Assay Detail
Binding
CHEMBL616082
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Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Hippocampus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.60 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284716 | — | — | 1 | 9.52 |
| CHEMBL25554 | — | — | 1 | 8.57 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 8.37 |
| CHEMBL110239 | — | — | 1 | 8.29 |
| CHEMBL285755 | — | — | 1 | 7.14 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 6.95 |
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 6.22 |
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 5.74 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | - |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284716 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL25554 | — | Ki | = | 2.68 | nM | 8.57 |
| CHEMBL39 | SEROTONIN | Ki | = | 4.31 | nM | 8.37 |
| CHEMBL110239 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL285755 | — | Ki | = | 72.7 | nM | 7.14 |
| CHEMBL27 | PROPRANOLOL | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL267930 | SPIPERONE | Ki | = | 602.0 | nM | 6.22 |
| CHEMBL51 | KETANSERIN | Ki | = | 1817.0 | nM | 5.74 |
| CHEMBL59 | DOPAMINE | Ki | > | 10000.0 | nM | - |
| CHEMBL517712 | ATROPINE | Ki | > | 20000.0 | nM | - |