Assay Detail
Binding
CHEMBL669148
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Displacement of [3H]raclopride from human dopamine D2A receptors expressed in LtK cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LtK |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.13 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.36 |
| CHEMBL67923 | — | — | 1 | 7.66 |
| CHEMBL71599 | — | — | 1 | 7.36 |
| CHEMBL68573 | — | — | 1 | 7.34 |
| CHEMBL433121 | — | — | 1 | 7.23 |
| CHEMBL68545 | — | — | 1 | 7.18 |
| CHEMBL71275 | — | — | 1 | 6.94 |
| CHEMBL303502 | — | — | 1 | 6.90 |
| CHEMBL69706 | — | — | 1 | 6.82 |
| CHEMBL69985 | — | — | 1 | 6.70 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 6.12 |
| CHEMBL65896 | — | — | 1 | 6.00 |
| CHEMBL69705 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL67923 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL71599 | — | Ki | = | 43.8 | nM | 7.36 |
| CHEMBL68573 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL433121 | — | Ki | = | 59.2 | nM | 7.23 |
| CHEMBL68545 | — | Ki | = | 65.6 | nM | 7.18 |
| CHEMBL71275 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL303502 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL69706 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL69985 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL59 | DOPAMINE | Ki | = | 759.0 | nM | 6.12 |
| CHEMBL65896 | — | Ki | = | 1010.0 | nM | 6.00 |
| CHEMBL69705 | — | Ki | > | 5000.0 | nM | - |