Assay Detail
Functional
CHEMBL746894
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Screened in AP1 cells expressing human NHE-1 for sodium hydrogen exchange activity
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | AP1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Arylcyclopropanecarboxyl guanidines as novel, potent, and selective inhibitors of the sodium hydrogen exchanger isoform-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.01 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419578 | — | — | 1 | 8.52 |
| CHEMBL112903 | — | — | 1 | 8.30 |
| CHEMBL113443 | — | — | 1 | 8.30 |
| CHEMBL51363 | — | — | 1 | 8.22 |
| CHEMBL51879 | — | — | 1 | 8.05 |
| CHEMBL321198 | — | — | 1 | 7.92 |
| CHEMBL297962 | — | — | 1 | 7.85 |
| CHEMBL110637 | — | — | 1 | 7.77 |
| CHEMBL109362 | — | — | 1 | 7.50 |
| CHEMBL110578 | — | — | 1 | 7.40 |
| CHEMBL113620 | — | — | 1 | 7.16 |
| CHEMBL112899 | — | — | 1 | 7.05 |
| CHEMBL114393 | — | — | 1 | 6.92 |
| CHEMBL331141 | — | — | 1 | 6.55 |
| CHEMBL64360 | ENIPORIDE | 2.0 | 1 | 6.42 |
| CHEMBL114342 | — | — | 1 | 6.27 |
| CHEMBL112146 | — | — | 1 | 6.01 |
| CHEMBL110029 | — | — | 1 | 5.80 |
| CHEMBL113369 | — | — | 1 | 5.80 |
| CHEMBL113462 | — | — | 1 | 5.54 |
| CHEMBL436559 | CARIPORIDE | 2.0 | 1 | 5.47 |
| CHEMBL113201 | — | — | 1 | 5.46 |
| CHEMBL112867 | — | — | 1 | - |
| CHEMBL333603 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419578 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL112903 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL113443 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL51363 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL51879 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL321198 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL297962 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL110637 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL109362 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL110578 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL113620 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL112899 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL114393 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL331141 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL64360 | ENIPORIDE | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL114342 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL112146 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL110029 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL113369 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL113462 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL436559 | CARIPORIDE | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL113201 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL112867 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL333603 | — | IC50 | > | 30000.0 | nM | - |