Assay Detail
Functional
CHEMBL2343053
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay
8
Total Activities
4
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 |
|---|---|---|---|
| Ki | 8 | 7.21 | 8.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3187365 | ASENAPINE | 4.0 | 2 | 8.61 |
| CHEMBL6437 | MIANSERIN | 4.0 | 2 | 8.10 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 7.14 |
| CHEMBL18972 | GLEMANSERIN | 2.0 | 2 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3187365 | ASENAPINE | Ki | = | 2.455 | nM | 8.61 |
| CHEMBL3187365 | ASENAPINE | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL6437 | MIANSERIN | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL6437 | MIANSERIN | Ki | = | 8.128 | nM | 8.09 |
| CHEMBL42 | CLOZAPINE | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL42 | CLOZAPINE | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL18972 | GLEMANSERIN | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL18972 | GLEMANSERIN | Ki | = | 10000.0 | nM | 5.00 |