Assay Detail
Binding
CHEMBL872784
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Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 7.15 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98305 | — | — | 1 | 7.75 |
| CHEMBL330216 | — | — | 1 | 7.35 |
| CHEMBL70565 | — | — | 1 | 6.77 |
| CHEMBL98836 | — | — | 1 | 6.71 |
| CHEMBL98197 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98305 | — | Ki | = | 17.6 | nM | 7.75 |
| CHEMBL330216 | — | Ki | = | 44.4 | nM | 7.35 |
| CHEMBL70565 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL98836 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL98197 | — | Ki | > | 3300.0 | nM | - |