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Assay Detail

CHEMBL660914

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

Binding
Inhibition of [3H]ouabain binding to Na/K ATP-ase in dog heart muscle
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Tissue Muscle tissue
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Sodium/potassium-transporting ATPase (CHEMBL2095186)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Pregnanes that bind to the digitalis receptor: synthesis of 14-hydroxy-5 beta,14 beta-pregnane glycosides from digitoxin and digitoxigenin.
Templeton JF, Setiloane P, Kumar VP, Yan YL, Zeglam TH, LaBella FS.
J Med Chem (1991) 34 : 2778 -2782
PubMed 1895297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.67 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2092909 1 8.52
CHEMBL2092738 1 8.15
CHEMBL3085467 1 8.10
CHEMBL3085497 1 8.10
CHEMBL3085468 1 8.05
CHEMBL1453 DIGITOXIGENIN 1 7.70
CHEMBL3085496 1 7.16
CHEMBL2092910 1 7.12
CHEMBL2092911 1 6.82
CHEMBL2092826 1 6.40
CHEMBL2092827 1 6.30
CHEMBL3085471 1 6.19
CHEMBL3085500 1 6.19
CHEMBL3085469 1 6.19
CHEMBL3085501 1 6.10
CHEMBL3085470 1 6.00
CHEMBL3085502 1 5.89
CHEMBL3085578 1 5.19
CHEMBL3085579 1 4.70
CHEMBL3085498 1 4.62
CHEMBL3085499 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2092909 IC50 = 3.0 nM 8.52
CHEMBL2092738 IC50 = 7.0 nM 8.15
CHEMBL3085467 IC50 = 8.0 nM 8.10
CHEMBL3085497 IC50 = 8.0 nM 8.10
CHEMBL3085468 IC50 = 9.0 nM 8.05
CHEMBL1453 DIGITOXIGENIN IC50 = 20.0 nM 7.70
CHEMBL3085496 IC50 = 70.0 nM 7.16
CHEMBL2092910 IC50 = 75.0 nM 7.12
CHEMBL2092911 IC50 = 150.0 nM 6.82
CHEMBL2092826 IC50 = 400.0 nM 6.40
CHEMBL2092827 IC50 = 500.0 nM 6.30
CHEMBL3085471 IC50 = 650.0 nM 6.19
CHEMBL3085500 IC50 = 650.0 nM 6.19
CHEMBL3085469 IC50 = 650.0 nM 6.19
CHEMBL3085501 IC50 = 800.0 nM 6.10
CHEMBL3085470 IC50 = 1000.0 nM 6.00
CHEMBL3085502 IC50 = 1300.0 nM 5.89
CHEMBL3085578 IC50 = 6400.0 nM 5.19
CHEMBL3085579 IC50 = 20000.0 nM 4.70
CHEMBL3085498 IC50 = 24000.0 nM 4.62
CHEMBL3085499 IC50 > 200000.0 nM -