 1 7.22
CHEMBL353422 1 7.00
CHEMBL433726 1 7.00
CHEMBL422212 1 6.89
CHEMBL167539 1 6.75
CHEMBL354758 1 6.58
CHEMBL169392 1 6.52
CHEMBL169154 1 6.05
CHEMBL353978 1 5.92
CHEMBL171049 1 4.35
CHEMBL355161 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL353613 IC50 = 10.0 nM 8.00
CHEMBL354754 IC50 = 60.0 nM 7.22
CHEMBL353422 IC50 = 100.0 nM 7.00
CHEMBL433726 IC50 = 100.0 nM 7.00
CHEMBL422212 IC50 = 130.0 nM 6.89
CHEMBL167539 IC50 = 180.0 nM 6.75
CHEMBL354758 IC50 = 260.0 nM 6.58
CHEMBL169392 IC50 = 300.0 nM 6.52
CHEMBL169154 IC50 = 900.0 nM 6.05
CHEMBL353978 IC50 = 1200.0 nM 5.92
CHEMBL171049 IC50 = 45000.0 nM 4.35
CHEMBL355161 IC50 = 150000.0 nM -