Assay Detail
Binding
CHEMBL5554842
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin from human 5-HT2C 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 | HEK293T |
| 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 | 8.41 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5575767 | — | — | 1 | 9.41 |
| CHEMBL5575992 | — | — | 1 | 9.25 |
| CHEMBL5563839 | — | — | 1 | 8.72 |
| CHEMBL5569065 | — | — | 1 | 8.72 |
| CHEMBL5592950 | — | — | 1 | 8.27 |
| CHEMBL2111101 | PIMAVANSERIN | 4.0 | 1 | 8.24 |
| CHEMBL5570644 | — | — | 1 | 7.54 |
| CHEMBL5594392 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5575767 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL5575992 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL5563839 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL5569065 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL5592950 | — | Ki | = | 5.39 | nM | 8.27 |
| CHEMBL2111101 | PIMAVANSERIN | Ki | = | 5.72 | nM | 8.24 |
| CHEMBL5570644 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL5594392 | — | Ki | = | 73.0 | nM | 7.14 |