Assay Detail
Binding
CHEMBL615959
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of radioligand [3H]2-(di-N-propylamino)-8-hydroxytetralin from 5-hydroxytryptamine 1A receptor in rat frontal cortex homogenate
35
Total Activities
35
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
Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 7.94 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL28143 | — | — | 1 | 9.60 |
| CHEMBL27457 | — | — | 1 | 9.30 |
| CHEMBL27558 | — | — | 1 | 9.27 |
| CHEMBL285158 | — | — | 1 | 9.21 |
| CHEMBL26834 | — | — | 1 | 9.09 |
| CHEMBL94115 | — | — | 1 | 9.00 |
| CHEMBL26988 | — | — | 1 | 8.77 |
| CHEMBL26601 | — | — | 1 | 8.66 |
| CHEMBL279906 | — | — | 1 | 8.57 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.55 |
| CHEMBL8412 | IPSAPIRONE | 2.0 | 1 | 8.26 |
| CHEMBL280825 | — | — | 1 | 8.23 |
| CHEMBL27655 | — | — | 1 | 8.11 |
| CHEMBL26355 | — | — | 1 | 8.10 |
| CHEMBL286287 | — | — | 1 | 8.09 |
| CHEMBL282205 | — | — | 1 | 7.96 |
| CHEMBL80574 | — | — | 1 | 7.95 |
| CHEMBL28288 | — | — | 1 | 7.92 |
| CHEMBL61032 | — | — | 1 | 7.89 |
| CHEMBL26650 | — | — | 1 | 7.74 |
| CHEMBL416382 | — | — | 1 | 7.70 |
| CHEMBL329246 | — | — | 1 | 7.64 |
| CHEMBL27694 | — | — | 1 | 7.62 |
| CHEMBL26645 | — | — | 1 | 7.54 |
| CHEMBL282614 | ELTOPRAZINE | 2.0 | 1 | 7.40 |
| CHEMBL26819 | — | — | 1 | 7.25 |
| CHEMBL96658 | — | — | 1 | 7.19 |
| CHEMBL28110 | — | — | 1 | 7.19 |
| CHEMBL26905 | — | — | 1 | 7.18 |
| CHEMBL27590 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL28143 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL27457 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL27558 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL285158 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL26834 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL94115 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL26988 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL26601 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL279906 | — | Ki | = | 2.67 | nM | 8.57 |
| CHEMBL56 | 8-OH-DPAT | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL8412 | IPSAPIRONE | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL280825 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL27655 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL26355 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL286287 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL282205 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL80574 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL28288 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL61032 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL26650 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL416382 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL329246 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL27694 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL26645 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL282614 | ELTOPRAZINE | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL26819 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL96658 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL28110 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL26905 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL27590 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL27192 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL26737 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL307204 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL9666 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL413527 | — | Ki | = | 220.0 | nM | 6.66 |