Assay Detail
Binding
CHEMBL618162
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Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Optimization of the pharmacophore model for 5-HT7R antagonism. Design and synthesis of new naphtholactam and naphthosultam derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.45 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282199 | — | — | 1 | 8.90 |
| CHEMBL347286 | — | — | 1 | 8.70 |
| CHEMBL12624 | SB-258741 | — | 1 | 8.50 |
| CHEMBL153398 | — | — | 1 | 8.40 |
| CHEMBL94261 | — | — | 1 | 8.00 |
| CHEMBL153156 | — | — | 1 | 8.00 |
| CHEMBL152595 | — | — | 1 | 7.80 |
| CHEMBL154090 | — | — | 1 | 7.80 |
| CHEMBL152292 | — | — | 1 | 7.70 |
| CHEMBL422146 | — | — | 1 | 7.50 |
| CHEMBL347115 | — | — | 1 | 7.50 |
| CHEMBL12264 | SB-258719 | — | 1 | 7.50 |
| CHEMBL152873 | — | — | 1 | 6.90 |
| CHEMBL151858 | — | — | 1 | 6.20 |
| CHEMBL347511 | — | — | 1 | 5.80 |
| CHEMBL345971 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282199 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL347286 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL12624 | SB-258741 | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL153398 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL94261 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL153156 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL152595 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL154090 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL152292 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL422146 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL347115 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL12264 | SB-258719 | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL152873 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL151858 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL347511 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL345971 | — | Ki | = | 100000.0 | nM | 4.00 |