Assay Detail
Binding
CHEMBL4707447
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Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa 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 | 8.02 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4753328 | — | — | 1 | 9.37 |
| CHEMBL4741857 | — | — | 1 | 9.10 |
| CHEMBL4754941 | — | — | 1 | 9.06 |
| CHEMBL230963 | — | — | 1 | 8.33 |
| CHEMBL4753414 | — | — | 1 | 8.31 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.09 |
| CHEMBL4786537 | — | — | 1 | 7.90 |
| CHEMBL4759629 | — | — | 1 | 7.89 |
| CHEMBL4754363 | — | — | 1 | 7.88 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.82 |
| CHEMBL4740097 | — | — | 1 | 7.76 |
| CHEMBL4742122 | — | — | 1 | 7.62 |
| CHEMBL4789505 | — | — | 1 | 7.59 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 7.48 |
| CHEMBL4746734 | — | — | 1 | 7.28 |
| CHEMBL4793515 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4753328 | — | EC50 | = | 0.4266 | nM | 9.37 |
| CHEMBL4741857 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4754941 | — | EC50 | = | 0.871 | nM | 9.06 |
| CHEMBL230963 | — | EC50 | = | 4.677 | nM | 8.33 |
| CHEMBL4753414 | — | EC50 | = | 4.898 | nM | 8.31 |
| CHEMBL56 | 8-OH-DPAT | EC50 | = | 8.128 | nM | 8.09 |
| CHEMBL4786537 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4759629 | — | EC50 | = | 12.88 | nM | 7.89 |
| CHEMBL4754363 | — | EC50 | = | 13.18 | nM | 7.88 |
| CHEMBL49 | BUSPIRONE | EC50 | = | 15.14 | nM | 7.82 |
| CHEMBL4740097 | — | EC50 | = | 17.38 | nM | 7.76 |
| CHEMBL4742122 | — | EC50 | = | 23.99 | nM | 7.62 |
| CHEMBL4789505 | — | EC50 | = | 25.7 | nM | 7.59 |
| CHEMBL39 | SEROTONIN | EC50 | = | 33.11 | nM | 7.48 |
| CHEMBL4746734 | — | EC50 | = | 52.48 | nM | 7.28 |
| CHEMBL4793515 | — | EC50 | = | 169.82 | nM | 6.77 |