Assay Detail
Binding
CHEMBL1066138
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Displacement of [125I]LSD from human recombinant 5HT2B 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 | 7.19 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL590078 | — | — | 2 | 8.07 |
| CHEMBL590580 | — | — | 1 | 8.00 |
| CHEMBL590333 | — | — | 1 | 7.89 |
| CHEMBL605402 | — | — | 1 | 7.75 |
| CHEMBL590483 | — | — | 1 | 7.64 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | 2.0 | 1 | 7.62 |
| CHEMBL590531 | — | — | 2 | 7.39 |
| CHEMBL590089 | — | — | 1 | 7.21 |
| CHEMBL590816 | — | — | 1 | 7.17 |
| CHEMBL590482 | — | — | 1 | 7.14 |
| CHEMBL590077 | — | — | 1 | 6.86 |
| CHEMBL590331 | — | — | 1 | 6.55 |
| CHEMBL590721 | — | — | 1 | 6.13 |
| CHEMBL590332 | — | — | 1 | 5.62 |
| CHEMBL603527 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL590078 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL590580 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL590333 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL605402 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL590483 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL590531 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL590531 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL590089 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL590816 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL590482 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL590077 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL590078 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL590331 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL590721 | — | Ki | = | 734.0 | nM | 6.13 |
| CHEMBL590332 | — | Ki | = | 2395.0 | nM | 5.62 |
| CHEMBL603527 | — | Ki | > | 10000.0 | nM | - |