Assay Detail
Binding
CHEMBL673597
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In vitro binding affinity towards dopamine receptor D2 in rat striatal membranes by [3H]sulpiride displacement.
18
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 7.36 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.33 |
| CHEMBL284163 | — | — | 3 | 9.15 |
| CHEMBL285712 | — | — | 3 | 8.77 |
| CHEMBL291254 | — | — | 3 | 8.59 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 7.33 |
| CHEMBL38151 | — | — | 3 | 7.00 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.78 |
| CHEMBL284172 | — | — | 3 | 6.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL284163 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL285712 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL291254 | — | Ki | = | 2.59 | nM | 8.59 |
| CHEMBL284163 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL291254 | — | Ki | = | 2.77 | nM | 8.56 |
| CHEMBL285712 | — | Ki | = | 4.43 | nM | 8.35 |
| CHEMBL267777 | RITANSERIN | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL38151 | — | Ki | = | 99.3 | nM | 7.00 |
| CHEMBL285712 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL42 | CLOZAPINE | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL38151 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL284172 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL284172 | — | Ki | = | 308.0 | nM | 6.51 |
| CHEMBL291254 | — | Ki | = | 755.0 | nM | 6.12 |
| CHEMBL38151 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL284172 | — | Ki | = | 1840.0 | nM | 5.74 |
| CHEMBL284163 | — | Ki | = | 2380.0 | nM | 5.62 |