Assay Detail
Binding
CHEMBL5223843
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay
73
Total Activities
73
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Preclinical Characterization of Usmarapride (SUVN-D4010): A Potent, Selective 5-HT<sub>4</sub> Receptor Partial Agonist for the Treatment of Cognitive Deficits Associated with Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 73 | 7.31 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2152922 | PF-04995274 | 1.0 | 1 | 8.89 |
| CHEMBL85251 | — | — | 1 | 8.70 |
| CHEMBL5274456 | — | — | 1 | 8.52 |
| CHEMBL5281474 | — | — | 1 | 8.43 |
| CHEMBL5276171 | — | — | 1 | 8.42 |
| CHEMBL5274204 | — | — | 1 | 8.38 |
| CHEMBL5289203 | — | — | 1 | 8.37 |
| CHEMBL5271080 | — | — | 1 | 8.30 |
| CHEMBL5274379 | — | — | 1 | 8.28 |
| CHEMBL5278851 | — | — | 1 | 8.24 |
| CHEMBL5281078 | — | — | 1 | 8.24 |
| CHEMBL5280851 | — | — | 1 | 8.19 |
| CHEMBL5287000 | — | — | 1 | 8.14 |
| CHEMBL5283820 | — | — | 1 | 8.07 |
| CHEMBL5283568 | — | — | 1 | 7.98 |
| CHEMBL5275962 | — | — | 1 | 7.98 |
| CHEMBL5289747 | — | — | 1 | 7.91 |
| CHEMBL5286277 | — | — | 1 | 7.85 |
| CHEMBL5267237 | — | — | 1 | 7.83 |
| CHEMBL5275060 | — | — | 1 | 7.82 |
| CHEMBL5283556 | — | — | 1 | 7.73 |
| CHEMBL5278277 | — | — | 1 | 7.70 |
| CHEMBL5286257 | — | — | 1 | 7.67 |
| CHEMBL5288438 | — | — | 1 | 7.66 |
| CHEMBL5275260 | — | — | 1 | 7.64 |
| CHEMBL5285364 | — | — | 1 | 7.64 |
| CHEMBL5290568 | — | — | 1 | 7.64 |
| CHEMBL5286642 | — | — | 1 | 7.62 |
| CHEMBL5290222 | — | — | 1 | 7.60 |
| CHEMBL5275895 | — | — | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2152922 | PF-04995274 | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL85251 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5274456 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5281474 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5276171 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5274204 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5289203 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5271080 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5274379 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5278851 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5281078 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5280851 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5287000 | — | EC50 | = | 7.3 | nM | 8.14 |
| CHEMBL5283820 | — | EC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5275962 | — | EC50 | = | 10.5 | nM | 7.98 |
| CHEMBL5283568 | — | EC50 | = | 10.4 | nM | 7.98 |
| CHEMBL5289747 | — | EC50 | = | 12.4 | nM | 7.91 |
| CHEMBL5286277 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5267237 | — | EC50 | = | 14.8 | nM | 7.83 |
| CHEMBL5275060 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5283556 | — | EC50 | = | 18.5 | nM | 7.73 |
| CHEMBL5278277 | — | EC50 | = | 19.9 | nM | 7.70 |
| CHEMBL5286257 | — | EC50 | = | 21.6 | nM | 7.67 |
| CHEMBL5288438 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5290568 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5285364 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5275260 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5286642 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5290222 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5275895 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5275886 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5270492 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5279298 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5281000 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5284140 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5273457 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5288891 | — | EC50 | = | 49.4 | nM | 7.31 |
| CHEMBL5268956 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3306918 | PRX-03140 | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5278176 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5286398 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5286814 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5277726 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5290981 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5287697 | — | EC50 | = | 106.7 | nM | 6.97 |
| CHEMBL5288809 | — | EC50 | = | 116.0 | nM | 6.94 |
| CHEMBL5270858 | — | EC50 | = | 127.0 | nM | 6.90 |
| CHEMBL5272596 | — | EC50 | = | 143.0 | nM | 6.84 |
| CHEMBL5277017 | — | EC50 | = | 151.0 | nM | 6.82 |
| CHEMBL5275605 | — | EC50 | = | 156.0 | nM | 6.81 |