Assay Detail
Binding
CHEMBL645394
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Binding affinity towards alpha-1 adrenergic receptor in rat cortical membranes
30
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.29 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 7.75 |
| CHEMBL444590 | — | — | 1 | 7.26 |
| CHEMBL140406 | — | — | 1 | 7.22 |
| CHEMBL344432 | — | — | 1 | 7.08 |
| CHEMBL423181 | — | — | 1 | 6.93 |
| CHEMBL2112773 | — | — | 2 | 6.52 |
| CHEMBL138892 | — | — | 1 | 6.39 |
| CHEMBL344146 | — | — | 1 | 6.33 |
| CHEMBL2112776 | — | — | 2 | 6.33 |
| CHEMBL140287 | — | — | 1 | 6.29 |
| CHEMBL138900 | — | — | 1 | 6.23 |
| CHEMBL2112780 | — | — | 2 | 6.14 |
| CHEMBL2112779 | — | — | 2 | 6.14 |
| CHEMBL139146 | — | — | 1 | 6.13 |
| CHEMBL2112778 | — | — | 2 | 6.12 |
| CHEMBL2112771 | — | — | 2 | 6.11 |
| CHEMBL139505 | — | — | 1 | 6.08 |
| CHEMBL138289 | — | — | 1 | 6.01 |
| CHEMBL138109 | — | — | 1 | 5.89 |
| CHEMBL139848 | — | — | 1 | 5.29 |
| CHEMBL2112774 | — | — | 2 | - |
| CHEMBL138899 | — | — | 1 | - |
| CHEMBL136563 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL597 | PHENTOLAMINE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL444590 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL140406 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL344432 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL423181 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL2112773 | — | Ki | = | 303.0 | nM | 6.52 |
| CHEMBL138892 | — | Ki | = | 408.0 | nM | 6.39 |
| CHEMBL344146 | — | Ki | = | 467.0 | nM | 6.33 |
| CHEMBL2112776 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL140287 | — | Ki | = | 512.0 | nM | 6.29 |
| CHEMBL138900 | — | Ki | = | 585.0 | nM | 6.23 |
| CHEMBL2112773 | — | Ki | = | 712.0 | nM | 6.15 |
| CHEMBL2112780 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL2112779 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL139146 | — | Ki | = | 733.0 | nM | 6.13 |
| CHEMBL2112778 | — | Ki | = | 767.0 | nM | 6.12 |
| CHEMBL2112778 | — | Ki | = | 783.0 | nM | 6.11 |
| CHEMBL2112771 | — | Ki | = | 786.0 | nM | 6.11 |
| CHEMBL139505 | — | Ki | = | 833.0 | nM | 6.08 |
| CHEMBL2112771 | — | Ki | = | 847.0 | nM | 6.07 |
| CHEMBL138289 | — | Ki | = | 986.0 | nM | 6.01 |
| CHEMBL2112779 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL138109 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL2112780 | — | Ki | = | 2250.0 | nM | 5.65 |
| CHEMBL139848 | — | Ki | = | 5160.0 | nM | 5.29 |
| CHEMBL2112776 | — | Ki | = | 5540.0 | nM | 5.26 |
| CHEMBL138899 | — | Ki | > | 850.0 | nM | - |
| CHEMBL2112774 | — | Ki | > | 850.0 | nM | - |
| CHEMBL136563 | — | Ki | > | 850.0 | nM | - |
| CHEMBL2112774 | — | Ki | > | 850.0 | nM | - |