Assay Detail
Binding
CHEMBL4032440
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Displacement of [125I]ABN from human dopamine D3 receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting method
16
Total Activities
16
Compounds Tested
1
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
Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.10 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 9.48 |
| CHEMBL4083252 | — | — | 1 | 8.19 |
| CHEMBL4084262 | — | — | 1 | 7.92 |
| CHEMBL4062553 | — | — | 1 | 7.71 |
| CHEMBL4076516 | — | — | 1 | 7.62 |
| CHEMBL4073927 | — | — | 1 | 7.59 |
| CHEMBL4101993 | — | — | 1 | 7.08 |
| CHEMBL4100699 | — | — | 1 | 7.01 |
| CHEMBL4092015 | — | — | 1 | 6.77 |
| CHEMBL4089290 | — | — | 1 | 6.72 |
| CHEMBL4071189 | — | — | 1 | 6.63 |
| CHEMBL4076086 | — | — | 1 | 6.36 |
| CHEMBL4077251 | — | — | 1 | 6.08 |
| CHEMBL4076527 | — | — | 1 | 6.06 |
| CHEMBL4079642 | — | — | 1 | 5.32 |
| CHEMBL4098399 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL4083252 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4084262 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4062553 | — | Ki | = | 19.6 | nM | 7.71 |
| CHEMBL4076516 | — | Ki | = | 24.2 | nM | 7.62 |
| CHEMBL4073927 | — | Ki | = | 25.6 | nM | 7.59 |
| CHEMBL4101993 | — | Ki | = | 82.4 | nM | 7.08 |
| CHEMBL4100699 | — | Ki | = | 97.7 | nM | 7.01 |
| CHEMBL4092015 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL4089290 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL4071189 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL4076086 | — | Ki | = | 438.0 | nM | 6.36 |
| CHEMBL4077251 | — | Ki | = | 833.0 | nM | 6.08 |
| CHEMBL4076527 | — | Ki | = | 871.0 | nM | 6.06 |
| CHEMBL4079642 | — | Ki | = | 4790.0 | nM | 5.32 |
| CHEMBL4098399 | — | Ki | = | 181888.0 | nM | - |