Assay Detail
Functional
CHEMBL5046499
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Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Dual-Target μ-Opioid Receptor and Dopamine D<sub>3</sub> Receptor Ligands as Potential Nonaddictive Pharmacotherapeutics for Pain Management.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 7.33 | 9.05 |
| pEC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 9.05 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 8.62 |
| CHEMBL5073754 | — | — | 1 | 7.58 |
| CHEMBL5089655 | — | — | 1 | 6.78 |
| CHEMBL5085974 | — | — | 1 | 6.13 |
| CHEMBL5077114 | — | — | 1 | 5.83 |
| CHEMBL5075990 | — | — | 1 | - |
| CHEMBL5080654 | — | — | 1 | - |
| CHEMBL5082465 | — | — | 1 | - |
| CHEMBL5086564 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | EC50 | = | 0.8913 | nM | 9.05 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 2.399 | nM | 8.62 |
| CHEMBL5073754 | — | EC50 | = | 26.3 | nM | 7.58 |
| CHEMBL5089655 | — | EC50 | = | 165.96 | nM | 6.78 |
| CHEMBL5085974 | — | EC50 | = | 741.31 | nM | 6.13 |
| CHEMBL5077114 | — | EC50 | = | 1479.11 | nM | 5.83 |
| CHEMBL5075990 | — | pEC50 | - | — | - | |
| CHEMBL5080654 | — | pEC50 | - | — | - | |
| CHEMBL5082465 | — | pEC50 | - | — | - | |
| CHEMBL5086564 | — | EC50 | = | 45.6 | nM | - |