Assay Detail
Binding
CHEMBL829674
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Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.89 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 9.38 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.57 |
| CHEMBL1255588 | — | — | 1 | 8.44 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 8.18 |
| CHEMBL178700 | — | — | 1 | 6.35 |
| CHEMBL179145 | — | — | 1 | 6.24 |
| CHEMBL179371 | — | — | 1 | 6.06 |
| CHEMBL178650 | — | — | 1 | 6.03 |
| CHEMBL178519 | — | — | 1 | 5.96 |
| CHEMBL434905 | — | — | 1 | 5.96 |
| CHEMBL180327 | — | — | 1 | 5.94 |
| CHEMBL179373 | — | — | 1 | 5.60 |
| CHEMBL369133 | — | — | 1 | - |
| CHEMBL179697 | — | — | 1 | - |
| CHEMBL179808 | — | — | 1 | - |
| CHEMBL276784 | — | — | 1 | - |
| CHEMBL425867 | — | — | 1 | - |
| CHEMBL360351 | — | — | 1 | - |
| CHEMBL178924 | — | — | 1 | - |
| CHEMBL178680 | — | — | 1 | - |
| CHEMBL179530 | — | — | 1 | - |
| CHEMBL180119 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.69 | nM | 8.57 |
| CHEMBL1255588 | — | Ki | = | 3.61 | nM | 8.44 |
| CHEMBL85 | RISPERIDONE | Ki | = | 6.65 | nM | 8.18 |
| CHEMBL178700 | — | Ki | = | 447.0 | nM | 6.35 |
| CHEMBL179145 | — | Ki | = | 575.0 | nM | 6.24 |
| CHEMBL179371 | — | Ki | = | 866.0 | nM | 6.06 |
| CHEMBL178650 | — | Ki | = | 924.0 | nM | 6.03 |
| CHEMBL178519 | — | Ki | = | 1093.0 | nM | 5.96 |
| CHEMBL434905 | — | Ki | = | 1093.0 | nM | 5.96 |
| CHEMBL180327 | — | Ki | = | 1145.0 | nM | 5.94 |
| CHEMBL179373 | — | Ki | = | 2493.0 | nM | 5.60 |
| CHEMBL369133 | — | Ki | - | nM | - | |
| CHEMBL179697 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL179808 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL276784 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL425867 | — | Ki | - | nM | - | |
| CHEMBL360351 | — | Ki | - | nM | - | |
| CHEMBL178924 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL178680 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL179530 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL180119 | — | Ki | > | 1000.0 | nM | - |