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Assay Detail

CHEMBL650776

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

Functional
Inhibition of autophosphorylation of the two-component signal transduction system kinase was measured using the KinA/Spo0F regulatory system of Bacillus subtilis.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Bacillus subtilis
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

KinA/Spo0F (sporulation kinase A/sporulation initiation phosphotransferase F) (CHEMBL2111331)
Type PROTEIN FAMILY
Organism Bacillus subtilis (strain 168)

Publication

Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria.
Macielag MJ, Demers JP, Fraga-Spano SA, Hlasta DJ, Johnson SG, Kanojia RM, Russell RK, Sui Z, Weidner-Wells MA, Werblood H, Foleno BD, Goldschmidt RM, Loeloff MJ, Webb GC, Barrett JF.
J Med Chem (1998) 41 : 2939 -2945
PubMed 9685233 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.77 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327734 1 5.55
CHEMBL12131 CLOSANTEL 2.0 1 5.42
CHEMBL98026 1 5.32
CHEMBL101786 1 5.05
CHEMBL100719 1 5.02
CHEMBL98273 1 4.72
CHEMBL57656 1 4.68
CHEMBL431272 1 4.57
CHEMBL291338 3,3',4',5-TETRACHLOROSALICYLANILIDE 4.0 1 4.35
CHEMBL319252 1 4.30
CHEMBL100688 1 4.17
CHEMBL99708 1 4.07
CHEMBL299692 1 -
CHEMBL330654 1 -
CHEMBL318371 1 -
CHEMBL319852 1 -
CHEMBL431816 1 -
CHEMBL101264 1 -
CHEMBL98743 1 -
CHEMBL100633 1 -
CHEMBL419162 1 -
CHEMBL97945 1 -
CHEMBL330397 1 -
CHEMBL319962 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327734 IC50 = 2800.0 nM 5.55
CHEMBL12131 CLOSANTEL IC50 = 3800.0 nM 5.42
CHEMBL98026 IC50 = 4800.0 nM 5.32
CHEMBL101786 IC50 = 9000.0 nM 5.05
CHEMBL100719 IC50 = 9500.0 nM 5.02
CHEMBL98273 IC50 = 19000.0 nM 4.72
CHEMBL57656 IC50 = 21000.0 nM 4.68
CHEMBL431272 IC50 = 27000.0 nM 4.57
CHEMBL291338 3,3',4',5-TETRACHLOROSALICYLANILIDE IC50 = 45000.0 nM 4.35
CHEMBL319252 IC50 = 50000.0 nM 4.30
CHEMBL100688 IC50 = 67000.0 nM 4.17
CHEMBL99708 IC50 = 86000.0 nM 4.07
CHEMBL299692 IC50 > 500000.0 nM -
CHEMBL330654 IC50 > 500000.0 nM -
CHEMBL318371 IC50 > 500000.0 nM -
CHEMBL319852 IC50 > 500000.0 nM -
CHEMBL431816 IC50 > 500000.0 nM -
CHEMBL101264 IC50 > 500000.0 nM -
CHEMBL98743 IC50 = 250000.0 nM -
CHEMBL100633 IC50 > 500000.0 nM -
CHEMBL419162 IC50 > 500000.0 nM -
CHEMBL97945 IC50 = 185000.0 nM -
CHEMBL330397 IC50 > 500000.0 nM -
CHEMBL319962 IC50 > 500000.0 nM -