Assay Detail
Binding
CHEMBL4707367
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]8-OH-DPAT from recombinant human 5HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by microbeta2 scintillation counting method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Subcellular | Cell membrane |
| 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 |
|---|---|---|---|
| Ki | 21 | 8.73 | 10.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4742112 | — | — | 1 | 10.83 |
| CHEMBL4754941 | — | — | 1 | 10.47 |
| CHEMBL4741857 | — | — | 1 | 10.21 |
| CHEMBL4753328 | — | — | 1 | 10.19 |
| CHEMBL4754363 | — | — | 1 | 9.32 |
| CHEMBL4753414 | — | — | 1 | 9.28 |
| CHEMBL4793515 | — | — | 1 | 9.25 |
| CHEMBL4759629 | — | — | 1 | 9.21 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 9.09 |
| CHEMBL4740097 | — | — | 1 | 8.90 |
| CHEMBL4742122 | — | — | 1 | 8.82 |
| CHEMBL4789505 | — | — | 1 | 8.73 |
| CHEMBL230963 | — | — | 1 | 8.66 |
| CHEMBL4786537 | — | — | 1 | 8.59 |
| CHEMBL4748858 | — | — | 1 | 8.42 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 8.30 |
| CHEMBL4746734 | — | — | 1 | 7.86 |
| CHEMBL4745099 | — | — | 1 | 7.45 |
| CHEMBL4753988 | — | — | 1 | 6.70 |
| CHEMBL4777084 | — | — | 1 | 6.68 |
| CHEMBL4761382 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4742112 | — | Ki | = | 0.01479 | nM | 10.83 |
| CHEMBL4754941 | — | Ki | = | 0.03388 | nM | 10.47 |
| CHEMBL4741857 | — | Ki | = | 0.06166 | nM | 10.21 |
| CHEMBL4753328 | — | Ki | = | 0.06457 | nM | 10.19 |
| CHEMBL4754363 | — | Ki | = | 0.4786 | nM | 9.32 |
| CHEMBL4753414 | — | Ki | = | 0.5248 | nM | 9.28 |
| CHEMBL4793515 | — | Ki | = | 0.5623 | nM | 9.25 |
| CHEMBL4759629 | — | Ki | = | 0.6166 | nM | 9.21 |
| CHEMBL56 | 8-OH-DPAT | Ki | = | 0.8128 | nM | 9.09 |
| CHEMBL4740097 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL4742122 | — | Ki | = | 1.514 | nM | 8.82 |
| CHEMBL4789505 | — | Ki | = | 1.862 | nM | 8.73 |
| CHEMBL230963 | — | Ki | = | 2.188 | nM | 8.66 |
| CHEMBL4786537 | — | Ki | = | 2.57 | nM | 8.59 |
| CHEMBL4748858 | — | Ki | = | 3.802 | nM | 8.42 |
| CHEMBL49 | BUSPIRONE | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL4746734 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL4745099 | — | Ki | = | 35.48 | nM | 7.45 |
| CHEMBL4753988 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL4777084 | — | Ki | = | 208.93 | nM | 6.68 |
| CHEMBL4761382 | — | Ki | = | 389.05 | nM | 6.41 |