Assay Detail
Binding
CHEMBL616694
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Binding affinity against 5-hydroxytryptamine 1A receptor in homogenated rat brain tissue, using by [3H]8-OH-DPAT as radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.59 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL28313 | — | — | 1 | 8.42 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.06 |
| CHEMBL28437 | — | — | 1 | 8.02 |
| CHEMBL324750 | — | — | 1 | 6.80 |
| CHEMBL114433 | — | — | 1 | 6.44 |
| CHEMBL11615 | — | — | 1 | 6.36 |
| CHEMBL273273 | 5-OH-DPAT | — | 1 | 5.98 |
| CHEMBL285755 | — | — | 1 | 5.55 |
| CHEMBL301559 | — | — | 1 | 5.49 |
| CHEMBL442203 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL28313 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL56 | 8-OH-DPAT | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL28437 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL324750 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL114433 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL11615 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL273273 | 5-OH-DPAT | Ki | = | 1040.0 | nM | 5.98 |
| CHEMBL285755 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL301559 | — | Ki | = | 3260.0 | nM | 5.49 |
| CHEMBL442203 | — | Ki | = | 16000.0 | nM | 4.80 |