Assay Detail
Binding
CHEMBL2167565
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Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.80 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164349 | — | — | 1 | 7.82 |
| CHEMBL2164346 | — | — | 1 | 7.46 |
| CHEMBL514874 | — | — | 1 | 7.28 |
| CHEMBL2164353 | — | — | 1 | 7.25 |
| CHEMBL2164348 | — | — | 1 | 7.16 |
| CHEMBL2164347 | — | — | 1 | 6.74 |
| CHEMBL2164345 | — | — | 1 | 6.60 |
| CHEMBL2164355 | — | — | 1 | 6.54 |
| CHEMBL2164354 | — | — | 1 | 6.42 |
| CHEMBL2164352 | — | — | 1 | 6.26 |
| CHEMBL2164351 | — | — | 1 | 6.09 |
| CHEMBL2164350 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164349 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2164346 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL514874 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL2164353 | — | Ki | = | 56.8 | nM | 7.25 |
| CHEMBL2164348 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL2164347 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL2164345 | — | Ki | = | 252.0 | nM | 6.60 |
| CHEMBL2164355 | — | Ki | = | 291.0 | nM | 6.54 |
| CHEMBL2164354 | — | Ki | = | 385.0 | nM | 6.42 |
| CHEMBL2164352 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL2164351 | — | Ki | = | 807.0 | nM | 6.09 |
| CHEMBL2164350 | — | Ki | = | 946.0 | nM | 6.02 |