Assay Detail
Binding
CHEMBL617878
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In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus.
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical antipsychotics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.50 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.80 |
| CHEMBL540822 | — | — | 1 | 7.09 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 7.04 |
| CHEMBL543613 | — | — | 1 | 6.90 |
| CHEMBL539544 | — | — | 1 | 6.69 |
| CHEMBL545488 | — | — | 1 | 6.40 |
| CHEMBL544318 | — | — | 1 | 6.04 |
| CHEMBL544319 | — | — | 1 | 6.03 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 5.60 |
| CHEMBL542428 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL540822 | — | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL85 | RISPERIDONE | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL543613 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL539544 | — | Ki | = | 204.17 | nM | 6.69 |
| CHEMBL545488 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL544318 | — | Ki | = | 912.01 | nM | 6.04 |
| CHEMBL544319 | — | Ki | = | 933.25 | nM | 6.03 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL542428 | — | Ki | = | 3981.07 | nM | 5.40 |