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Assay Detail

CHEMBL4027657

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

Binding
Inhibition of CrtN in methicillin-resistant Staphylococcus aureus Mu50 assessed as reduction in staphyloxanthin levels after 48 hrs by spectrophotometric method-based pigment inhibition assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Staphylococcus aureus subsp. aureus Mu50
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

4,4'-diapophytoene desaturase (4,4'-diaponeurosporene-forming) (CHEMBL4105905)
Type SINGLE PROTEIN
Organism Staphylococcus aureus (strain Mu50 / ATCC 700699)

Publication

Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
Li B, Ni S, Mao F, Chen F, Liu Y, Wei H, Chen W, Zhu J, Lan L, Li J.
J Med Chem (2018) 61 : 224 -250
PubMed 29243920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.30 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4101749 1 9.40
CHEMBL3814424 1 9.40
CHEMBL4086008 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4101749 IC50 = 0.4 nM 9.40
CHEMBL3814424 IC50 = 0.4 nM 9.40
CHEMBL4086008 IC50 = 0.8 nM 9.10