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Assay Detail

CHEMBL4121750

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

Binding
Inhibition of Aeromonas hydrophila CphA using fluorogenic cephalosporin as substrate
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Aeromonas hydrophila
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metallo-beta-lactamase type 2 (CHEMBL1169593)
Type SINGLE PROTEIN
Organism Aeromonas hydrophila

Publication

Structure activity relationship studies on rhodanines and derived enethiol inhibitors of metallo-β-lactamases.
Zhang D, Markoulides MS, Stepanovs D, Rydzik AM, El-Hussein A, Bon C, Kamps JJAG, Umland KD, Collins PM, Cahill ST, Wang DY, von Delft F, Brem J, McDonough MA, Schofield CJ.
Bioorg Med Chem (2018) 26 : 2928 -2936
PubMed 29655609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.51 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3792857 1 6.70
CHEMBL4095898 1 5.68
CHEMBL3234727 1 4.15
CHEMBL4126979 1 -
CHEMBL4068716 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3792857 IC50 = 200.0 nM 6.70
CHEMBL4095898 IC50 = 2100.0 nM 5.68
CHEMBL3234727 IC50 = 71000.0 nM 4.15
CHEMBL4126979 IC50 = 130000.0 nM -
CHEMBL4068716 IC50 > 50000.0 nM -