Assay Detail
ADMET
CHEMBL3871854
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Displacement of [125I]DOI from recombinant human 5-HT2B receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT2C receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.60 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3895972 | — | — | 1 | 8.20 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | 2.0 | 1 | 8.00 |
| CHEMBL3956394 | — | — | 1 | 7.90 |
| CHEMBL3947276 | — | — | 1 | 7.60 |
| CHEMBL3959570 | — | — | 1 | 7.60 |
| CHEMBL3919795 | — | — | 1 | 7.40 |
| CHEMBL3912721 | — | — | 1 | 7.20 |
| CHEMBL3935339 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3895972 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3956394 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL3947276 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL3959570 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL3919795 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL3912721 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL3935339 | — | Ki | = | 125.89 | nM | 6.90 |