Assay Detail
Binding
CHEMBL4345336
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at C-terminal RLuc8-fused D1R (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 | 6.35 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL62 | SCH-23390 | — | 2 | 8.36 |
| CHEMBL4564103 | — | — | 2 | 7.00 |
| CHEMBL4513262 | — | — | 2 | 6.63 |
| CHEMBL4579687 | — | — | 2 | 6.09 |
| CHEMBL4589737 | — | — | 2 | 5.85 |
| CHEMBL4442011 | — | — | 2 | 5.82 |
| CHEMBL4439029 | — | — | 2 | 5.80 |
| CHEMBL4467483 | — | — | 2 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL62 | SCH-23390 | IC50 | = | 4.365 | nM | 8.36 |
| CHEMBL62 | SCH-23390 | IC50 | = | 4.34 | nM | 8.36 |
| CHEMBL4564103 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4564103 | — | IC50 | = | 110.7 | nM | 6.96 |
| CHEMBL4513262 | — | IC50 | = | 232.4 | nM | 6.63 |
| CHEMBL4513262 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4579687 | — | IC50 | = | 815.7 | nM | 6.09 |
| CHEMBL4589737 | — | IC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL4589737 | — | IC50 | = | 1427.0 | nM | 5.85 |
| CHEMBL4579687 | — | IC50 | = | 1479.11 | nM | 5.83 |
| CHEMBL4442011 | — | IC50 | = | 1513.56 | nM | 5.82 |
| CHEMBL4442011 | — | IC50 | = | 1522.0 | nM | 5.82 |
| CHEMBL4439029 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4439029 | — | IC50 | = | 1603.0 | nM | 5.79 |
| CHEMBL4467483 | — | IC50 | = | 4073.8 | nM | 5.39 |
| CHEMBL4467483 | — | IC50 | = | 4080.0 | nM | 5.39 |