Assay Detail
Functional
CHEMBL5363883
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
25
Total Activities
13
Compounds Tested
3
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
Pharmacological and Physicochemical Properties Optimization for Dual-Target Dopamine D<sub>3</sub> (D<sub>3</sub>R) and μ-Opioid (MOR) Receptor Ligands as Potentially Safer Analgesics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.48 | 8.56 |
| EC50 | 12 | 6.48 | 8.56 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | 8.56 |
| CHEMBL5414796 | — | — | 2 | 7.10 |
| CHEMBL5395539 | — | — | 2 | 7.04 |
| CHEMBL5399270 | — | — | 2 | 6.57 |
| CHEMBL5433458 | — | — | 2 | 6.57 |
| CHEMBL5412606 | — | — | 2 | 6.50 |
| CHEMBL5404724 | — | — | 2 | 6.41 |
| CHEMBL5415842 | — | — | 2 | 6.25 |
| CHEMBL5412995 | — | — | 2 | 6.21 |
| CHEMBL5397609 | — | — | 2 | 5.76 |
| CHEMBL5434650 | — | — | 2 | 5.53 |
| CHEMBL5398913 | — | — | 2 | 5.26 |
| CHEMBL5432993 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | IC50 | = | 2.754 | nM | 8.56 |
| CHEMBL54 | HALOPERIDOL | EC50 | = | 2.76 | nM | 8.56 |
| CHEMBL5414796 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL5414796 | — | EC50 | = | 78.9 | nM | 7.10 |
| CHEMBL5395539 | — | EC50 | = | 90.9 | nM | 7.04 |
| CHEMBL5395539 | — | IC50 | = | 91.2 | nM | 7.04 |
| CHEMBL5433458 | — | EC50 | = | 271.0 | nM | 6.57 |
| CHEMBL5433458 | — | IC50 | = | 269.15 | nM | 6.57 |
| CHEMBL5399270 | — | IC50 | = | 269.15 | nM | 6.57 |
| CHEMBL5399270 | — | EC50 | = | 269.0 | nM | 6.57 |
| CHEMBL5412606 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL5412606 | — | EC50 | = | 316.0 | nM | 6.50 |
| CHEMBL5404724 | — | EC50 | = | 386.0 | nM | 6.41 |
| CHEMBL5404724 | — | IC50 | = | 389.05 | nM | 6.41 |
| CHEMBL5415842 | — | IC50 | = | 562.34 | nM | 6.25 |
| CHEMBL5415842 | — | EC50 | = | 566.0 | nM | 6.25 |
| CHEMBL5412995 | — | IC50 | = | 616.6 | nM | 6.21 |
| CHEMBL5412995 | — | EC50 | = | 616.0 | nM | 6.21 |
| CHEMBL5397609 | — | IC50 | = | 1737.8 | nM | 5.76 |
| CHEMBL5397609 | — | EC50 | = | 1737.0 | nM | 5.76 |
| CHEMBL5434650 | — | IC50 | = | 2951.21 | nM | 5.53 |
| CHEMBL5434650 | — | EC50 | = | 2962.0 | nM | 5.53 |
| CHEMBL5398913 | — | EC50 | = | 5446.0 | nM | 5.26 |
| CHEMBL5398913 | — | IC50 | = | 5495.41 | nM | 5.26 |
| CHEMBL5432993 | — | Activity | - | — | - |