Assay Detail
Binding
CHEMBL616075
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Binding affinity was evaluated by determining in vitro displacement of [3H]8-OH-DPAT from the central 5-hydroxytryptamine 1A receptor recognition site in rat frontal cortex homogenate.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 8.22 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL294633 | — | — | 1 | 9.82 |
| CHEMBL81728 | — | — | 1 | 9.52 |
| CHEMBL107141 | — | — | 1 | 9.49 |
| CHEMBL108229 | — | — | 1 | 9.10 |
| CHEMBL316960 | — | — | 1 | 9.00 |
| CHEMBL58792 | FLUANISONE | 2.0 | 1 | 9.00 |
| CHEMBL58377 | — | — | 1 | 9.00 |
| CHEMBL105345 | — | — | 1 | 8.96 |
| CHEMBL106854 | — | — | 1 | 8.89 |
| CHEMBL419910 | — | — | 1 | 8.80 |
| CHEMBL1742477 | FLESINOXAN | 2.0 | 1 | 8.77 |
| CHEMBL104805 | — | — | 1 | 8.74 |
| CHEMBL104515 | ANISOPIROL | 2.0 | 1 | 8.60 |
| CHEMBL105747 | — | — | 1 | 8.47 |
| CHEMBL107903 | — | — | 1 | 8.35 |
| CHEMBL104578 | — | — | 1 | 8.31 |
| CHEMBL61032 | — | — | 1 | 7.89 |
| CHEMBL107336 | — | — | 1 | 7.82 |
| CHEMBL278799 | — | — | 1 | 7.80 |
| CHEMBL104204 | — | — | 1 | 7.75 |
| CHEMBL104593 | — | — | 1 | 7.75 |
| CHEMBL323982 | — | — | 1 | 7.66 |
| CHEMBL282614 | ELTOPRAZINE | 2.0 | 1 | 7.40 |
| CHEMBL106413 | — | — | 1 | 7.23 |
| CHEMBL26447 | — | — | 1 | 6.85 |
| CHEMBL9666 | — | — | 1 | 6.77 |
| CHEMBL9434 | PHENYLPIPERAZINE | — | 1 | 6.30 |
| CHEMBL104591 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL294633 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL81728 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL107141 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL108229 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL316960 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL58792 | FLUANISONE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL58377 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL105345 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL106854 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL419910 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1742477 | FLESINOXAN | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL104805 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL104515 | ANISOPIROL | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL105747 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL107903 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL104578 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL61032 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL107336 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL278799 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL104204 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL104593 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL323982 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL282614 | ELTOPRAZINE | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL106413 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL26447 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL9666 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL9434 | PHENYLPIPERAZINE | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL104591 | — | Ki | = | 800.0 | nM | 6.10 |