Assay Detail
Binding
CHEMBL2327488
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Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells after 30 mins by scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.84 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.35 |
| CHEMBL2325926 | — | — | 1 | 7.82 |
| CHEMBL2325930 | — | — | 1 | 7.57 |
| CHEMBL2325935 | — | — | 1 | 7.16 |
| CHEMBL2325932 | — | — | 1 | 7.12 |
| CHEMBL1259203 | — | — | 1 | 6.92 |
| CHEMBL319352 | — | — | 1 | 6.85 |
| CHEMBL2325928 | — | — | 1 | 6.82 |
| CHEMBL2326176 | — | — | 1 | 6.80 |
| CHEMBL2326175 | — | — | 1 | 6.66 |
| CHEMBL2325931 | — | — | 1 | 6.58 |
| CHEMBL328187 | — | — | 1 | 6.51 |
| CHEMBL2325934 | — | — | 1 | 6.08 |
| CHEMBL2325927 | — | — | 1 | 6.06 |
| CHEMBL2325933 | — | — | 1 | 5.96 |
| CHEMBL2325929 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL2325926 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2325930 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2325935 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL2325932 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL1259203 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL319352 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL2325928 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL2326176 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL2326175 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL2325931 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL328187 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL2325934 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL2325927 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL2325933 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL2325929 | — | Ki | = | 6400.0 | nM | 5.19 |