Assay Detail
Binding
CHEMBL2328745
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Displacement of [3H]raclopride from human D2 dopamine receptor expressed in CHO cell membranes
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D2 partial agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 6.65 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 9.70 |
| CHEMBL218166 | BIFEPRUNOX | 3.0 | 1 | 9.22 |
| CHEMBL2326472 | — | — | 1 | 7.82 |
| CHEMBL2326480 | — | — | 1 | 7.47 |
| CHEMBL2326485 | — | — | 1 | 7.42 |
| CHEMBL2326482 | — | — | 1 | 7.38 |
| CHEMBL2326481 | — | — | 1 | 7.38 |
| CHEMBL2326478 | — | — | 1 | 7.38 |
| CHEMBL2326477 | — | — | 1 | 7.12 |
| CHEMBL2326476 | — | — | 1 | 7.10 |
| CHEMBL2326479 | — | — | 1 | 7.04 |
| CHEMBL2326486 | — | — | 1 | 6.82 |
| CHEMBL2326484 | — | — | 1 | 6.70 |
| CHEMBL2326468 | — | — | 1 | 6.50 |
| CHEMBL2326473 | — | — | 1 | 6.46 |
| CHEMBL2326469 | — | — | 1 | 6.31 |
| CHEMBL2326470 | — | — | 1 | 6.24 |
| CHEMBL2326474 | — | — | 1 | 6.10 |
| CHEMBL2326490 | — | — | 1 | 5.96 |
| CHEMBL2326488 | — | — | 1 | 5.82 |
| CHEMBL2326489 | — | — | 1 | 5.60 |
| CHEMBL2326487 | — | — | 1 | 5.41 |
| CHEMBL2326475 | — | — | 1 | 5.37 |
| CHEMBL2326483 | — | — | 1 | 5.30 |
| CHEMBL2326492 | — | — | 1 | 5.30 |
| CHEMBL2326491 | — | — | 1 | 5.30 |
| CHEMBL2326471 | — | — | 1 | 5.30 |
| CHEMBL301265 | PRAMIPEXOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL218166 | BIFEPRUNOX | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2326472 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2326480 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL2326485 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL2326482 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL2326481 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL2326478 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL2326477 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL2326476 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL2326479 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL2326486 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL2326484 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2326468 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL2326473 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL2326469 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL2326470 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL2326474 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL2326490 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL2326488 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL2326489 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL2326487 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL2326475 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL2326483 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL2326492 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL2326491 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL2326471 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL301265 | PRAMIPEXOLE | Ki | - | — | - |