Assay Detail
Binding
CHEMBL2343042
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis
40
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | tsA201 |
| 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 | 40 | 6.16 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | 4.0 | 2 | 8.77 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 8.03 |
| CHEMBL494947 | — | — | 2 | 8.03 |
| CHEMBL39 | SEROTONIN | 3.0 | 2 | 7.10 |
| CHEMBL2331788 | — | — | 2 | 6.51 |
| CHEMBL2331794 | — | — | 2 | 5.92 |
| CHEMBL2331807 | — | — | 2 | 5.64 |
| CHEMBL269521 | MK-212 | — | 2 | 5.47 |
| CHEMBL2331789 | — | — | 2 | 5.32 |
| CHEMBL2331790 | — | — | 2 | 5.14 |
| CHEMBL2331793 | — | — | 2 | 4.00 |
| CHEMBL2331806 | — | — | 2 | 4.00 |
| CHEMBL2331792 | — | — | 2 | - |
| CHEMBL2331791 | — | — | 2 | - |
| CHEMBL2331808 | — | — | 2 | - |
| CHEMBL2331805 | — | — | 2 | - |
| CHEMBL2331804 | — | — | 2 | - |
| CHEMBL309689 | — | — | 2 | - |
| CHEMBL2331795 | — | — | 2 | - |
| CHEMBL2331796 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL6437 | MIANSERIN | Ki | = | 1.738 | nM | 8.76 |
| CHEMBL494947 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL42 | CLOZAPINE | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL42 | CLOZAPINE | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL494947 | — | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL39 | SEROTONIN | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL39 | SEROTONIN | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL2331788 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL2331788 | — | Ki | = | 309.03 | nM | 6.51 |
| CHEMBL2331794 | — | Ki | = | 1202.26 | nM | 5.92 |
| CHEMBL2331794 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2331807 | — | Ki | = | 2290.87 | nM | 5.64 |
| CHEMBL2331807 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL269521 | MK-212 | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL269521 | MK-212 | Ki | = | 3388.44 | nM | 5.47 |
| CHEMBL2331789 | — | Ki | = | 4786.3 | nM | 5.32 |
| CHEMBL2331789 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL2331790 | — | Ki | = | 7244.36 | nM | 5.14 |
| CHEMBL2331790 | — | Ki | = | 7200.0 | nM | 5.14 |
| CHEMBL2331793 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2331793 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2331806 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2331806 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2331808 | — | Ki | > | 316227.77 | nM | - |
| CHEMBL2331805 | — | Ki | = | 316227.77 | nM | - |
| CHEMBL2331804 | — | Ki | > | 316227.77 | nM | - |
| CHEMBL309689 | — | Ki | > | 316227.77 | nM | - |
| CHEMBL2331792 | — | Ki | = | 316227.77 | nM | - |
| CHEMBL2331795 | — | Ki | > | 316227.77 | nM | - |
| CHEMBL2331796 | — | Ki | > | 316227.77 | nM | - |
| CHEMBL2331791 | — | Ki | > | 316227.77 | nM | - |
| CHEMBL2331795 | — | Ki | > | 300000.0 | nM | - |
| CHEMBL2331792 | — | Ki | = | 300000.0 | nM | - |
| CHEMBL2331791 | — | Ki | > | 300000.0 | nM | - |
| CHEMBL2331796 | — | Ki | > | 300000.0 | nM | - |
| CHEMBL2331808 | — | Ki | > | 300000.0 | nM | - |
| CHEMBL2331805 | — | Ki | = | 300000.0 | nM | - |
| CHEMBL309689 | — | Ki | > | 300000.0 | nM | - |
| CHEMBL2331804 | — | Ki | > | 300000.0 | nM | - |