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Assay Detail

CHEMBL4054005

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

Binding
Inhibition of Klebsiella pneumoniae 6His-tagged NDM1 (G36 to R280 residues) expressed in Escherichia coli BL21 Star(DE3) pLysS using imipenem as substrate preincubated for 5 mins followed by substrate addition by spectrophotometric analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Klebsiella pneumoniae
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Metallo-β-lactamase inhibitors by bioisosteric replacement: Preparation, activity and binding.
Skagseth S, Akhter S, Paulsen MH, Muhammad Z, Lauksund S, Samuelsen Ø, Leiros HS, Bayer A.
Eur J Med Chem (2017) 135 : 159 -173
PubMed 28445786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 4.98 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4066078 1 5.75
CHEMBL4089201 1 5.66
CHEMBL4090938 1 5.60
CHEMBL4104728 1 5.54
CHEMBL4103833 1 5.23
CHEMBL4063031 1 5.18
CHEMBL4079577 1 5.15
CHEMBL4061495 1 5.07
CHEMBL4077011 1 5.00
CHEMBL4102909 1 4.92
CHEMBL174367 1 4.25
CHEMBL4090030 1 4.23
CHEMBL4069211 1 4.11
CHEMBL4064978 1 4.09
CHEMBL4105658 1 -
CHEMBL4087458 1 -
CHEMBL4091349 1 -
CHEMBL4075324 1 -
CHEMBL4075406 1 -
CHEMBL4088285 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4066078 IC50 = 1800.0 nM 5.75
CHEMBL4089201 IC50 = 2200.0 nM 5.66
CHEMBL4090938 IC50 = 2500.0 nM 5.60
CHEMBL4104728 IC50 = 2900.0 nM 5.54
CHEMBL4103833 IC50 = 5900.0 nM 5.23
CHEMBL4063031 IC50 = 6600.0 nM 5.18
CHEMBL4079577 IC50 = 7100.0 nM 5.15
CHEMBL4061495 IC50 = 8500.0 nM 5.07
CHEMBL4077011 IC50 = 10000.0 nM 5.00
CHEMBL4102909 IC50 = 12000.0 nM 4.92
CHEMBL174367 IC50 = 56000.0 nM 4.25
CHEMBL4090030 IC50 = 59000.0 nM 4.23
CHEMBL4069211 IC50 = 77000.0 nM 4.11
CHEMBL4064978 IC50 = 81000.0 nM 4.09
CHEMBL4105658 IC50 > 10000.0 nM -
CHEMBL4087458 IC50 - -
CHEMBL4091349 IC50 > 10000.0 nM -
CHEMBL4075324 IC50 > 10000.0 nM -
CHEMBL4075406 IC50 = 127000.0 nM -
CHEMBL4088285 IC50 = 144000.0 nM -