Assay Detail
Functional
CHEMBL2060288
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulation
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 8.64 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL538635 | — | — | 1 | 9.40 |
| CHEMBL2059588 | — | — | 1 | 9.40 |
| CHEMBL2059583 | — | — | 1 | 9.20 |
| CHEMBL2059587 | — | — | 1 | 9.10 |
| CHEMBL2059585 | — | — | 1 | 9.10 |
| CHEMBL2059582 | — | — | 1 | 9.10 |
| CHEMBL76370 | TEGASEROD | 4.0 | 1 | 9.00 |
| CHEMBL2059584 | — | — | 1 | 8.80 |
| CHEMBL2059577 | — | — | 1 | 8.70 |
| CHEMBL2059581 | — | — | 1 | 8.60 |
| CHEMBL2059590 | — | — | 1 | 8.60 |
| CHEMBL2059578 | — | — | 1 | 8.60 |
| CHEMBL2059589 | — | — | 1 | 8.40 |
| CHEMBL2059580 | — | — | 1 | 8.30 |
| CHEMBL2059579 | — | — | 1 | 8.30 |
| CHEMBL2059586 | — | — | 1 | 7.90 |
| CHEMBL74656 | REL-CISAPRIDE | — | 1 | 7.70 |
| CHEMBL550064 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL538635 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL2059588 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL2059583 | — | EC50 | = | 0.631 | nM | 9.20 |
| CHEMBL2059587 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL2059585 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL2059582 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL76370 | TEGASEROD | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2059584 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL2059577 | — | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL2059581 | — | EC50 | = | 2.512 | nM | 8.60 |
| CHEMBL2059590 | — | EC50 | = | 2.512 | nM | 8.60 |
| CHEMBL2059578 | — | EC50 | = | 2.512 | nM | 8.60 |
| CHEMBL2059589 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL2059580 | — | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL2059579 | — | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL2059586 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL74656 | REL-CISAPRIDE | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL550064 | — | EC50 | = | 39.81 | nM | 7.40 |