Assay Detail
Functional
CHEMBL2328744
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| IC50 | 28 | 5.80 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218166 | BIFEPRUNOX | 3.0 | 1 | 8.54 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.12 |
| CHEMBL2326481 | — | — | 1 | 6.52 |
| CHEMBL2326478 | — | — | 1 | 6.40 |
| CHEMBL2326479 | — | — | 1 | 6.40 |
| CHEMBL2326477 | — | — | 1 | 6.22 |
| CHEMBL2326486 | — | — | 1 | 6.17 |
| CHEMBL2326472 | — | — | 1 | 6.06 |
| CHEMBL2326480 | — | — | 1 | 6.05 |
| CHEMBL2326482 | — | — | 1 | 6.00 |
| CHEMBL2326469 | — | — | 1 | 5.92 |
| CHEMBL2326488 | — | — | 1 | 5.85 |
| CHEMBL2326470 | — | — | 1 | 5.82 |
| CHEMBL2326484 | — | — | 1 | 5.77 |
| CHEMBL2326468 | — | — | 1 | 5.60 |
| CHEMBL2326476 | — | — | 1 | 5.54 |
| CHEMBL2326473 | — | — | 1 | 5.36 |
| CHEMBL2326490 | — | — | 1 | 5.35 |
| CHEMBL2326485 | — | — | 1 | 5.35 |
| CHEMBL2326487 | — | — | 1 | 5.12 |
| CHEMBL2326492 | — | — | 1 | 5.11 |
| CHEMBL2326483 | — | — | 1 | 5.10 |
| CHEMBL2326475 | — | — | 1 | 5.00 |
| CHEMBL2326474 | — | — | 1 | 5.00 |
| CHEMBL2326471 | — | — | 1 | 5.00 |
| CHEMBL2326489 | — | — | 1 | 4.72 |
| CHEMBL2326491 | — | — | 1 | 4.52 |
| CHEMBL301265 | PRAMIPEXOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218166 | BIFEPRUNOX | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1112 | ARIPIPRAZOLE | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL2326481 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2326478 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2326479 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2326477 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2326486 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL2326472 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL2326480 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2326482 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2326469 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2326488 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2326470 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2326484 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2326468 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2326476 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2326473 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL2326490 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2326485 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2326487 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL2326492 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL2326483 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL2326475 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2326474 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2326471 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2326489 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL2326491 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL301265 | PRAMIPEXOLE | IC50 | > | 10000.0 | nM | - |