Assay Detail
Binding
CHEMBL647616
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Binding affinity to alpha-1 adrenergic receptor from rat brain homogenate, using [3H]- prazosin as the competitive ligand
34
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.17 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.40 |
| CHEMBL1202216 | — | — | 1 | 8.30 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.15 |
| CHEMBL1202205 | — | — | 1 | 8.10 |
| CHEMBL1202219 | — | — | 1 | 8.05 |
| CHEMBL1202215 | — | — | 1 | 8.00 |
| CHEMBL1202214 | — | — | 1 | 7.85 |
| CHEMBL341497 | — | — | 1 | 7.66 |
| CHEMBL1202211 | — | — | 1 | 7.54 |
| CHEMBL1202209 | — | — | 1 | 7.51 |
| CHEMBL1202212 | — | — | 1 | 7.35 |
| CHEMBL1203260 | — | — | 1 | 7.26 |
| CHEMBL1202223 | — | — | 1 | 7.25 |
| CHEMBL1202222 | — | — | 1 | 7.21 |
| CHEMBL1202206 | — | — | 1 | 7.21 |
| CHEMBL1202221 | — | — | 1 | 7.16 |
| CHEMBL1202202 | — | — | 1 | 7.13 |
| CHEMBL1202220 | — | — | 1 | 7.09 |
| CHEMBL1202208 | — | — | 1 | 6.88 |
| CHEMBL1204119 | — | — | 1 | 6.86 |
| CHEMBL2092961 | — | — | 1 | 6.84 |
| CHEMBL1203257 | — | — | 1 | 6.78 |
| CHEMBL1202204 | — | — | 1 | 6.71 |
| CHEMBL1202210 | — | — | 1 | 6.51 |
| CHEMBL1204116 | — | — | 2 | 6.51 |
| CHEMBL1202217 | — | — | 1 | 6.49 |
| CHEMBL1202213 | — | — | 1 | 6.48 |
| CHEMBL125455 | — | — | 1 | 6.46 |
| CHEMBL1202224 | — | — | 1 | 6.20 |
| CHEMBL1202225 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1202216 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1202205 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1202219 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1202215 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1202214 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL341497 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1202211 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1202209 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1202212 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1203260 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1202223 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1202222 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1202206 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1202221 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1202202 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1202220 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL1202208 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL1204119 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL2092961 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL1203257 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL1202204 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL1202210 | — | IC50 | = | 307.0 | nM | 6.51 |
| CHEMBL1204116 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL1204116 | — | IC50 | = | 322.0 | nM | 6.49 |
| CHEMBL1202217 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL1202213 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL125455 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL1202224 | — | IC50 | = | 633.0 | nM | 6.20 |
| CHEMBL1202225 | — | IC50 | = | 1341.0 | nM | 5.87 |
| CHEMBL1202207 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1202203 | — | IC50 | > | 1246.0 | nM | - |
| CHEMBL22242 | REMOXIPRIDE | IC50 | > | 4000.0 | nM | - |