Assay Detail
Functional
CHEMBL3887361
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Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HTLA |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Functionally selective ligands of dopamine D2 receptors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 43 | 7.89 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3983588 | — | — | 1 | 9.40 |
| CHEMBL160296 | — | — | 1 | 9.30 |
| CHEMBL3912435 | — | — | 1 | 9.22 |
| CHEMBL3966956 | — | — | 1 | 9.05 |
| CHEMBL3982360 | — | — | 1 | 8.82 |
| CHEMBL3916047 | — | — | 1 | 8.66 |
| CHEMBL3957278 | — | — | 1 | 8.60 |
| CHEMBL2165120 | — | — | 1 | 8.55 |
| CHEMBL3918805 | — | — | 1 | 8.51 |
| CHEMBL2165126 | — | — | 1 | 8.48 |
| CHEMBL2165119 | — | — | 1 | 8.48 |
| CHEMBL3935170 | — | — | 1 | 8.40 |
| CHEMBL3952761 | — | — | 1 | 8.38 |
| CHEMBL3921903 | — | — | 1 | 8.38 |
| CHEMBL3891542 | — | — | 1 | 8.37 |
| CHEMBL3973357 | — | — | 1 | 8.34 |
| CHEMBL3978288 | — | — | 1 | 8.34 |
| CHEMBL3944009 | — | — | 1 | 8.32 |
| CHEMBL3929710 | — | — | 1 | 8.21 |
| CHEMBL3943838 | — | — | 1 | 8.21 |
| CHEMBL2165118 | — | — | 1 | 8.10 |
| CHEMBL3915863 | — | — | 1 | 8.07 |
| CHEMBL3899117 | — | — | 1 | 8.04 |
| CHEMBL3937643 | — | — | 1 | 7.77 |
| CHEMBL2165133 | — | — | 1 | 7.75 |
| CHEMBL2165114 | — | — | 1 | 7.64 |
| CHEMBL2165115 | — | — | 1 | 7.60 |
| CHEMBL3934712 | — | — | 1 | 7.60 |
| CHEMBL3896746 | — | — | 1 | 7.58 |
| CHEMBL2165117 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3983588 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL160296 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3912435 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3966956 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3982360 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3916047 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3957278 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2165120 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3918805 | — | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL2165126 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2165119 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3935170 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3952761 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3921903 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3891542 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3973357 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3978288 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3944009 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3929710 | — | EC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3943838 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL2165118 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3915863 | — | EC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3899117 | — | EC50 | = | 9.2 | nM | 8.04 |
| CHEMBL3937643 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2165133 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2165114 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2165115 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3934712 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3896746 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2165117 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2165131 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL2165116 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2165140 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2165135 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL2165136 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3898054 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2165137 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2165134 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL2165138 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2165139 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL2165132 | — | EC50 | = | 399.0 | nM | 6.40 |
| CHEMBL2165129 | — | EC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3903542 | — | EC50 | = | 2100.0 | nM | 5.68 |