Assay Detail
Functional
CHEMBL5547428
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Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as IP2 production measured after 30 mins incubation by HTRF assay
22
Total Activities
15
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
Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT<sub>2</sub> Receptor Agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 7.88 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5592769 | — | — | 2 | 9.18 |
| CHEMBL5591197 | — | — | 2 | 8.74 |
| CHEMBL5566821 | — | — | 2 | 8.45 |
| CHEMBL5575032 | — | — | 1 | 8.38 |
| CHEMBL5566894 | — | — | 2 | 8.27 |
| CHEMBL5566866 | — | — | 2 | 8.21 |
| CHEMBL5563475 | — | — | 2 | 7.39 |
| CHEMBL5571221 | — | — | 2 | 7.32 |
| CHEMBL5569144 | — | — | 1 | 7.05 |
| CHEMBL127285 | — | — | 1 | 6.82 |
| CHEMBL5592265 | — | — | 1 | 6.28 |
| CHEMBL5565571 | — | — | 1 | 6.07 |
| CHEMBL5592656 | — | — | 1 | - |
| CHEMBL5590167 | — | — | 1 | - |
| CHEMBL5566311 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5592769 | — | EC50 | = | 0.6607 | nM | 9.18 |
| CHEMBL5592769 | — | EC50 | = | 0.67 | nM | 9.17 |
| CHEMBL5591197 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5591197 | — | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL5566821 | — | EC50 | = | 3.548 | nM | 8.45 |
| CHEMBL5566821 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5575032 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5566894 | — | EC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5566894 | — | EC50 | = | 5.495 | nM | 8.26 |
| CHEMBL5566866 | — | EC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5566866 | — | EC50 | = | 6.166 | nM | 8.21 |
| CHEMBL5563475 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5563475 | — | EC50 | = | 41.69 | nM | 7.38 |
| CHEMBL5571221 | — | EC50 | = | 47.86 | nM | 7.32 |
| CHEMBL5571221 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5569144 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL127285 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5592265 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL5565571 | — | EC50 | = | 850.0 | nM | 6.07 |
| CHEMBL5566311 | — | EC50 | - | — | - | |
| CHEMBL5590167 | — | EC50 | - | — | - | |
| CHEMBL5592656 | — | EC50 | - | — | - |