Assay Detail
Binding
CHEMBL4345338
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
16
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.02 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8809 | RACLOPRIDE | 2.0 | 2 | 8.74 |
| CHEMBL4439029 | — | — | 2 | 7.55 |
| CHEMBL4467483 | — | — | 2 | 7.52 |
| CHEMBL4442011 | — | — | 2 | 7.39 |
| CHEMBL4579687 | — | — | 2 | 7.35 |
| CHEMBL4564103 | — | — | 2 | 6.50 |
| CHEMBL4513262 | — | — | 2 | 5.71 |
| CHEMBL4589737 | — | — | 2 | 5.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8809 | RACLOPRIDE | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL8809 | RACLOPRIDE | IC50 | = | 1.83 | nM | 8.74 |
| CHEMBL4439029 | — | IC50 | = | 28.18 | nM | 7.55 |
| CHEMBL4439029 | — | IC50 | = | 28.2 | nM | 7.55 |
| CHEMBL4467483 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL4467483 | — | IC50 | = | 30.35 | nM | 7.52 |
| CHEMBL4442011 | — | IC50 | = | 40.74 | nM | 7.39 |
| CHEMBL4442011 | — | IC50 | = | 40.77 | nM | 7.39 |
| CHEMBL4579687 | — | IC50 | = | 44.67 | nM | 7.35 |
| CHEMBL4579687 | — | IC50 | = | 45.07 | nM | 7.35 |
| CHEMBL4564103 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4564103 | — | IC50 | = | 337.5 | nM | 6.47 |
| CHEMBL4513262 | — | IC50 | = | 1949.84 | nM | 5.71 |
| CHEMBL4513262 | — | IC50 | = | 1957.0 | nM | 5.71 |
| CHEMBL4589737 | — | IC50 | = | 3630.78 | nM | 5.44 |
| CHEMBL4589737 | — | IC50 | = | 3629.0 | nM | 5.44 |