Assay Detail
Binding
CHEMBL2211561
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]methylspiperone from human low affinity Dopamine D2S receptor by competition binding assay
19
Total Activities
19
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.62 | 8.57 |
| Ki(app) | 1 | - | - |
| IC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 8.57 |
| CHEMBL708 | ZIPRASIDONE | 4.0 | 1 | 8.07 |
| CHEMBL1423 | PIMOZIDE | 4.0 | 1 | 7.93 |
| CHEMBL2207484 | — | — | 1 | 7.57 |
| CHEMBL2207486 | — | — | 1 | 7.50 |
| CHEMBL2207496 | — | — | 1 | 6.95 |
| CHEMBL2207487 | — | — | 1 | 6.92 |
| CHEMBL2207489 | — | — | 1 | 6.71 |
| CHEMBL2207485 | — | — | 1 | 6.56 |
| CHEMBL2207493 | — | — | 1 | 6.43 |
| CHEMBL2207490 | — | — | 1 | 5.97 |
| CHEMBL2207491 | — | — | 1 | 5.95 |
| CHEMBL2207494 | — | — | 1 | 5.70 |
| CHEMBL2207498 | — | — | 1 | 5.63 |
| CHEMBL2207488 | — | — | 1 | 5.57 |
| CHEMBL2207497 | — | — | 1 | 5.54 |
| CHEMBL2207495 | — | — | 1 | 4.92 |
| CHEMBL2207492 | — | — | 1 | - |
| CHEMBL86304 | MOCLOBEMIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL708 | ZIPRASIDONE | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL1423 | PIMOZIDE | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL2207484 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2207486 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL2207496 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL2207487 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL2207489 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL2207485 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL2207493 | — | Ki | = | 371.0 | nM | 6.43 |
| CHEMBL2207490 | — | Ki | = | 1066.0 | nM | 5.97 |
| CHEMBL2207491 | — | Ki | = | 1136.0 | nM | 5.95 |
| CHEMBL2207494 | — | Ki | = | 2002.0 | nM | 5.70 |
| CHEMBL2207498 | — | Ki | = | 2325.0 | nM | 5.63 |
| CHEMBL2207488 | — | Ki | = | 2717.0 | nM | 5.57 |
| CHEMBL2207497 | — | Ki | = | 2870.0 | nM | 5.54 |
| CHEMBL2207495 | — | Ki | = | 12160.0 | nM | 4.92 |
| CHEMBL2207492 | — | IC50 | > | 580000.0 | nM | - |
| CHEMBL86304 | MOCLOBEMIDE | Ki(app) | - | — | - |