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Assay Detail

CHEMBL3829384

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

Binding
Inhibition of diapophytoene desaturase in Staphylococcus aureus Newman assessed as reduction in staphyloxanthin pigment formation after 48 hrs by spectrophotometry
36
Total Activities
36
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 Benzocycloalkane Derivatives Efficiently Blocking Bacterial Virulence for the Treatment of Methicillin-Resistant S. aureus (MRSA) Infections by Targeting Diapophytoene Desaturase (CrtN).
Wang Y, Di H, Chen F, Xu Y, Xiao Q, Wang X, Wei H, Lu Y, Zhang L, Zhu J, Lan L, Li J.
J Med Chem (2016) 59 : 4831 -4848
PubMed 27139780 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 7.53 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3827744 1 8.89
CHEMBL3828585 1 8.72
CHEMBL3827961 1 8.39
CHEMBL3828525 1 8.11
CHEMBL3827888 1 8.06
CHEMBL3828547 1 8.00
CHEMBL3827974 1 7.91
CHEMBL3827751 1 7.91
CHEMBL3827562 1 7.91
CHEMBL3827731 1 7.89
CHEMBL3827676 1 7.51
CHEMBL3827505 1 7.41
CHEMBL3828634 1 7.03
CHEMBL3828086 1 6.70
CHEMBL3828576 1 6.61
CHEMBL3828700 1 6.22
CHEMBL3827225 1 6.11
CHEMBL3828023 1 6.09
CHEMBL3828217 1 -
CHEMBL3827942 1 -
CHEMBL3828366 1 -
CHEMBL3828703 1 -
CHEMBL3827110 1 -
CHEMBL3827802 1 -
CHEMBL3827754 1 -
CHEMBL3827355 1 -
CHEMBL3828623 1 -
CHEMBL3827033 1 -
CHEMBL3828327 1 -
CHEMBL3827264 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3827744 IC50 = 1.3 nM 8.89
CHEMBL3828585 IC50 = 1.9 nM 8.72
CHEMBL3827961 IC50 = 4.1 nM 8.39
CHEMBL3828525 IC50 = 7.8 nM 8.11
CHEMBL3827888 IC50 = 8.8 nM 8.06
CHEMBL3828547 IC50 = 10.0 nM 8.00
CHEMBL3827974 IC50 = 12.2 nM 7.91
CHEMBL3827751 IC50 = 12.4 nM 7.91
CHEMBL3827562 IC50 = 12.2 nM 7.91
CHEMBL3827731 IC50 = 12.8 nM 7.89
CHEMBL3827676 IC50 = 31.0 nM 7.51
CHEMBL3827505 IC50 = 39.4 nM 7.41
CHEMBL3828634 IC50 = 94.5 nM 7.03
CHEMBL3828086 IC50 = 201.9 nM 6.70
CHEMBL3828576 IC50 = 245.6 nM 6.61
CHEMBL3828700 IC50 = 603.1 nM 6.22
CHEMBL3827225 IC50 = 770.1 nM 6.11
CHEMBL3828023 IC50 = 808.3 nM 6.09
CHEMBL3828692 IC50 > 2500.0 nM -
CHEMBL3827124 IC50 > 10000.0 nM -
CHEMBL3827289 IC50 > 10000.0 nM -
CHEMBL3827435 IC50 > 10000.0 nM -
CHEMBL3827460 IC50 > 10000.0 nM -
CHEMBL3828287 IC50 > 2500.0 nM -
CHEMBL3827264 IC50 > 1250.0 nM -
CHEMBL3828327 IC50 > 10000.0 nM -
CHEMBL3827033 IC50 > 50000.0 nM -
CHEMBL3828623 IC50 > 10000.0 nM -
CHEMBL3827355 IC50 > 20000.0 nM -
CHEMBL3827754 IC50 > 20000.0 nM -
CHEMBL3827802 IC50 > 20000.0 nM -
CHEMBL3827110 IC50 > 1000.0 nM -
CHEMBL3828703 IC50 > 10000.0 nM -
CHEMBL3828366 IC50 > 5000.0 nM -
CHEMBL3827942 IC50 > 1000.0 nM -
CHEMBL3828217 IC50 > 1250.0 nM -