Assay Detail
Binding
CHEMBL5524213
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Inhibition of rat NHE1 expressed in Chinese hamster ovary cells (AP-1) measured after 9 mins by BCECF-AM staining based NH4Cl pre-pulse method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Chinese hamster ovary cells (AP-1) |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of UTX-143, a selective sodium-hydrogen exchange subtype 5 inhibitor, using amiloride as a lead compound.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.21 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | — | 1 | 6.77 |
| CHEMBL945 | AMILORIDE | 4.0 | 1 | 5.68 |
| CHEMBL5555508 | — | — | 1 | 5.13 |
| CHEMBL5568323 | — | — | 1 | 5.12 |
| CHEMBL5563134 | — | — | 1 | 4.73 |
| CHEMBL5559174 | — | — | 1 | 4.68 |
| CHEMBL5556438 | — | — | 1 | 4.38 |
| CHEMBL5560204 | — | — | 1 | - |
| CHEMBL5556133 | — | — | 1 | - |
| CHEMBL5542750 | — | — | 1 | - |
| CHEMBL5567224 | — | — | 1 | - |
| CHEMBL5555889 | — | — | 1 | - |
| CHEMBL5559101 | — | — | 1 | - |
| CHEMBL5566999 | — | — | 1 | - |
| CHEMBL5563696 | — | — | 1 | - |
| CHEMBL5565656 | — | — | 1 | - |
| CHEMBL5562697 | — | — | 1 | - |
| CHEMBL5560463 | — | — | 1 | - |
| CHEMBL5562282 | — | — | 1 | - |
| CHEMBL5566603 | — | — | 1 | - |
| CHEMBL5561147 | — | — | 1 | - |
| CHEMBL5560348 | — | — | 1 | - |
| CHEMBL5561432 | — | — | 1 | - |
| CHEMBL5558607 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL945 | AMILORIDE | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL5555508 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL5568323 | — | IC50 | = | 7620.0 | nM | 5.12 |
| CHEMBL5563134 | — | IC50 | = | 18500.0 | nM | 4.73 |
| CHEMBL5559174 | — | IC50 | = | 20900.0 | nM | 4.68 |
| CHEMBL5556438 | — | IC50 | = | 41700.0 | nM | 4.38 |
| CHEMBL5560204 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5556133 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5542750 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5567224 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5555889 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL5559101 | — | IC50 | - | — | - | |
| CHEMBL5566999 | — | IC50 | - | — | - | |
| CHEMBL5563696 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL5565656 | — | IC50 | = | 249000.0 | nM | - |
| CHEMBL5562697 | — | IC50 | = | 201000.0 | nM | - |
| CHEMBL5560463 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL5562282 | — | IC50 | - | — | - | |
| CHEMBL5566603 | — | IC50 | - | — | - | |
| CHEMBL5561147 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5560348 | — | IC50 | - | — | - | |
| CHEMBL5561432 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL5558607 | — | IC50 | - | — | - |