Assay Detail
Functional
CHEMBL2404386
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Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 8.54 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2402900 | — | — | 1 | 9.40 |
| CHEMBL2402904 | FELCISETRAG | 2.0 | 1 | 9.30 |
| CHEMBL2402891 | — | — | 1 | 9.20 |
| CHEMBL2402892 | — | — | 1 | 9.20 |
| CHEMBL2402894 | — | — | 1 | 9.10 |
| CHEMBL2402897 | — | — | 1 | 9.10 |
| CHEMBL2402903 | — | — | 1 | 9.00 |
| CHEMBL2402890 | — | — | 1 | 9.00 |
| CHEMBL2401750 | — | — | 1 | 8.80 |
| CHEMBL2402902 | — | — | 1 | 8.80 |
| CHEMBL2402895 | — | — | 1 | 8.80 |
| CHEMBL2402898 | — | — | 1 | 8.80 |
| CHEMBL2402901 | — | — | 1 | 8.70 |
| CHEMBL76370 | TEGASEROD | 4.0 | 1 | 8.60 |
| CHEMBL2402899 | — | — | 1 | 8.50 |
| CHEMBL2402893 | — | — | 1 | 8.50 |
| CHEMBL2402887 | — | — | 1 | 8.00 |
| CHEMBL1729 | CISAPRIDE | 4.0 | 1 | 7.10 |
| CHEMBL2402888 | — | — | 1 | 6.60 |
| CHEMBL2402889 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2402900 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL2402904 | FELCISETRAG | EC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL2402891 | — | EC50 | = | 0.631 | nM | 9.20 |
| CHEMBL2402892 | — | EC50 | = | 0.631 | nM | 9.20 |
| CHEMBL2402894 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL2402897 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL2402903 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2402890 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2401750 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL2402902 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL2402895 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL2402898 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL2402901 | — | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL76370 | TEGASEROD | EC50 | = | 2.512 | nM | 8.60 |
| CHEMBL2402899 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL2402893 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL2402887 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1729 | CISAPRIDE | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL2402888 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL2402889 | — | EC50 | = | 630.96 | nM | 6.20 |