Assay Detail
Functional
CHEMBL873248
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of sodium dependent recovery of pH following imposed acidosis in AP1 cell line expressing the human NHE-1 isoform.
21
Total Activities
21
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
Aminoimidazoles as bioisosteres of acylguanidines: novel, potent, selective and orally bioavailable inhibitors of the sodium hydrogen exchanger isoform-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.18 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51363 | — | — | 1 | 8.22 |
| CHEMBL51950 | — | — | 1 | 8.10 |
| CHEMBL51879 | — | — | 1 | 8.05 |
| CHEMBL297962 | — | — | 1 | 7.68 |
| CHEMBL52381 | — | — | 1 | 7.41 |
| CHEMBL49235 | — | — | 1 | 6.75 |
| CHEMBL51727 | — | — | 1 | 6.12 |
| CHEMBL301286 | — | — | 1 | 6.02 |
| CHEMBL299011 | — | — | 1 | 5.58 |
| CHEMBL50529 | — | — | 1 | 5.44 |
| CHEMBL301068 | — | — | 1 | 5.42 |
| CHEMBL52345 | — | — | 1 | 5.40 |
| CHEMBL299962 | — | — | 1 | 5.31 |
| CHEMBL50671 | — | — | 1 | 5.10 |
| CHEMBL51010 | — | — | 1 | 5.00 |
| CHEMBL50955 | — | — | 1 | 4.96 |
| CHEMBL50670 | — | — | 1 | 4.52 |
| CHEMBL299442 | — | — | 1 | - |
| CHEMBL301321 | — | — | 1 | - |
| CHEMBL299212 | — | — | 1 | - |
| CHEMBL298358 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51363 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL51950 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL51879 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL297962 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL52381 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL49235 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL51727 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL301286 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL299011 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL50529 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL301068 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL52345 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL299962 | — | IC50 | = | 4850.0 | nM | 5.31 |
| CHEMBL50671 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL51010 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL50955 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL50670 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL299442 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL301321 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL299212 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL298358 | — | IC50 | > | 30000.0 | nM | - |