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Assay Detail

CHEMBL3595969

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Binding
Inhibition of human kidney Na(+)/K(+) ATPase alpha-1 assessed as amount of Pi release after 1 hr by colorimetric method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium/potassium-transporting ATPase subunit alpha-1 (CHEMBL1807)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

γ-Benzylidene digoxin derivatives synthesis and molecular modeling: Evaluation of anticancer and the Na,K-ATPase activity effect.
Alves SL, Paixão N, Ferreira LG, Santos FR, Neves LD, Oliveira GC, Cortes VF, Salomé KS, Barison A, Santos FV, Cenzi G, Varotti FP, Oliveira SM, Taranto AG, Comar M, Silva LM, Noël F, Quintas LE, Barbosa LA, Villar JA.
Bioorg Med Chem (2015) 23 : 4397 -4404
PubMed 26122772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.84 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1751 DIGOXIN 4.0 1 6.54
CHEMBL3594278 1 6.47
CHEMBL3594276 1 6.24
CHEMBL3856118 1 5.01
CHEMBL3594280 1 4.96
CHEMBL3594277 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1751 DIGOXIN IC50 = 290.0 nM 6.54
CHEMBL3594278 IC50 = 340.0 nM 6.47
CHEMBL3594276 IC50 = 570.0 nM 6.24
CHEMBL3856118 IC50 = 9800.0 nM 5.01
CHEMBL3594280 IC50 = 11000.0 nM 4.96
CHEMBL3594277 IC50 - -