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Assay Detail

CHEMBL4027809

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

Binding
Inhibition of CrtN in Staphylococcus aureus Newman after 12 resistant development passages under 0.15% v/v H2O2 assessed as reduction in staphyloxanthin levels under IC90 level after 48 hrs by spectrophotometric method-based pigment inhibition assay
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

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 2 8.67 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086008 1 8.74
CHEMBL4101749 1 8.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086008 IC50 = 1.8 nM 8.74
CHEMBL4101749 IC50 = 2.6 nM 8.59