Assay Detail
Functional
CHEMBL2343530
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
40
Total Activities
20
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 | 40 | 7.02 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | 3.0 | 2 | 8.59 |
| CHEMBL301466 | — | — | 2 | 7.93 |
| CHEMBL6557 | PNU-22394 | — | 2 | 7.64 |
| CHEMBL2331803 | — | — | 2 | 7.57 |
| CHEMBL494947 | — | — | 2 | 7.12 |
| CHEMBL2331794 | — | — | 2 | 6.62 |
| CHEMBL269521 | MK-212 | — | 2 | 6.38 |
| CHEMBL2331807 | — | — | 2 | 6.26 |
| CHEMBL2331793 | — | — | 2 | 5.10 |
| CHEMBL2331802 | — | — | 2 | - |
| CHEMBL2331801 | — | — | 2 | - |
| CHEMBL2331799 | — | — | 2 | - |
| CHEMBL2331798 | — | — | 2 | - |
| CHEMBL2331797 | — | — | 2 | - |
| CHEMBL2331796 | — | — | 2 | - |
| CHEMBL2331791 | — | — | 2 | - |
| CHEMBL2331808 | — | — | 2 | - |
| CHEMBL309689 | — | — | 2 | - |
| CHEMBL2331800 | — | — | 2 | - |
| CHEMBL2331795 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | EC50 | = | 2.57 | nM | 8.59 |
| CHEMBL39 | SEROTONIN | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL301466 | — | EC50 | = | 11.75 | nM | 7.93 |
| CHEMBL301466 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6557 | PNU-22394 | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL6557 | PNU-22394 | EC50 | = | 23.44 | nM | 7.63 |
| CHEMBL2331803 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2331803 | — | EC50 | = | 26.92 | nM | 7.57 |
| CHEMBL494947 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL494947 | — | EC50 | = | 75.86 | nM | 7.12 |
| CHEMBL2331794 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2331794 | — | EC50 | = | 245.47 | nM | 6.61 |
| CHEMBL269521 | MK-212 | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL269521 | MK-212 | EC50 | = | 426.58 | nM | 6.37 |
| CHEMBL2331807 | — | EC50 | = | 549.54 | nM | 6.26 |
| CHEMBL2331807 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2331793 | — | EC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL2331793 | — | EC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL2331800 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331797 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331798 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331799 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331800 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331801 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331802 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331795 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331795 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331808 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331791 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331796 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331797 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331798 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331799 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331801 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331802 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL309689 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331796 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331791 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2331808 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL309689 | — | EC50 | > | 1000000.0 | nM | - |