Assay Detail
Binding
CHEMBL954166
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Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.37 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 9.82 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.40 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.06 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.00 |
| CHEMBL496739 | — | — | 1 | 7.82 |
| CHEMBL461236 | — | — | 1 | 7.63 |
| CHEMBL462508 | — | — | 1 | 7.39 |
| CHEMBL495572 | — | — | 1 | 7.24 |
| CHEMBL496531 | — | — | 1 | 7.08 |
| CHEMBL522044 | — | — | 1 | 6.91 |
| CHEMBL497988 | — | — | 1 | 6.90 |
| CHEMBL517730 | — | — | 1 | 6.83 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.79 |
| CHEMBL461023 | — | — | 1 | 6.79 |
| CHEMBL495573 | — | — | 1 | 6.70 |
| CHEMBL497574 | — | — | 1 | 6.52 |
| CHEMBL497573 | — | — | 1 | 6.41 |
| CHEMBL497604 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL715 | OLANZAPINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL42 | CLOZAPINE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL496739 | — | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL461236 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL462508 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL495572 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL496531 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL522044 | — | Ki | = | 122.76 | nM | 6.91 |
| CHEMBL497988 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL517730 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL461023 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL495573 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL497574 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL497573 | — | Ki | = | 389.0 | nM | 6.41 |
| CHEMBL497604 | — | Ki | - | — | - |