Assay Detail
Binding
CHEMBL5554841
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin from human 5-HT2A receptor transfected in Jump-In GripTite HEK293 cell membrane measured after 3 hrs incubation by scintillation proximity assay (SPA)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dual 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> Receptor Inverse Agonist That Affords In Vivo Antipsychotic Efficacy with Minimal hERG Inhibition for the Treatment of Dementia-Related Psychosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 8.88 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5575992 | — | — | 1 | 9.24 |
| CHEMBL5575767 | — | — | 1 | 9.13 |
| CHEMBL2111101 | PIMAVANSERIN | 4.0 | 1 | 9.07 |
| CHEMBL5569065 | — | — | 1 | 9.05 |
| CHEMBL5592950 | — | — | 1 | 9.03 |
| CHEMBL5563839 | — | — | 1 | 9.01 |
| CHEMBL5594392 | — | — | 1 | 8.44 |
| CHEMBL5570644 | — | — | 1 | 8.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5575992 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL5575767 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL2111101 | PIMAVANSERIN | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL5569065 | — | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL5592950 | — | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL5563839 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL5594392 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL5570644 | — | Ki | = | 8.6 | nM | 8.07 |