Assay Detail
Functional
CHEMBL3744958
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and SAR of Imidazo[1,5-a]pyridine derivatives as 5-HT4 receptor partial agonists for the treatment of cognitive disorders associated with Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 55 | 7.41 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3741376 | — | — | 1 | 9.30 |
| CHEMBL2152922 | PF-04995274 | 1.0 | 1 | 8.89 |
| CHEMBL2402904 | FELCISETRAG | 2.0 | 1 | 8.82 |
| CHEMBL85251 | — | — | 1 | 8.70 |
| CHEMBL286136 | — | — | 1 | 8.60 |
| CHEMBL3739521 | — | — | 1 | 8.47 |
| CHEMBL3740908 | — | — | 1 | 8.41 |
| CHEMBL3741821 | — | — | 1 | 8.32 |
| CHEMBL117287 | PRUCALOPRIDE | 4.0 | 1 | 8.28 |
| CHEMBL3741548 | — | — | 1 | 8.24 |
| CHEMBL3740669 | — | — | 1 | 8.06 |
| CHEMBL3741733 | — | — | 1 | 8.01 |
| CHEMBL3741787 | — | — | 1 | 8.01 |
| CHEMBL3741608 | — | — | 1 | 8.00 |
| CHEMBL3739862 | — | — | 1 | 7.96 |
| CHEMBL3741224 | — | — | 1 | 7.88 |
| CHEMBL3741826 | — | — | 1 | 7.81 |
| CHEMBL3739931 | — | — | 1 | 7.75 |
| CHEMBL3741595 | — | — | 1 | 7.75 |
| CHEMBL3740844 | — | — | 1 | 7.74 |
| CHEMBL3741918 | — | — | 1 | 7.70 |
| CHEMBL3740612 | — | — | 1 | 7.68 |
| CHEMBL3740472 | — | — | 1 | 7.66 |
| CHEMBL3740732 | — | — | 1 | 7.60 |
| CHEMBL3739647 | — | — | 1 | 7.51 |
| CHEMBL3741377 | — | — | 1 | 7.47 |
| CHEMBL3739826 | — | — | 1 | 7.41 |
| CHEMBL3739611 | — | — | 1 | 7.40 |
| CHEMBL3741776 | — | — | 1 | 7.40 |
| CHEMBL3739933 | — | — | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3741376 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2152922 | PF-04995274 | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2402904 | FELCISETRAG | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL85251 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL286136 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3739521 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3740908 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3741821 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL117287 | PRUCALOPRIDE | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3741548 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3740669 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL3741733 | — | EC50 | = | 9.8 | nM | 8.01 |
| CHEMBL3741787 | — | EC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3741608 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3739862 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3741224 | — | EC50 | = | 13.2 | nM | 7.88 |
| CHEMBL3741826 | — | EC50 | = | 15.5 | nM | 7.81 |
| CHEMBL3739931 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3741595 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3740844 | — | EC50 | = | 18.3 | nM | 7.74 |
| CHEMBL3741918 | — | EC50 | = | 19.8 | nM | 7.70 |
| CHEMBL3740612 | — | EC50 | = | 20.7 | nM | 7.68 |
| CHEMBL3740472 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3740732 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3739647 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3741377 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3739826 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3739611 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3741776 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3739933 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3741322 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3739470 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3740400 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3741062 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3739459 | — | EC50 | = | 56.7 | nM | 7.25 |
| CHEMBL3306918 | PRX-03140 | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3742145 | — | EC50 | = | 72.3 | nM | 7.14 |
| CHEMBL3742080 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3742086 | — | EC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3740708 | — | EC50 | = | 144.0 | nM | 6.84 |
| CHEMBL3742190 | — | EC50 | = | 144.0 | nM | 6.84 |
| CHEMBL3741703 | — | EC50 | = | 196.0 | nM | 6.71 |
| CHEMBL3740030 | — | EC50 | = | 315.7 | nM | 6.50 |
| CHEMBL3741508 | — | EC50 | = | 467.0 | nM | 6.33 |
| CHEMBL3740313 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3739455 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3740864 | — | EC50 | = | 633.0 | nM | 6.20 |
| CHEMBL3739467 | — | EC50 | = | 736.0 | nM | 6.13 |
| CHEMBL3741199 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL3740000 | — | EC50 | = | 857.0 | nM | 6.07 |