Assay Detail
Binding
CHEMBL4189919
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
47
Total Activities
47
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 | Intermediate |
Publication
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT4 Receptor Partial Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 47 | 7.67 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4215329 | — | — | 1 | 10.00 |
| CHEMBL4217381 | — | — | 1 | 9.52 |
| CHEMBL4206847 | — | — | 1 | 9.52 |
| CHEMBL4211044 | — | — | 1 | 9.40 |
| CHEMBL4213334 | — | — | 1 | 9.22 |
| CHEMBL4208302 | — | — | 1 | 9.22 |
| CHEMBL4216003 | — | — | 1 | 9.15 |
| CHEMBL2152922 | PF-04995274 | 1.0 | 1 | 8.82 |
| CHEMBL4202791 | — | — | 1 | 8.82 |
| CHEMBL4203491 | — | — | 1 | 8.31 |
| CHEMBL117287 | PRUCALOPRIDE | 4.0 | 1 | 8.28 |
| CHEMBL4210176 | — | — | 1 | 8.14 |
| CHEMBL4205273 | — | — | 1 | 8.08 |
| CHEMBL4210063 | — | — | 1 | 8.08 |
| CHEMBL4212433 | — | — | 1 | 8.06 |
| CHEMBL4203734 | — | — | 1 | 8.06 |
| CHEMBL4218868 | — | — | 1 | 8.05 |
| CHEMBL4210983 | — | — | 1 | 7.98 |
| CHEMBL4215943 | — | — | 1 | 7.87 |
| CHEMBL4203277 | — | — | 1 | 7.86 |
| CHEMBL4213441 | — | — | 1 | 7.77 |
| CHEMBL4205936 | — | — | 1 | 7.68 |
| CHEMBL4203778 | — | — | 1 | 7.47 |
| CHEMBL4215651 | — | — | 1 | 7.44 |
| CHEMBL4210381 | — | — | 1 | 7.38 |
| CHEMBL4207586 | — | — | 1 | 7.32 |
| CHEMBL4203494 | — | — | 1 | 7.27 |
| CHEMBL3306918 | PRX-03140 | 2.0 | 1 | 7.24 |
| CHEMBL4215911 | — | — | 1 | 7.21 |
| CHEMBL4205387 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4215329 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4217381 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4206847 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4211044 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4213334 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4208302 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4216003 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2152922 | PF-04995274 | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4202791 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4203491 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL117287 | PRUCALOPRIDE | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4210176 | — | EC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4210063 | — | EC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4205273 | — | EC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4203734 | — | EC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4212433 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4218868 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4210983 | — | EC50 | = | 10.4 | nM | 7.98 |
| CHEMBL4215943 | — | EC50 | = | 13.6 | nM | 7.87 |
| CHEMBL4203277 | — | EC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4213441 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4205936 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4203778 | — | EC50 | = | 34.2 | nM | 7.47 |
| CHEMBL4215651 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4210381 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4207586 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4203494 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3306918 | PRX-03140 | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4215911 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4205387 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4210213 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4215511 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4208144 | — | EC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4217842 | — | EC50 | = | 291.0 | nM | 6.54 |
| CHEMBL4207136 | — | EC50 | = | 484.0 | nM | 6.32 |
| CHEMBL4212757 | — | EC50 | = | 598.0 | nM | 6.22 |
| CHEMBL4218152 | — | EC50 | = | 687.0 | nM | 6.16 |
| CHEMBL4207406 | — | EC50 | = | 758.0 | nM | 6.12 |
| CHEMBL4206608 | — | EC50 | = | 796.0 | nM | 6.10 |
| CHEMBL4208394 | — | EC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4202922 | — | EC50 | = | 1941.0 | nM | 5.71 |
| CHEMBL4206020 | — | EC50 | = | 1941.0 | nM | 5.71 |
| CHEMBL4212644 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4214953 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4209939 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4215820 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4209275 | — | EC50 | > | 10000.0 | nM | - |