Assay Detail
Functional
CHEMBL5039772
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Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
36
Total Activities
18
Compounds Tested
2
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 of G Protein-Biased Ligands against 5-HT<sub>7</sub>R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 6.94 | 7.68 |
| pEC50 | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4205349 | — | — | 2 | 7.68 |
| CHEMBL5074190 | — | — | 2 | 7.25 |
| CHEMBL5091373 | — | — | 2 | 7.15 |
| CHEMBL5077293 | — | — | 2 | 7.12 |
| CHEMBL39 | SEROTONIN | 3.0 | 2 | 6.96 |
| CHEMBL3961059 | — | — | 2 | 6.83 |
| CHEMBL3931889 | — | — | 2 | 6.32 |
| CHEMBL5083607 | — | — | 2 | 6.19 |
| CHEMBL5074880 | — | — | 2 | - |
| CHEMBL5081379 | — | — | 2 | - |
| CHEMBL5094680 | — | — | 2 | - |
| CHEMBL5071978 | — | — | 2 | - |
| CHEMBL5082177 | — | — | 2 | - |
| CHEMBL5094234 | — | — | 2 | - |
| CHEMBL5090884 | — | — | 2 | - |
| CHEMBL5084249 | — | — | 2 | - |
| CHEMBL5094493 | — | — | 2 | - |
| CHEMBL5093342 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4205349 | — | EC50 | = | 20.89 | nM | 7.68 |
| CHEMBL4205349 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5074190 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5074190 | — | EC50 | = | 56.23 | nM | 7.25 |
| CHEMBL5091373 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5091373 | — | EC50 | = | 70.79 | nM | 7.15 |
| CHEMBL5077293 | — | EC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5077293 | — | EC50 | = | 75.86 | nM | 7.12 |
| CHEMBL39 | SEROTONIN | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL39 | SEROTONIN | EC50 | = | 112.2 | nM | 6.95 |
| CHEMBL3961059 | — | EC50 | = | 147.91 | nM | 6.83 |
| CHEMBL3961059 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3931889 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3931889 | — | EC50 | = | 478.63 | nM | 6.32 |
| CHEMBL5083607 | — | EC50 | = | 645.65 | nM | 6.19 |
| CHEMBL5083607 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5094493 | — | pEC50 | - | — | - | |
| CHEMBL5090884 | — | pEC50 | - | — | - | |
| CHEMBL5093342 | — | pEC50 | - | — | - | |
| CHEMBL5094234 | — | pEC50 | - | — | - | |
| CHEMBL5082177 | — | pEC50 | - | — | - | |
| CHEMBL5074880 | — | EC50 | - | — | - | |
| CHEMBL5081379 | — | EC50 | - | — | - | |
| CHEMBL5094680 | — | EC50 | - | — | - | |
| CHEMBL5071978 | — | EC50 | - | — | - | |
| CHEMBL5084249 | — | pEC50 | - | — | - | |
| CHEMBL5071978 | — | pEC50 | - | — | - | |
| CHEMBL5094234 | — | EC50 | - | — | - | |
| CHEMBL5093342 | — | EC50 | - | — | - | |
| CHEMBL5090884 | — | EC50 | - | — | - | |
| CHEMBL5084249 | — | EC50 | - | — | - | |
| CHEMBL5094493 | — | EC50 | - | — | - | |
| CHEMBL5094680 | — | pEC50 | - | — | - | |
| CHEMBL5081379 | — | pEC50 | - | — | - | |
| CHEMBL5074880 | — | pEC50 | - | — | - | |
| CHEMBL5082177 | — | EC50 | - | — | - |