Assay Detail
Binding
CHEMBL5635640
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Binding affinity to human D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment preincubated for 30 mins followed by dopamine addition and measured after 90 mins by pathhunter assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of bitopic ligands based on fallypride and evaluation of their affinity and selectivity towards dopamine D<sub>2</sub> and D<sub>3</sub> receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.60 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5647189 | — | — | 1 | 8.89 |
| CHEMBL392158 | FALLYPRIDE | 3.0 | 1 | 8.77 |
| CHEMBL5641844 | — | — | 1 | 8.48 |
| CHEMBL5647611 | — | — | 1 | 8.09 |
| CHEMBL5646972 | — | — | 1 | 7.96 |
| CHEMBL5639796 | — | — | 1 | 7.93 |
| CHEMBL5641522 | — | — | 1 | 7.20 |
| CHEMBL5639121 | — | — | 1 | 7.10 |
| CHEMBL5646837 | — | — | 1 | 6.77 |
| CHEMBL1739963 | — | — | 1 | 6.21 |
| CHEMBL4438361 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5647189 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL392158 | FALLYPRIDE | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5641844 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5647611 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5646972 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5639796 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL5641522 | — | IC50 | = | 62.7 | nM | 7.20 |
| CHEMBL5639121 | — | IC50 | = | 79.2 | nM | 7.10 |
| CHEMBL5646837 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL1739963 | — | IC50 | = | 611.7 | nM | 6.21 |
| CHEMBL4438361 | — | IC50 | = | 678.1 | nM | 6.17 |