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Assay Detail

CHEMBL827871

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

Binding
In vitro inhibitory activity against porcine Na+/K+-ATPase
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Expert

Publication

Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
Van Quaquebeke E, Simon G, André A, Dewelle J, El Yazidi M, Bruyneel F, Tuti J, Nacoulma O, Guissou P, Decaestecker C, Braekman JC, Kiss R, Darro F.
J Med Chem (2005) 48 : 849 -856
PubMed 15689169 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.97 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175806 2 7.17
CHEMBL178993 1 7.12
CHEMBL369515 1 5.72
CHEMBL366906 1 5.39
CHEMBL175981 1 4.92
CHEMBL427124 1 4.30
CHEMBL360685 1 -
CHEMBL262795 1 -
CHEMBL426228 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175806 IC50 = 68.0 nM 7.17
CHEMBL175806 IC50 = 68.0 nM 7.17
CHEMBL178993 IC50 = 75.0 nM 7.12
CHEMBL369515 IC50 = 1888.0 nM 5.72
CHEMBL366906 IC50 = 4076.0 nM 5.39
CHEMBL175981 IC50 = 12105.0 nM 4.92
CHEMBL427124 IC50 = 50000.0 nM 4.30
CHEMBL360685 IC50 > 50000.0 nM -
CHEMBL262795 IC50 > 50000.0 nM -
CHEMBL426228 IC50 > 50000.0 nM -