Assay Detail
Binding
CHEMBL673593
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]raclopride from human dopamine receptor D2A expressed in mouse Ltk cells
14
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ltk |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Atropisomeric derivatives of 2',6'-disubstituted (R)-11-phenylaporphine: selective serotonin 5-HT(7) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.09 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 7.38 |
| CHEMBL25815 | — | — | 1 | 6.98 |
| CHEMBL25924 | — | — | 1 | 6.63 |
| CHEMBL282199 | — | — | 1 | 6.50 |
| CHEMBL28056 | — | — | 2 | 6.30 |
| CHEMBL281357 | — | — | 1 | 6.28 |
| CHEMBL283065 | — | — | 1 | 5.69 |
| CHEMBL27251 | — | — | 1 | 5.65 |
| CHEMBL282413 | — | — | 1 | 5.65 |
| CHEMBL26907 | — | — | 2 | 5.60 |
| CHEMBL12264 | SB-258719 | — | 1 | 5.40 |
| CHEMBL281273 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53 | APOMORPHINE | Ki | = | 41.9 | nM | 7.38 |
| CHEMBL25815 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL25924 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL282199 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL28056 | — | Ki | = | 498.0 | nM | 6.30 |
| CHEMBL281357 | — | Ki | = | 527.0 | nM | 6.28 |
| CHEMBL283065 | — | Ki | = | 2030.0 | nM | 5.69 |
| CHEMBL27251 | — | Ki | = | 2250.0 | nM | 5.65 |
| CHEMBL282413 | — | Ki | = | 2260.0 | nM | 5.65 |
| CHEMBL28056 | — | Ki | = | 2470.0 | nM | 5.61 |
| CHEMBL26907 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL26907 | — | Ki | = | 3380.0 | nM | 5.47 |
| CHEMBL12264 | SB-258719 | Ki | = | 3981.0 | nM | 5.40 |
| CHEMBL281273 | — | Ki | > | 1000.0 | nM | - |