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Assay Detail

CHEMBL857543

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

Binding
Inhibition of Na+/K+ ATPase from dog kidney
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium/potassium-transporting ATPase subunit alpha-1 (CHEMBL4838)
Type SINGLE PROTEIN
Organism Canis lupus familiaris

Publication

Synthesis, cardiotonic activity, and structure-activity relationships of 17 beta-guanylhydrazone derivatives of 5 beta-androstane-3 beta, 14 beta-diol acting on the Na+,K(+)-ATPase receptor.
Cerri A, Serra F, Ferrari P, Folpini E, Padoani G, Melloni P.
J Med Chem (1997) 40 : 3484 -3488
PubMed 9341924 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.70 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2068996 1 6.80
CHEMBL1751 DIGOXIN 4.0 1 6.30
CHEMBL1453 DIGITOXIGENIN 1 6.30
CHEMBL2068885 1 5.80
CHEMBL2069057 1 5.70
CHEMBL2068935 1 5.60
CHEMBL2069128 1 5.40
CHEMBL2068992 1 5.30
CHEMBL2068940 1 5.20
CHEMBL2068942 1 5.20
CHEMBL2068936 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2068996 IC50 = 160.0 nM 6.80
CHEMBL1751 DIGOXIN IC50 = 500.0 nM 6.30
CHEMBL1453 DIGITOXIGENIN IC50 = 500.0 nM 6.30
CHEMBL2068885 IC50 = 1580.0 nM 5.80
CHEMBL2069057 IC50 = 2000.0 nM 5.70
CHEMBL2068935 IC50 = 2500.0 nM 5.60
CHEMBL2069128 IC50 = 3980.0 nM 5.40
CHEMBL2068992 IC50 = 5000.0 nM 5.30
CHEMBL2068940 IC50 = 6310.0 nM 5.20
CHEMBL2068942 IC50 = 6310.0 nM 5.20
CHEMBL2068936 IC50 = 7940.0 nM 5.10