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Assay Detail

CHEMBL694305

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

Binding
Inhibition of histidine protein kinase (KinA) phosphorylation in the presence of response regulator (Spo0F)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Novel inhibitors of bacterial two-component systems with gram positive antibacterial activity: pharmacophore identification based on the screening hit closantel.
Hlasta DJ, Demers JP, Foleno BD, Fraga-Spano SA, Guan J, Hilliard JJ, Macielag MJ, Ohemeng KA, Sheppard CM, Sui Z, Webb GC, Weidner-Wells MA, Werblood H, Barrett JF.
Bioorg Med Chem Lett (1998) 8 : 1923 -1928
PubMed 9873460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.80 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57324 1 5.42
CHEMBL56579 1 5.32
CHEMBL57687 1 5.05
CHEMBL57656 1 4.66
CHEMBL291338 3,3',4',5-TETRACHLOROSALICYLANILIDE 4.0 1 4.35
CHEMBL56781 1 4.01
CHEMBL57828 1 -
CHEMBL57526 1 -
CHEMBL293285 1 -
CHEMBL57924 1 -
CHEMBL294403 1 -
CHEMBL301903 1 -
CHEMBL299692 1 -
CHEMBL57827 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57324 IC50 = 3800.0 nM 5.42
CHEMBL56579 IC50 = 4800.0 nM 5.32
CHEMBL57687 IC50 = 9000.0 nM 5.05
CHEMBL57656 IC50 = 22000.0 nM 4.66
CHEMBL291338 3,3',4',5-TETRACHLOROSALICYLANILIDE IC50 = 45000.0 nM 4.35
CHEMBL56781 IC50 = 98000.0 nM 4.01
CHEMBL57828 IC50 > 500000.0 nM -
CHEMBL57526 IC50 > 500000.0 nM -
CHEMBL293285 IC50 > 500000.0 nM -
CHEMBL57924 IC50 > 500000.0 nM -
CHEMBL294403 IC50 > 500000.0 nM -
CHEMBL301903 IC50 > 500000.0 nM -
CHEMBL299692 IC50 = 385000.0 nM -
CHEMBL57827 IC50 = 365000.0 nM -