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Assay Detail

CHEMBL4146867

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

Binding
Inhibition of Staphylococcus aureus Newman 6His-tagged CrtN expressed in Escherichia coli BL21(DE3) assessed as 4,4'-diapophytoene accumulation by Western blot analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Staphylococcus aureus subsp. aureus str. Newman
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

4,4'-diapophytoene desaturase (4,4'-diaponeurosporene-forming) (CHEMBL3813586)
Type SINGLE PROTEIN
Organism Staphylococcus aureus (strain Newman)

Publication

Discovery of novel piperonyl derivatives as diapophytoene desaturase inhibitors for the treatment of methicillin-, vancomycin- and linezolid-resistant Staphylococcus aureus infections.
Wei H, Mao F, Ni S, Chen F, Li B, Qiu X, Hu L, Wang M, Zheng X, Zhu J, Lan L, Li J.
Eur J Med Chem (2018) 145 : 235 -251
PubMed 29328999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.38 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4162120 1 6.39
CHEMBL4161555 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4162120 IC50 = 407.8 nM 6.39
CHEMBL4161555 IC50 = 430.0 nM 6.37