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Assay Detail

CHEMBL4027656

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

Binding
Inhibition of CrtN in methicillin-resistant Staphylococcus aureus LAC USA300 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 LAC
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

4,4'-diapophytoene desaturase (4,4'-diaponeurosporene-forming) (CHEMBL4105865)
Type SINGLE PROTEIN
Organism Staphylococcus aureus (strain USA300)

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 8.46 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086008 1 8.72
CHEMBL4101749 1 8.40
CHEMBL3814424 1 8.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086008 IC50 = 1.9 nM 8.72
CHEMBL4101749 IC50 = 4.0 nM 8.40
CHEMBL3814424 IC50 = 5.5 nM 8.26