Assay Detail
Binding
CHEMBL617896
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Ability to displace [3H]mesulergine (0.5 nM) from CHO cells of human 5-hydroxytryptamine 2C receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.13 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12314 | MESULERGINE | 2.0 | 1 | 9.04 |
| CHEMBL97242 | — | — | 1 | 6.39 |
| CHEMBL318901 | — | — | 1 | 5.96 |
| CHEMBL97333 | — | — | 1 | - |
| CHEMBL420997 | — | — | 1 | - |
| CHEMBL313424 | — | — | 1 | - |
| CHEMBL95175 | — | — | 1 | - |
| CHEMBL317333 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12314 | MESULERGINE | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL97242 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL318901 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL97333 | — | Ki | > | 4200.0 | nM | - |
| CHEMBL420997 | — | Ki | > | 4200.0 | nM | - |
| CHEMBL313424 | — | Ki | > | 4200.0 | nM | - |
| CHEMBL95175 | — | Ki | > | 4200.0 | nM | - |
| CHEMBL317333 | — | Ki | > | 4200.0 | nM | - |