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Assay Detail

CHEMBL3789280

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

Binding
Inhibition of His-tagged Klebsiella pneumoniae NDM-1 expressed in Escherichia coli BL21-AI cells using imipinem as substrate
10
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Klebsiella pneumoniae
Cell Type BL21-AI
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metallo-beta-lactamase type 2 (CHEMBL1667695)
Type SINGLE PROTEIN
Organism Klebsiella pneumoniae

Publication

Fragment-based discovery of inhibitor scaffolds targeting the metallo-β-lactamases NDM-1 and VIM-2.
Christopeit T, Leiros HK.
Bioorg Med Chem Lett (2016) 26 : 1973 -1977
PubMed 26976213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 3.16 4.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1560 CAPTOPRIL 4.0 2 4.30
CHEMBL3278535 2 3.32
CHEMBL1327484 2 2.97
CHEMBL582878 2 2.71
CHEMBL1379384 2 2.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1560 CAPTOPRIL IC50 = 49800.0 nM 4.30
CHEMBL1560 CAPTOPRIL IC50 = 50118.72 nM 4.30
CHEMBL3278535 IC50 = 480000.0 nM 3.32
CHEMBL3278535 IC50 = 478630.09 nM 3.32
CHEMBL1327484 IC50 = 1071519.31 nM 2.97
CHEMBL1327484 IC50 = 1238000.0 nM 2.91
CHEMBL582878 IC50 = 1946000.0 nM 2.71
CHEMBL582878 IC50 = 1949844.6 nM 2.71
CHEMBL1379384 IC50 = 3109000.0 nM 2.51
CHEMBL1379384 IC50 = 3090295.43 nM 2.51