Assay Detail
Binding
CHEMBL1261465
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Displacement of [3H]Prazosin from adrenergic alpha1 receptor in pig cerebral cortex homogenates
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Tissue | Cerebral cortex |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.44 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1257689 | — | — | 1 | 8.89 |
| CHEMBL1257688 | — | — | 1 | 8.54 |
| CHEMBL1258037 | — | — | 1 | 8.49 |
| CHEMBL210567 | — | — | 1 | 8.38 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.17 |
| CHEMBL1257927 | — | — | 1 | 7.96 |
| CHEMBL476935 | — | — | 1 | 7.89 |
| CHEMBL1258494 | — | — | 1 | 7.85 |
| CHEMBL424294 | — | — | 1 | 7.85 |
| CHEMBL1258383 | — | — | 1 | 7.70 |
| CHEMBL1258155 | — | — | 1 | 7.58 |
| CHEMBL1258495 | — | — | 1 | 7.54 |
| CHEMBL1257811 | — | — | 1 | 7.46 |
| CHEMBL1258270 | — | — | 1 | 7.22 |
| CHEMBL1258036 | — | — | 1 | 7.15 |
| CHEMBL1257810 | — | — | 1 | 6.80 |
| CHEMBL1258154 | — | — | 1 | 6.75 |
| CHEMBL1258382 | — | — | 1 | 6.31 |
| CHEMBL1256171 | — | — | 1 | 6.08 |
| CHEMBL1256170 | — | — | 1 | 6.00 |
| CHEMBL1256169 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1257689 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1257688 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL1258037 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL210567 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL1257927 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL476935 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1258494 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL424294 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1258383 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1258155 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL1258495 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL1257811 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL1258270 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL1258036 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL1257810 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL1258154 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL1258382 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL1256171 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL1256170 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1256169 | — | Ki | = | 2800.0 | nM | 5.55 |