Assay Detail
Binding
CHEMBL4037345
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant rat Na+/K+-ATPase alpha4/beta1 expressed in baculovirus infected insect Sf9 cell membranes using [gamma-32P]ATP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins in presence of Na+, K+ and Mg2+ by liquid scintillation counting
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
N+/K+ ATPase alpha-4/beta-1 (CHEMBL4106165) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Design, Synthesis, and in Vitro and in Vivo Evaluation of Ouabain Analogues as Potent and Selective Na,K-ATPase α4 Isoform Inhibitors for Male Contraception.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.61 | 10.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4092961 | — | — | 1 | 10.96 |
| CHEMBL4059538 | — | — | 1 | 9.22 |
| CHEMBL4066361 | — | — | 1 | 8.85 |
| CHEMBL111743 | STROPHANTHIDIN | — | 1 | 8.62 |
| CHEMBL4071710 | — | — | 1 | 8.40 |
| CHEMBL222863 | OUABAIN | -1.0 | 1 | 8.37 |
| CHEMBL4076623 | — | — | 1 | 8.31 |
| CHEMBL4085219 | — | — | 1 | 8.30 |
| CHEMBL1751 | DIGOXIN | 4.0 | 1 | 8.26 |
| CHEMBL4067657 | — | — | 1 | 8.00 |
| CHEMBL1075788 | CYMARIN | -1.0 | 1 | 7.92 |
| CHEMBL4072996 | — | — | 1 | 7.92 |
| CHEMBL4074239 | — | — | 1 | 7.89 |
| CHEMBL4077606 | — | — | 1 | 7.50 |
| CHEMBL4093925 | — | — | 1 | 7.50 |
| CHEMBL4072200 | — | — | 1 | 7.48 |
| CHEMBL4095064 | — | — | 1 | 7.41 |
| CHEMBL4087192 | — | — | 1 | 5.92 |
| CHEMBL4095871 | — | — | 1 | 5.68 |
| CHEMBL4095996 | — | — | 1 | 5.25 |
| CHEMBL4063601 | — | — | 1 | 4.82 |
| CHEMBL4069491 | — | — | 1 | 4.80 |
| CHEMBL4081196 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4092961 | — | IC50 | = | 0.011 | nM | 10.96 |
| CHEMBL4059538 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4066361 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL111743 | STROPHANTHIDIN | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4071710 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL222863 | OUABAIN | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4076623 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4085219 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1751 | DIGOXIN | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4067657 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1075788 | CYMARIN | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4072996 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4074239 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4077606 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4093925 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4072200 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4095064 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4087192 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4095871 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4095996 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4063601 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4069491 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4081196 | — | IC50 | = | 0.0017 | nM | - |