Assay Detail
Functional
CHEMBL2188197
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Inverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activation
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 7.23 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181171 | — | — | 1 | 8.00 |
| CHEMBL2181189 | — | — | 1 | 7.20 |
| CHEMBL2181187 | — | — | 1 | 7.10 |
| CHEMBL2181188 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181171 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2181189 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL2181187 | — | EC50 | = | 79.4 | nM | 7.10 |
| CHEMBL2181188 | — | EC50 | = | 251.0 | nM | 6.60 |