Assay Detail
Binding
CHEMBL615975
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Displacement of [3H]8-OH-DPAT from human 5-hydroxytryptamine 1A receptor expressed in CHO cells
14
Total Activities
12
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 | 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 | 6.86 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25924 | — | — | 1 | 8.74 |
| CHEMBL26907 | — | — | 2 | 7.31 |
| CHEMBL281357 | — | — | 1 | 7.10 |
| CHEMBL281273 | — | — | 1 | 6.86 |
| CHEMBL28056 | — | — | 2 | 6.85 |
| CHEMBL25815 | — | — | 1 | 6.77 |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 6.53 |
| CHEMBL27251 | — | — | 1 | 6.45 |
| CHEMBL283065 | — | — | 1 | 6.26 |
| CHEMBL282199 | — | — | 1 | - |
| CHEMBL282413 | — | — | 1 | - |
| CHEMBL12264 | SB-258719 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25924 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL26907 | — | Ki | = | 48.8 | nM | 7.31 |
| CHEMBL281357 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL281273 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL28056 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL25815 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL53 | APOMORPHINE | Ki | = | 296.0 | nM | 6.53 |
| CHEMBL26907 | — | Ki | = | 319.0 | nM | 6.50 |
| CHEMBL27251 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL283065 | — | Ki | = | 554.0 | nM | 6.26 |
| CHEMBL28056 | — | Ki | = | 778.0 | nM | 6.11 |
| CHEMBL282199 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL282413 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL12264 | SB-258719 | Ki | > | 7943.0 | nM | - |