Assay Detail
Binding
CHEMBL617327
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 26 | 7.69 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 9.70 |
| CHEMBL544091 | — | — | 1 | 8.84 |
| CHEMBL308480 | — | — | 1 | 8.80 |
| CHEMBL554199 | — | — | 1 | 8.76 |
| CHEMBL87717 | — | — | 1 | 8.60 |
| CHEMBL539544 | — | — | 1 | 8.33 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.30 |
| CHEMBL541842 | — | — | 1 | 8.17 |
| CHEMBL92673 | — | — | 1 | 8.15 |
| CHEMBL87943 | — | — | 1 | 8.11 |
| CHEMBL558817 | — | — | 1 | 7.95 |
| CHEMBL87026 | — | — | 1 | 7.88 |
| CHEMBL310734 | — | — | 1 | 7.75 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.70 |
| CHEMBL545727 | — | — | 1 | 7.58 |
| CHEMBL92145 | — | — | 1 | 7.39 |
| CHEMBL95112 | — | — | 1 | 7.37 |
| CHEMBL544089 | — | — | 1 | 7.34 |
| CHEMBL544319 | — | — | 1 | 7.24 |
| CHEMBL96781 | — | — | 1 | 7.14 |
| CHEMBL542428 | — | — | 1 | 6.97 |
| CHEMBL95098 | — | — | 1 | 6.91 |
| CHEMBL540822 | — | — | 1 | 6.84 |
| CHEMBL310153 | — | — | 1 | 6.29 |
| CHEMBL542181 | — | — | 1 | 6.05 |
| CHEMBL544318 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL544091 | — | Ki | = | 1.445 | nM | 8.84 |
| CHEMBL308480 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL554199 | — | Ki | = | 1.738 | nM | 8.76 |
| CHEMBL87717 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL539544 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL42 | CLOZAPINE | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL541842 | — | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL92673 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL87943 | — | Ki | = | 7.762 | nM | 8.11 |
| CHEMBL558817 | — | Ki | = | 11.22 | nM | 7.95 |
| CHEMBL87026 | — | Ki | = | 13.18 | nM | 7.88 |
| CHEMBL310734 | — | Ki | = | 17.78 | nM | 7.75 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL545727 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL92145 | — | Ki | = | 40.74 | nM | 7.39 |
| CHEMBL95112 | — | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL544089 | — | Ki | = | 45.71 | nM | 7.34 |
| CHEMBL544319 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL96781 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL542428 | — | Ki | = | 107.15 | nM | 6.97 |
| CHEMBL95098 | — | Ki | = | 123.03 | nM | 6.91 |
| CHEMBL540822 | — | Ki | = | 144.54 | nM | 6.84 |
| CHEMBL310153 | — | Ki | = | 512.86 | nM | 6.29 |
| CHEMBL542181 | — | Ki | = | 891.25 | nM | 6.05 |
| CHEMBL544318 | — | Ki | = | 1513.56 | nM | 5.82 |