Assay Detail
Functional
CHEMBL4707449
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Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 7.24 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4741857 | — | — | 1 | 8.09 |
| CHEMBL4753328 | — | — | 1 | 8.05 |
| CHEMBL4754941 | — | — | 1 | 8.04 |
| CHEMBL4753414 | — | — | 1 | 7.68 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 7.51 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 7.50 |
| CHEMBL4786537 | — | — | 1 | 7.33 |
| CHEMBL4742122 | — | — | 1 | 7.32 |
| CHEMBL4740097 | — | — | 1 | 7.26 |
| CHEMBL230963 | — | — | 1 | 7.22 |
| CHEMBL4759629 | — | — | 1 | 7.18 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.14 |
| CHEMBL4754363 | — | — | 1 | 7.10 |
| CHEMBL4789505 | — | — | 1 | 6.73 |
| CHEMBL4746734 | — | — | 1 | 6.03 |
| CHEMBL4793515 | — | — | 1 | 5.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4741857 | — | EC50 | = | 8.128 | nM | 8.09 |
| CHEMBL4753328 | — | EC50 | = | 8.913 | nM | 8.05 |
| CHEMBL4754941 | — | EC50 | = | 9.12 | nM | 8.04 |
| CHEMBL4753414 | — | EC50 | = | 20.89 | nM | 7.68 |
| CHEMBL39 | SEROTONIN | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL56 | 8-OH-DPAT | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4786537 | — | EC50 | = | 46.77 | nM | 7.33 |
| CHEMBL4742122 | — | EC50 | = | 47.86 | nM | 7.32 |
| CHEMBL4740097 | — | EC50 | = | 54.95 | nM | 7.26 |
| CHEMBL230963 | — | EC50 | = | 60.26 | nM | 7.22 |
| CHEMBL4759629 | — | EC50 | = | 66.07 | nM | 7.18 |
| CHEMBL49 | BUSPIRONE | EC50 | = | 72.44 | nM | 7.14 |
| CHEMBL4754363 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4789505 | — | EC50 | = | 186.21 | nM | 6.73 |
| CHEMBL4746734 | — | EC50 | = | 933.25 | nM | 6.03 |
| CHEMBL4793515 | — | EC50 | = | 2454.71 | nM | 5.61 |