Assay Detail
Binding
CHEMBL3882219
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Inhibition of rat NHE-3
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 5.36 | 5.62 |
| IC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517986 | 5-(N-ETHYL-N-ISOPROPYL)AMILORIDE | — | 1 | 5.62 |
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | — | 1 | 5.62 |
| CHEMBL465179 | — | — | 1 | 4.85 |
| CHEMBL945 | AMILORIDE | 4.0 | 1 | - |
| CHEMBL355862 | ZONIPORIDE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517986 | 5-(N-ETHYL-N-ISOPROPYL)AMILORIDE | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL465179 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL945 | AMILORIDE | Ki | > | 100000.0 | nM | - |
| CHEMBL355862 | ZONIPORIDE | IC50 | > | 500000.0 | nM | - |