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Assay Detail

CHEMBL3860118

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

Binding
Binding affinity to native signal deficient and TEV cleavage site containing His-tagged Klebsiella pneumoniae OXA-48 expressed in Escherichia coli assessed as dissociation constant by SPR assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

OXA-48 (CHEMBL1287604)
Type SINGLE PROTEIN
Organism Klebsiella pneumoniae

Publication

Screening and Design of Inhibitor Scaffolds for the Antibiotic Resistance Oxacillinase-48 (OXA-48) through Surface Plasmon Resonance Screening.
Lund BA, Christopeit T, Guttormsen Y, Bayer A, Leiros HK.
J Med Chem (2016) 59 : 5542 -5554
PubMed 27165692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 18 5.19 6.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127 MEROPENEM 4.0 1 6.07
CHEMBL3910343 1 4.30
CHEMBL3913021 1 -
CHEMBL3896367 1 -
CHEMBL3967375 1 -
CHEMBL1834963 1 -
CHEMBL1327484 1 -
CHEMBL582878 1 -
CHEMBL2018158 1 -
CHEMBL3950623 1 -
CHEMBL107518 1 -
CHEMBL109074 1 -
CHEMBL123234 1 -
CHEMBL3908259 1 -
CHEMBL3931620 1 -
CHEMBL541 BENZOIC ACID -1.0 1 -
CHEMBL72628 2-PICOLINIC ACID 1 -
CHEMBL3951674 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127 MEROPENEM Kd = 850.0 nM 6.07
CHEMBL3910343 Kd = 50000.0 nM 4.30
CHEMBL3913021 Kd = 280000.0 nM -
CHEMBL3896367 Kd = 280000.0 nM -
CHEMBL3967375 Kd = 310000.0 nM -
CHEMBL1834963 Kd - -
CHEMBL1327484 Kd - -
CHEMBL582878 Kd = 430000.0 nM -
CHEMBL2018158 Kd = 1380000.0 nM -
CHEMBL3950623 Kd = 1180000.0 nM -
CHEMBL107518 Kd = 660000.0 nM -
CHEMBL109074 Kd > 1000000.0 nM -
CHEMBL123234 Kd = 370000.0 nM -
CHEMBL3908259 Kd = 330000.0 nM -
CHEMBL3931620 Kd > 1000000.0 nM -
CHEMBL541 BENZOIC ACID Kd > 1000000.0 nM -
CHEMBL72628 2-PICOLINIC ACID Kd > 1000000.0 nM -
CHEMBL3951674 Kd = 700000.0 nM -