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Assay Detail

CHEMBL4054003

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

Binding
Inhibition of Pseudomonas aeruginosa 301-5473 6His-tagged VIM-2 (V27 to E268 residues) expressed in Escherichia coli BL21 Star(DE3) pLysS using nitrocefin as substrate preincubated for 5 mins followed by substrate addition by spectrophotometric analysis
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-lactamase VIM-2 (CHEMBL5798)
Type SINGLE PROTEIN
Organism Pseudomonas aeruginosa

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 23 5.11 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4066078 1 6.42
CHEMBL4089201 1 6.05
CHEMBL4087458 1 5.78
CHEMBL4090938 1 5.75
CHEMBL4104728 1 5.64
CHEMBL174367 1 5.54
CHEMBL4075406 1 5.35
CHEMBL4063031 1 5.33
CHEMBL4077011 1 5.30
CHEMBL4103833 1 5.11
CHEMBL4061495 1 5.07
CHEMBL4081245 1 4.70
CHEMBL4090030 1 4.57
CHEMBL4102909 1 4.55
CHEMBL4079577 1 4.48
CHEMBL4095160 1 4.47
CHEMBL4069211 1 4.47
CHEMBL4088285 1 4.38
CHEMBL4064978 1 4.17
CHEMBL4077556 1 -
CHEMBL4091349 1 -
CHEMBL4075324 1 -
CHEMBL4105658 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4066078 IC50 = 380.0 nM 6.42
CHEMBL4089201 IC50 = 890.0 nM 6.05
CHEMBL4087458 IC50 = 1670.0 nM 5.78
CHEMBL4090938 IC50 = 1800.0 nM 5.75
CHEMBL4104728 IC50 = 2300.0 nM 5.64
CHEMBL174367 IC50 = 2900.0 nM 5.54
CHEMBL4075406 IC50 = 4500.0 nM 5.35
CHEMBL4063031 IC50 = 4700.0 nM 5.33
CHEMBL4077011 IC50 = 5000.0 nM 5.30
CHEMBL4103833 IC50 = 7800.0 nM 5.11
CHEMBL4061495 IC50 = 8600.0 nM 5.07
CHEMBL4081245 IC50 = 20000.0 nM 4.70
CHEMBL4090030 IC50 = 27000.0 nM 4.57
CHEMBL4102909 IC50 = 28000.0 nM 4.55
CHEMBL4079577 IC50 = 33200.0 nM 4.48
CHEMBL4095160 IC50 = 34000.0 nM 4.47
CHEMBL4069211 IC50 = 34000.0 nM 4.47
CHEMBL4088285 IC50 = 42000.0 nM 4.38
CHEMBL4064978 IC50 = 67000.0 nM 4.17
CHEMBL4077556 IC50 = 133000.0 nM -
CHEMBL4091349 IC50 > 10000.0 nM -
CHEMBL4075324 IC50 > 10000.0 nM -
CHEMBL4105658 IC50 > 10000.0 nM -