Assay Detail
Functional
CHEMBL2168902
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Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HTLA |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-functional selectivity relationship studies of β-arrestin-biased dopamine D₂ receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 7.36 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL160296 | — | — | 1 | 9.22 |
| CHEMBL2165126 | — | — | 1 | 8.70 |
| CHEMBL2165133 | — | — | 1 | 8.40 |
| CHEMBL2165135 | — | — | 1 | 7.80 |
| CHEMBL2165136 | — | — | 1 | 7.20 |
| CHEMBL2165134 | — | — | 1 | 7.00 |
| CHEMBL2165129 | — | — | 1 | 6.70 |
| CHEMBL2165131 | — | — | 1 | 6.50 |
| CHEMBL2165132 | — | — | 1 | 6.30 |
| CHEMBL2165128 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL160296 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2165126 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2165133 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2165135 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2165136 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2165134 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2165129 | — | EC50 | = | 199.0 | nM | 6.70 |
| CHEMBL2165131 | — | EC50 | = | 316.0 | nM | 6.50 |
| CHEMBL2165132 | — | EC50 | = | 501.0 | nM | 6.30 |
| CHEMBL2165128 | — | EC50 | = | 1580.0 | nM | 5.80 |