Assay Detail
Binding
CHEMBL1680101
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Displacement of [3H]domperidone from dopamine D2 receptor high binding site in Sprague-Dawley rat striatum by scintillation counting
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and Evaluation of Fluorinated Aporphines: Potential Positron Emission Tomography Ligands for D2 Receptors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.49 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225230 | R-N-PROPYLNORAPOMORPHINE | — | 1 | 9.74 |
| CHEMBL1672309 | — | — | 1 | 9.27 |
| CHEMBL1672312 | — | — | 1 | 9.08 |
| CHEMBL1672313 | — | — | 1 | 8.92 |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 8.74 |
| CHEMBL1672308 | — | — | 1 | 8.70 |
| CHEMBL1672306 | — | — | 1 | 8.60 |
| CHEMBL106622 | — | — | 1 | 8.57 |
| CHEMBL1672311 | — | — | 1 | 8.49 |
| CHEMBL1672310 | — | — | 1 | 8.46 |
| CHEMBL1672304 | — | — | 1 | 8.43 |
| CHEMBL27559 | — | — | 1 | 8.31 |
| CHEMBL53294 | — | — | 1 | 8.29 |
| CHEMBL1672305 | — | — | 1 | 8.21 |
| CHEMBL1672302 | — | — | 1 | 8.16 |
| CHEMBL405345 | — | — | 1 | 7.70 |
| CHEMBL1672303 | — | — | 1 | 7.55 |
| CHEMBL1672307 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225230 | R-N-PROPYLNORAPOMORPHINE | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL1672309 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL1672312 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL1672313 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL53 | APOMORPHINE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1672308 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1672306 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL106622 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1672311 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL1672310 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL1672304 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL27559 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL53294 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL1672305 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL1672302 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL405345 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1672303 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL1672307 | — | Ki | = | 31.0 | nM | 7.51 |