Assay Detail
Binding
CHEMBL4707451
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Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Aryloxyethyl Derivatives of 1-(1-Benzoylpiperidin-4-yl)methanamine as the Extracellular Regulated Kinases 1/2 (ERK1/2) Phosphorylation-Preferring Serotonin 5-HT Receptor-Biased Agonists with Robust Antidepressant-like Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 6.76 | 7.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4741857 | — | — | 1 | 7.98 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 7.84 |
| CHEMBL4753328 | — | — | 1 | 7.68 |
| CHEMBL4753414 | — | — | 1 | 7.60 |
| CHEMBL4786537 | — | — | 1 | 6.94 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 6.89 |
| CHEMBL4742122 | — | — | 1 | 6.87 |
| CHEMBL4754941 | — | — | 1 | 6.76 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 6.73 |
| CHEMBL230963 | — | — | 1 | 6.71 |
| CHEMBL4740097 | — | — | 1 | 6.58 |
| CHEMBL4759629 | — | — | 1 | 6.54 |
| CHEMBL4754363 | — | — | 1 | 6.35 |
| CHEMBL4789505 | — | — | 1 | 5.70 |
| CHEMBL4746734 | — | — | 1 | 5.56 |
| CHEMBL4793515 | — | — | 1 | 5.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4741857 | — | EC50 | = | 10.47 | nM | 7.98 |
| CHEMBL56 | 8-OH-DPAT | EC50 | = | 14.45 | nM | 7.84 |
| CHEMBL4753328 | — | EC50 | = | 20.89 | nM | 7.68 |
| CHEMBL4753414 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4786537 | — | EC50 | = | 114.82 | nM | 6.94 |
| CHEMBL39 | SEROTONIN | EC50 | = | 128.82 | nM | 6.89 |
| CHEMBL4742122 | — | EC50 | = | 134.9 | nM | 6.87 |
| CHEMBL4754941 | — | EC50 | = | 173.78 | nM | 6.76 |
| CHEMBL49 | BUSPIRONE | EC50 | = | 186.21 | nM | 6.73 |
| CHEMBL230963 | — | EC50 | = | 194.98 | nM | 6.71 |
| CHEMBL4740097 | — | EC50 | = | 263.03 | nM | 6.58 |
| CHEMBL4759629 | — | EC50 | = | 288.4 | nM | 6.54 |
| CHEMBL4754363 | — | EC50 | = | 446.68 | nM | 6.35 |
| CHEMBL4789505 | — | EC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4746734 | — | EC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL4793515 | — | EC50 | = | 3630.78 | nM | 5.44 |