Assay Detail
Binding
CHEMBL895632
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Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.47 | 8.20 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.20 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 8.10 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.10 |
| CHEMBL708 | ZIPRASIDONE | 4.0 | 1 | 7.80 |
| CHEMBL131495 | — | — | 1 | 7.50 |
| CHEMBL716 | QUETIAPINE | 4.0 | 1 | 7.40 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 7.30 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 7.00 |
| CHEMBL196514 | — | — | 1 | 6.90 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.40 |
| CHEMBL221692 | ADOPRAZINE | 2.0 | 1 | - |
| CHEMBL243712 | AMISULPRIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL85 | RISPERIDONE | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL42 | CLOZAPINE | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL708 | ZIPRASIDONE | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL131495 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL716 | QUETIAPINE | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL196514 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL221692 | ADOPRAZINE | Activity | - | — | - | |
| CHEMBL243712 | AMISULPRIDE | Activity | - | — | - |