Assay Detail
ADMET
CHEMBL4709845
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Displacement of [3H]pyrilamine from guinea pig cerebellum histamine H1 receptor measured after 60 mins by liquid scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Isoquinolinone derivatives as potent CNS multi-receptor D/5-HT/5-HT/5-HT/5-HT agents: Synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 6.91 | 7.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 7.49 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 7.31 |
| CHEMBL4743324 | — | — | 1 | 6.93 |
| CHEMBL4764679 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | Ki | = | 32.6 | nM | 7.49 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 48.9 | nM | 7.31 |
| CHEMBL4743324 | — | Ki | = | 117.9 | nM | 6.93 |
| CHEMBL4764679 | — | Ki | = | 1196.0 | nM | 5.92 |