Assay Detail
Functional
CHEMBL2343045
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 6.93 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL494947 | — | — | 2 | 8.09 |
| CHEMBL39 | SEROTONIN | 3.0 | 2 | 7.36 |
| CHEMBL6557 | PNU-22394 | — | 2 | 6.92 |
| CHEMBL269521 | MK-212 | — | 2 | 6.80 |
| CHEMBL2331794 | — | — | 2 | 6.64 |
| CHEMBL2331807 | — | — | 2 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL494947 | — | EC50 | = | 8.128 | nM | 8.09 |
| CHEMBL494947 | — | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL39 | SEROTONIN | EC50 | = | 43.65 | nM | 7.36 |
| CHEMBL39 | SEROTONIN | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL6557 | PNU-22394 | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL6557 | PNU-22394 | EC50 | = | 123.03 | nM | 6.91 |
| CHEMBL269521 | MK-212 | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL269521 | MK-212 | EC50 | = | 162.18 | nM | 6.79 |
| CHEMBL2331794 | — | EC50 | = | 229.09 | nM | 6.64 |
| CHEMBL2331794 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2331807 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2331807 | — | EC50 | = | 1737.8 | nM | 5.76 |