Assay Detail
Binding
CHEMBL856311
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NHE1 expressed in Ap1 cell line
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ap1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological activity of 5-aryl-4-(4-(5-methyl-1H-imidazol-4-yl)piperidin-1-yl)pyrimidine analogs as potent, highly selective, and orally bioavailable NHE-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.78 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384143 | — | — | 1 | 8.34 |
| CHEMBL211924 | — | — | 1 | 8.27 |
| CHEMBL217698 | — | — | 1 | 8.19 |
| CHEMBL213568 | — | — | 1 | 8.13 |
| CHEMBL385944 | — | — | 1 | 7.82 |
| CHEMBL376979 | — | — | 1 | 7.68 |
| CHEMBL212033 | — | — | 1 | 7.57 |
| CHEMBL380382 | — | — | 1 | 7.39 |
| CHEMBL384466 | — | — | 1 | 7.21 |
| CHEMBL215399 | — | — | 1 | 7.21 |
| CHEMBL214646 | — | — | 1 | 7.06 |
| CHEMBL215510 | — | — | 1 | 6.60 |
| CHEMBL425073 | — | — | 1 | 6.46 |
| CHEMBL450633 | — | — | 1 | 6.46 |
| CHEMBL64360 | ENIPORIDE | 2.0 | 1 | 6.40 |
| CHEMBL215509 | — | — | 1 | 6.28 |
| CHEMBL215928 | — | — | 1 | 6.24 |
| CHEMBL211922 | — | — | 1 | 6.09 |
| CHEMBL212856 | — | — | 1 | 6.03 |
| CHEMBL214922 | — | — | 1 | 6.00 |
| CHEMBL379871 | — | — | 1 | 5.72 |
| CHEMBL436559 | CARIPORIDE | 2.0 | 1 | 5.46 |
| CHEMBL384410 | — | — | 1 | 5.07 |
| CHEMBL378339 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384143 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL211924 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL217698 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL213568 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL385944 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL376979 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL212033 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL380382 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL384466 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL215399 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL214646 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL215510 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL425073 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL450633 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL64360 | ENIPORIDE | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL215509 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL215928 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL211922 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL212856 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL214922 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL379871 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL436559 | CARIPORIDE | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL384410 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL378339 | — | IC50 | = | 11000.0 | nM | 4.96 |