Assay Detail
Binding
CHEMBL616065
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat cortex membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.80 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL118704 | — | — | 1 | 9.46 |
| CHEMBL119680 | — | — | 1 | 9.40 |
| CHEMBL118661 | — | — | 1 | 9.38 |
| CHEMBL48163 | — | — | 1 | 9.09 |
| CHEMBL47792 | — | — | 1 | 9.05 |
| CHEMBL264731 | — | — | 1 | 8.99 |
| CHEMBL118770 | — | — | 1 | 8.94 |
| CHEMBL300094 | — | — | 1 | 8.88 |
| CHEMBL118910 | — | — | 1 | 8.82 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.70 |
| CHEMBL117996 | — | — | 1 | 8.61 |
| CHEMBL300093 | — | — | 1 | 8.60 |
| CHEMBL116323 | — | — | 1 | 7.96 |
| CHEMBL331049 | — | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL118704 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL119680 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL118661 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL48163 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL47792 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL264731 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL118770 | — | Ki | = | 1.16 | nM | 8.94 |
| CHEMBL300094 | — | Ki | = | 1.32 | nM | 8.88 |
| CHEMBL118910 | — | Ki | = | 1.52 | nM | 8.82 |
| CHEMBL56 | 8-OH-DPAT | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL117996 | — | Ki | = | 2.47 | nM | 8.61 |
| CHEMBL300093 | — | Ki | = | 2.54 | nM | 8.60 |
| CHEMBL116323 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL331049 | — | Ki | = | 49.8 | nM | 7.30 |