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Assay Detail

CHEMBL5366113

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

Binding
Inhibition of C-terminal 6His-tagged full length NDM-1 (unknown origin) expressed in Escherichia coli BL21-DE3 using nitrocefin as substrate incubated for 15 mins followed by substrate addition by absorbance based microplate reader analysis
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metallo-beta-lactamase type 2 (CHEMBL5465386)
Type SINGLE PROTEIN
Organism Bacteria

Publication

Kinetics, Thermodynamics, and Structural Effects of Quinoline-2-Carboxylates, Zinc-Binding Inhibitors of New Delhi Metallo-β-lactamase-1 Re-sensitizing Multidrug-Resistant Bacteria for Carbapenems.
Jia Y, Schroeder B, Pfeifer Y, Fröhlich C, Deng L, Arkona C, Kuropka B, Sticht J, Ataka K, Bergemann S, Wolber G, Nitsche C, Mielke M, Leiros HS, Werner G, Rademann J.
J Med Chem (2023) 66 : 11761 -11791
PubMed 37585683 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 5.85 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5436058 1 6.68
CHEMBL5434850 1 6.64
CHEMBL5429713 1 6.60
CHEMBL5421632 1 6.55
CHEMBL5421999 1 6.54
CHEMBL5409968 1 6.54
CHEMBL5425851 1 6.52
CHEMBL5434080 1 6.43
CHEMBL5436857 1 6.43
CHEMBL5424619 1 6.39
CHEMBL5394233 1 6.36
CHEMBL5423672 1 6.36
CHEMBL5418994 1 6.35
CHEMBL5426105 1 6.34
CHEMBL5432742 1 6.33
CHEMBL5425950 1 6.32
CHEMBL5393815 1 6.30
CHEMBL5416932 1 6.28
CHEMBL5408328 1 6.27
CHEMBL5415172 1 6.25
CHEMBL5408921 1 6.17
CHEMBL5402652 1 6.15
CHEMBL5397784 1 6.15
CHEMBL5417195 1 6.12
CHEMBL5405077 1 6.08
CHEMBL5426400 1 6.05
CHEMBL5427511 1 6.02
CHEMBL5435754 1 6.00
CHEMBL5414788 1 5.89
CHEMBL5430671 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5436058 IC50 = 210.0 nM 6.68
CHEMBL5434850 IC50 = 230.0 nM 6.64
CHEMBL5429713 IC50 = 250.0 nM 6.60
CHEMBL5421632 IC50 = 280.0 nM 6.55
CHEMBL5421999 IC50 = 290.0 nM 6.54
CHEMBL5409968 IC50 = 290.0 nM 6.54
CHEMBL5425851 IC50 = 300.0 nM 6.52
CHEMBL5434080 IC50 = 370.0 nM 6.43
CHEMBL5436857 IC50 = 370.0 nM 6.43
CHEMBL5424619 IC50 = 410.0 nM 6.39
CHEMBL5394233 IC50 = 440.0 nM 6.36
CHEMBL5423672 IC50 = 440.0 nM 6.36
CHEMBL5418994 IC50 = 450.0 nM 6.35
CHEMBL5426105 IC50 = 460.0 nM 6.34
CHEMBL5432742 IC50 = 470.0 nM 6.33
CHEMBL5425950 IC50 = 480.0 nM 6.32
CHEMBL5393815 IC50 = 500.0 nM 6.30
CHEMBL5416932 IC50 = 520.0 nM 6.28
CHEMBL5408328 IC50 = 540.0 nM 6.27
CHEMBL5415172 IC50 = 560.0 nM 6.25
CHEMBL5408921 IC50 = 680.0 nM 6.17
CHEMBL5402652 IC50 = 710.0 nM 6.15
CHEMBL5397784 IC50 = 710.0 nM 6.15
CHEMBL5417195 IC50 = 750.0 nM 6.12
CHEMBL5405077 IC50 = 830.0 nM 6.08
CHEMBL5426400 IC50 = 900.0 nM 6.05
CHEMBL5427511 IC50 = 950.0 nM 6.02
CHEMBL5435754 IC50 = 1000.0 nM 6.00
CHEMBL5414788 IC50 = 1280.0 nM 5.89
CHEMBL5430671 IC50 = 1410.0 nM 5.85
CHEMBL5436726 IC50 = 1400.0 nM 5.85
CHEMBL5422140 IC50 = 1400.0 nM 5.85
CHEMBL5412136 IC50 = 1470.0 nM 5.83
CHEMBL1321754 IC50 = 1600.0 nM 5.80
CHEMBL5439532 IC50 = 1640.0 nM 5.79
CHEMBL5432778 IC50 = 1700.0 nM 5.77
CHEMBL5423006 IC50 = 2100.0 nM 5.68
CHEMBL86754 IODOQUINOL IC50 = 2500.0 nM 5.60
CHEMBL497 CLIOQUINOL IC50 = 3000.0 nM 5.52
CHEMBL223448 BROXYQUINOLINE IC50 = 4200.0 nM 5.38
CHEMBL1200596 CHLOROXINE IC50 = 4900.0 nM 5.31
CHEMBL5418575 IC50 = 6200.0 nM 5.21
CHEMBL284104 DIPICOLINIC ACID IC50 = 7000.0 nM 5.16
CHEMBL5404428 IC50 = 7200.0 nM 5.14
CHEMBL1368601 IC50 = 9100.0 nM 5.04
CHEMBL5265803 IC50 = 11200.0 nM 4.95
CHEMBL5279638 IC50 = 13700.0 nM 4.86
CHEMBL5413714 IC50 = 17600.0 nM 4.75
CHEMBL5415337 IC50 = 22700.0 nM 4.64
CHEMBL5437131 IC50 = 27800.0 nM 4.56