Assay Detail
Functional
CHEMBL3887360
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cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| 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 | 25 | 7.45 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3921903 | — | — | 1 | 10.00 |
| CHEMBL3978288 | — | — | 1 | 9.70 |
| CHEMBL3912435 | — | — | 1 | 9.40 |
| CHEMBL3983588 | — | — | 1 | 8.74 |
| CHEMBL2165118 | — | — | 1 | 8.25 |
| CHEMBL2165132 | — | — | 1 | 8.24 |
| CHEMBL2165134 | — | — | 1 | 8.24 |
| CHEMBL3918805 | — | — | 1 | 8.21 |
| CHEMBL2165139 | — | — | 1 | 8.01 |
| CHEMBL2165116 | — | — | 1 | 8.01 |
| CHEMBL3937643 | — | — | 1 | 7.96 |
| CHEMBL2165119 | — | — | 1 | 7.89 |
| CHEMBL3916047 | — | — | 1 | 7.89 |
| CHEMBL2165137 | — | — | 1 | 7.68 |
| CHEMBL3944009 | — | — | 1 | 7.57 |
| CHEMBL2165126 | — | — | 1 | 6.90 |
| CHEMBL3973357 | — | — | 1 | 6.79 |
| CHEMBL3929710 | — | — | 1 | 6.65 |
| CHEMBL3957278 | — | — | 1 | 6.51 |
| CHEMBL2165140 | — | — | 1 | 6.46 |
| CHEMBL3934712 | — | — | 1 | 6.29 |
| CHEMBL2165129 | — | — | 1 | 6.00 |
| CHEMBL2165133 | — | — | 1 | 5.43 |
| CHEMBL3943838 | — | — | 1 | 5.01 |
| CHEMBL3903542 | — | — | 1 | 4.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3921903 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3978288 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3912435 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3983588 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2165118 | — | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL2165132 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL2165134 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3918805 | — | EC50 | = | 6.1 | nM | 8.21 |
| CHEMBL2165139 | — | EC50 | = | 9.8 | nM | 8.01 |
| CHEMBL2165116 | — | EC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3937643 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2165119 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3916047 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2165137 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3944009 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2165126 | — | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL3973357 | — | EC50 | = | 163.0 | nM | 6.79 |
| CHEMBL3929710 | — | EC50 | = | 222.0 | nM | 6.65 |
| CHEMBL3957278 | — | EC50 | = | 306.0 | nM | 6.51 |
| CHEMBL2165140 | — | EC50 | = | 348.0 | nM | 6.46 |
| CHEMBL3934712 | — | EC50 | = | 512.0 | nM | 6.29 |
| CHEMBL2165129 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2165133 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3943838 | — | EC50 | = | 9870.0 | nM | 5.01 |
| CHEMBL3903542 | — | EC50 | = | 46000.0 | nM | 4.34 |