Assay Detail
Binding
CHEMBL5584717
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Binding affinity to human 5-HT1A receptor extracted from HEK293 cell membrane assessed as inhibition of [3H]-OH-DPAT binding to 5-HT1A by measuring inhibition constant at 1 uM incubated for 1 hrs by microbeta2 reader
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and biological evaluation of aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT<sub>1A</sub>/5-HT<sub>7</sub>.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.85 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56 | 8-OH-DPAT | — | 1 | 9.80 |
| CHEMBL225284 | — | — | 1 | 9.66 |
| CHEMBL5598295 | — | — | 1 | 9.34 |
| CHEMBL5597217 | — | — | 1 | 9.17 |
| CHEMBL5598106 | — | — | 1 | 8.89 |
| CHEMBL3401493 | — | — | 1 | 8.52 |
| CHEMBL4434876 | — | — | 1 | 8.24 |
| CHEMBL224820 | — | — | 1 | 8.18 |
| CHEMBL5597415 | — | — | 1 | 7.85 |
| CHEMBL5597179 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56 | 8-OH-DPAT | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL225284 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL5598295 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL5597217 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL5598106 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3401493 | — | Ki | = | 2.99 | nM | 8.52 |
| CHEMBL4434876 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL224820 | — | Ki | = | 6.64 | nM | 8.18 |
| CHEMBL5597415 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5597179 | — | Ki | < | 0.04 | nM | - |