Assay Detail
Binding
CHEMBL1067825
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Displacement of [125I]DOI from human recombinant 5HT2C receptor expressed in HEK293E cells
17
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293E |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.78 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL590580 | — | — | 1 | 8.54 |
| CHEMBL590531 | — | — | 2 | 8.19 |
| CHEMBL590483 | — | — | 1 | 8.05 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | 2.0 | 1 | 7.77 |
| CHEMBL590816 | — | — | 1 | 7.31 |
| CHEMBL590078 | — | — | 2 | 7.05 |
| CHEMBL590333 | — | — | 1 | 6.82 |
| CHEMBL605402 | — | — | 1 | 6.65 |
| CHEMBL590331 | — | — | 1 | 6.32 |
| CHEMBL590482 | — | — | 1 | 6.12 |
| CHEMBL590089 | — | — | 1 | 6.00 |
| CHEMBL590721 | — | — | 1 | 5.81 |
| CHEMBL590077 | — | — | 1 | 5.71 |
| CHEMBL590332 | — | — | 1 | 5.21 |
| CHEMBL603527 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL590580 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL590531 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL590483 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL590816 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL590531 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL590078 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL590333 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL605402 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL590331 | — | Ki | = | 479.0 | nM | 6.32 |
| CHEMBL590482 | — | Ki | = | 757.0 | nM | 6.12 |
| CHEMBL590089 | — | Ki | = | 998.0 | nM | 6.00 |
| CHEMBL590721 | — | Ki | = | 1547.0 | nM | 5.81 |
| CHEMBL590077 | — | Ki | = | 1936.0 | nM | 5.71 |
| CHEMBL590078 | — | Ki | = | 2076.0 | nM | 5.68 |
| CHEMBL590332 | — | Ki | = | 6145.0 | nM | 5.21 |
| CHEMBL603527 | — | Ki | > | 10000.0 | nM | - |