Assay Detail
Binding
CHEMBL620755
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Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells
14
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 7.64 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282199 | — | — | 1 | 8.90 |
| CHEMBL25815 | — | — | 1 | 8.48 |
| CHEMBL28056 | — | — | 2 | 8.42 |
| CHEMBL25924 | — | — | 1 | 8.01 |
| CHEMBL283065 | — | — | 1 | 7.89 |
| CHEMBL27251 | — | — | 1 | 7.75 |
| CHEMBL26907 | — | — | 2 | 7.64 |
| CHEMBL12264 | SB-258719 | — | 1 | 7.50 |
| CHEMBL281273 | — | — | 1 | 7.44 |
| CHEMBL281357 | — | — | 1 | 7.06 |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 6.73 |
| CHEMBL282413 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282199 | — | Ki | = | 1.26 | nM | 8.90 |
| CHEMBL25815 | — | Ki | = | 3.31 | nM | 8.48 |
| CHEMBL28056 | — | Ki | = | 3.79 | nM | 8.42 |
| CHEMBL25924 | — | Ki | = | 9.78 | nM | 8.01 |
| CHEMBL283065 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL27251 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL28056 | — | Ki | = | 20.8 | nM | 7.68 |
| CHEMBL26907 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL12264 | SB-258719 | Ki | = | 31.6 | nM | 7.50 |
| CHEMBL281273 | — | Ki | = | 36.2 | nM | 7.44 |
| CHEMBL26907 | — | Ki | = | 43.1 | nM | 7.37 |
| CHEMBL281357 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL53 | APOMORPHINE | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL282413 | — | Ki | = | 708.0 | nM | 6.15 |