Assay Detail
Binding
CHEMBL5058461
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Modulation of human 5HT2C expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Improved 5-HT2 Selective Receptor Modulators for the Treatment of Psychological Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.41 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5078731 | — | — | 1 | 9.92 |
| CHEMBL5077004 | — | — | 1 | 9.05 |
| CHEMBL5071818 | — | — | 1 | 8.57 |
| CHEMBL5085055 | — | — | 1 | 8.55 |
| CHEMBL65547 | PSILOCIN | 2.0 | 1 | 8.11 |
| CHEMBL197664 | — | — | 1 | 8.02 |
| CHEMBL5081637 | — | — | 1 | 7.83 |
| CHEMBL5079070 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5078731 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5077004 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5071818 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5085055 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL65547 | PSILOCIN | IC50 | = | 7.79 | nM | 8.11 |
| CHEMBL197664 | — | IC50 | = | 9.51 | nM | 8.02 |
| CHEMBL5081637 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL5079070 | — | IC50 | = | 63.5 | nM | 7.20 |