Assay Detail
Binding
CHEMBL4032441
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Displacement of [125I]ABN from human dopamine D2 long 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 | 5.27 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 10.22 |
| CHEMBL4083252 | — | — | 1 | 6.58 |
| CHEMBL4062553 | — | — | 1 | 5.21 |
| CHEMBL4076516 | — | — | 1 | 5.20 |
| CHEMBL4101993 | — | — | 1 | 5.12 |
| CHEMBL4073927 | — | — | 1 | 5.01 |
| CHEMBL4084262 | — | — | 1 | 4.96 |
| CHEMBL4077251 | — | — | 1 | 4.67 |
| CHEMBL4092015 | — | — | 1 | 4.53 |
| CHEMBL4071189 | — | — | 1 | 4.42 |
| CHEMBL4076086 | — | — | 1 | 4.24 |
| CHEMBL4089290 | — | — | 1 | 4.22 |
| CHEMBL4076527 | — | — | 1 | 4.08 |
| CHEMBL4098399 | — | — | 1 | - |
| CHEMBL4079642 | — | — | 1 | - |
| CHEMBL4100699 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL4083252 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL4062553 | — | Ki | = | 6168.0 | nM | 5.21 |
| CHEMBL4076516 | — | Ki | = | 6370.0 | nM | 5.20 |
| CHEMBL4101993 | — | Ki | = | 7501.0 | nM | 5.12 |
| CHEMBL4073927 | — | Ki | = | 9792.0 | nM | 5.01 |
| CHEMBL4084262 | — | Ki | = | 10895.0 | nM | 4.96 |
| CHEMBL4077251 | — | Ki | = | 21216.0 | nM | 4.67 |
| CHEMBL4092015 | — | Ki | = | 29300.0 | nM | 4.53 |
| CHEMBL4071189 | — | Ki | = | 37579.0 | nM | 4.42 |
| CHEMBL4076086 | — | Ki | = | 57101.0 | nM | 4.24 |
| CHEMBL4089290 | — | Ki | = | 60152.0 | nM | 4.22 |
| CHEMBL4076527 | — | Ki | = | 83671.0 | nM | 4.08 |
| CHEMBL4098399 | — | Ki | > | 109574.0 | nM | - |
| CHEMBL4079642 | — | Ki | = | 114945.0 | nM | - |
| CHEMBL4100699 | — | Ki | = | 104847.0 | nM | - |