Assay Detail
Functional
CHEMBL2168916
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
28
Total Activities
28
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 | 28 | 8.05 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL160357 | — | — | 1 | 9.40 |
| CHEMBL443034 | — | — | 1 | 9.10 |
| CHEMBL160630 | — | — | 1 | 9.10 |
| CHEMBL160921 | — | — | 1 | 9.10 |
| CHEMBL2165119 | — | — | 1 | 8.80 |
| CHEMBL2165121 | — | — | 1 | 8.70 |
| CHEMBL157923 | — | — | 1 | 8.70 |
| CHEMBL2165125 | — | — | 1 | 8.70 |
| CHEMBL2165120 | — | — | 1 | 8.60 |
| CHEMBL2165122 | — | — | 1 | 8.60 |
| CHEMBL346129 | — | — | 1 | 8.49 |
| CHEMBL1774063 | — | — | 1 | 8.49 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.40 |
| CHEMBL160744 | — | — | 1 | 8.30 |
| CHEMBL161792 | — | — | 1 | 8.20 |
| CHEMBL2165118 | — | — | 1 | 8.20 |
| CHEMBL2165123 | — | — | 1 | 8.00 |
| CHEMBL2165115 | — | — | 1 | 7.70 |
| CHEMBL2165117 | — | — | 1 | 7.70 |
| CHEMBL2165114 | — | — | 1 | 7.60 |
| CHEMBL2165124 | — | — | 1 | 7.30 |
| CHEMBL2165138 | — | — | 1 | 7.30 |
| CHEMBL2165140 | — | — | 1 | 7.20 |
| CHEMBL2165127 | — | — | 1 | 7.10 |
| CHEMBL2165137 | — | — | 1 | 7.10 |
| CHEMBL2165139 | — | — | 1 | 6.90 |
| CHEMBL2165116 | — | — | 1 | 6.70 |
| CHEMBL2165130 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL160357 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL443034 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL160630 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL160921 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2165119 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2165121 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL157923 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2165125 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2165120 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2165122 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL346129 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1774063 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL160744 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL161792 | — | EC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2165118 | — | EC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2165123 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2165115 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2165117 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2165114 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2165124 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2165138 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2165140 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2165127 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL2165137 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL2165139 | — | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL2165116 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2165130 | — | EC50 | = | 1260.0 | nM | 5.90 |