Assay Detail
Binding
CHEMBL829975
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Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.35 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193639 | — | — | 2 | 9.68 |
| CHEMBL363581 | — | — | 1 | 9.19 |
| CHEMBL329566 | — | — | 1 | 9.03 |
| CHEMBL366164 | — | — | 1 | 8.82 |
| CHEMBL435301 | — | — | 1 | 8.62 |
| CHEMBL364270 | — | — | 1 | 8.43 |
| CHEMBL194659 | — | — | 1 | 8.37 |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 8.36 |
| CHEMBL195706 | — | — | 1 | 8.12 |
| CHEMBL193435 | — | — | 1 | 8.05 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 7.92 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.85 |
| CHEMBL195856 | — | — | 1 | 7.77 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.68 |
| CHEMBL654 | MIRTAZAPINE | 4.0 | 1 | 7.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193639 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL363581 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL329566 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL366164 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL435301 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL364270 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL194659 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL6437 | MIANSERIN | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL195706 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL193435 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL85 | RISPERIDONE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL715 | OLANZAPINE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL195856 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL42 | CLOZAPINE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL654 | MIRTAZAPINE | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL193639 | — | Ki | < | 0.42 | nM | - |