Assay Detail
Functional
CHEMBL857027
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Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Ketones related to the benzoate 5-HT4 receptor antagonist RS-23597 are high affinity partial agonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 7.41 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL83899 | — | — | 1 | 8.60 |
| CHEMBL85251 | — | — | 1 | 8.40 |
| CHEMBL84398 | — | — | 1 | 8.00 |
| CHEMBL79637 | — | — | 1 | 7.90 |
| CHEMBL82360 | — | — | 1 | 7.80 |
| CHEMBL34291 | — | — | 1 | 7.70 |
| CHEMBL286136 | — | — | 1 | 7.70 |
| CHEMBL80015 | — | — | 1 | 7.40 |
| CHEMBL83841 | — | — | 1 | 7.40 |
| CHEMBL314489 | — | — | 1 | 7.20 |
| CHEMBL310451 | — | — | 1 | 6.90 |
| CHEMBL82833 | — | — | 1 | 6.90 |
| CHEMBL420969 | — | — | 1 | 6.60 |
| CHEMBL309655 | — | — | 1 | 6.50 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL83899 | — | EC50 | = | 2.512 | nM | 8.60 |
| CHEMBL85251 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL84398 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL79637 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL82360 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL34291 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL286136 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL80015 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL83841 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL314489 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL310451 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL82833 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL420969 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL309655 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL86 | METOCLOPRAMIDE | EC50 | = | 794.33 | nM | 6.10 |