Assay Detail
Binding
CHEMBL4625518
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human 5-HT2C expressed in human U2OS cells by pathhunter beta-arrestin assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of thioadatanserin and its dialkylated products as partial 5-HTR<sub>1A</sub> agonists and 5-HTR<sub>2A</sub> antagonists for potential use in depression and anxiety disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.09 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14563 | SB-242084 | — | 1 | 9.48 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 8.90 |
| CHEMBL2107510 | ADATANSERIN HYDROCHLORIDE | -1.0 | 1 | 5.90 |
| CHEMBL4637409 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14563 | SB-242084 | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL39 | SEROTONIN | IC50 | = | 1.25 | nM | 8.90 |
| CHEMBL2107510 | ADATANSERIN HYDROCHLORIDE | IC50 | = | 1261.0 | nM | 5.90 |
| CHEMBL4637409 | — | IC50 | > | 3333.0 | nM | - |