Assay Detail
Binding
CHEMBL619862
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Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 11 | 7.85 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL428892 | — | — | 1 | 9.00 |
| CHEMBL19215 | METERGOLINE | 2.0 | 1 | 8.20 |
| CHEMBL12314 | MESULERGINE | 2.0 | 1 | 8.10 |
| CHEMBL274384 | — | — | 1 | 8.00 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.90 |
| CHEMBL1065 | METHYSERGIDE | 4.0 | 1 | 7.90 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 7.80 |
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 7.70 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 1 | 7.30 |
| CHEMBL1255588 | — | — | 1 | 7.20 |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL428892 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL19215 | METERGOLINE | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL12314 | MESULERGINE | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL274384 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL42 | CLOZAPINE | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1065 | METHYSERGIDE | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL267777 | RITANSERIN | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL267930 | SPIPERONE | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1255588 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL6437 | MIANSERIN | Ki | = | 63.1 | nM | 7.20 |