Assay Detail
Binding
CHEMBL617668
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In vitro binding affinity towards 5-hydroxytryptamine 2 receptor in rat striatal membranes by [3H]ketanserin displacement.
18
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serotonin 2 (5-HT2) receptor (CHEMBL2093870) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.24 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 9.21 |
| CHEMBL38151 | — | — | 3 | 9.10 |
| CHEMBL291254 | — | — | 3 | 8.73 |
| CHEMBL285712 | — | — | 3 | 8.67 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.43 |
| CHEMBL284172 | — | — | 3 | 8.37 |
| CHEMBL284163 | — | — | 3 | 8.21 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267777 | RITANSERIN | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL38151 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL291254 | — | Ki | = | 1.87 | nM | 8.73 |
| CHEMBL38151 | — | Ki | = | 1.96 | nM | 8.71 |
| CHEMBL285712 | — | Ki | = | 2.13 | nM | 8.67 |
| CHEMBL38151 | — | Ki | = | 2.56 | nM | 8.59 |
| CHEMBL285712 | — | Ki | = | 2.81 | nM | 8.55 |
| CHEMBL291254 | — | Ki | = | 2.98 | nM | 8.53 |
| CHEMBL42 | CLOZAPINE | Ki | = | 3.68 | nM | 8.43 |
| CHEMBL284172 | — | Ki | = | 4.25 | nM | 8.37 |
| CHEMBL284163 | — | Ki | = | 6.11 | nM | 8.21 |
| CHEMBL284172 | — | Ki | = | 6.62 | nM | 8.18 |
| CHEMBL284163 | — | Ki | = | 7.98 | nM | 8.10 |
| CHEMBL284172 | — | Ki | = | 8.54 | nM | 8.07 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 26.5 | nM | 7.58 |
| CHEMBL285712 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL291254 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL284163 | — | Ki | = | 170.0 | nM | 6.77 |