Assay Detail
ADMET
CHEMBL4397362
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Antagonist activity at recombinant human D2 receptor expressed in CHOK1 cells assessed as inhibition of quinpirole-induced beta arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D<sub>3</sub> Receptor (D<sub>3</sub>R) Ligand Promiscuity across Highly Conserved Aminergic G-Protein-Coupled Receptors (GPCRs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.36 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.80 |
| CHEMBL4083252 | — | — | 1 | 6.48 |
| CHEMBL4084262 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL4083252 | — | IC50 | = | 328.3 | nM | 6.48 |
| CHEMBL4084262 | — | IC50 | = | 1616.0 | nM | 5.79 |