Assay Detail
Binding
CHEMBL3117737
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]spiperone from low-affinity state of human dopamine D2S receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
26
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 6.95 | 8.31 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL538542 | — | — | 2 | 8.31 |
| CHEMBL2106804 | NAXAGOLIDE HYDROCHLORIDE | -1.0 | 2 | 7.77 |
| CHEMBL3115575 | — | — | 2 | 7.54 |
| CHEMBL3115574 | — | — | 2 | 7.09 |
| CHEMBL3115576 | — | — | 2 | 7.08 |
| CHEMBL3115579 | — | — | 2 | 7.04 |
| CHEMBL3115578 | — | — | 2 | 7.02 |
| CHEMBL134807 | — | — | 2 | 6.73 |
| CHEMBL3115582 | — | — | 2 | 6.63 |
| CHEMBL3115585 | — | — | 2 | 6.59 |
| CHEMBL3115580 | — | — | 2 | 6.45 |
| CHEMBL1557 | DOPAMINE HYDROCHLORIDE | 4.0 | 2 | 6.06 |
| CHEMBL3115581 | — | — | 1 | - |
| CHEMBL3115577 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL538542 | — | Ki | = | 4.898 | nM | 8.31 |
| CHEMBL538542 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL2106804 | NAXAGOLIDE HYDROCHLORIDE | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL2106804 | NAXAGOLIDE HYDROCHLORIDE | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL3115575 | — | Ki | = | 28.84 | nM | 7.54 |
| CHEMBL3115575 | — | Ki | = | 30.8 | nM | 7.51 |
| CHEMBL3115574 | — | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL3115576 | — | Ki | = | 83.18 | nM | 7.08 |
| CHEMBL3115579 | — | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL3115579 | — | Ki | = | 92.7 | nM | 7.03 |
| CHEMBL3115578 | — | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL3115578 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL3115574 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL3115576 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL134807 | — | Ki | = | 186.21 | nM | 6.73 |
| CHEMBL3115582 | — | Ki | = | 234.42 | nM | 6.63 |
| CHEMBL3115582 | — | Ki | = | 252.0 | nM | 6.60 |
| CHEMBL3115585 | — | Ki | = | 257.04 | nM | 6.59 |
| CHEMBL3115585 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL3115580 | — | Ki | = | 354.81 | nM | 6.45 |
| CHEMBL3115580 | — | Ki | = | 452.0 | nM | 6.34 |
| CHEMBL134807 | — | Ki | = | 736.0 | nM | 6.13 |
| CHEMBL1557 | DOPAMINE HYDROCHLORIDE | Ki | = | 870.96 | nM | 6.06 |
| CHEMBL1557 | DOPAMINE HYDROCHLORIDE | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL3115577 | — | Inhibition | - | % | - | |
| CHEMBL3115581 | — | Inhibition | - | % | - |