Assay Detail
Binding
CHEMBL5362776
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells membrane incubated for 1 hr by microbeta liquid scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel arylpiperazine-based DA/5-HT modulators as potential antipsychotic agents - Design, synthesis, structural studies and pharmacological profiling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.76 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 9.64 |
| CHEMBL5431642 | — | — | 1 | 7.18 |
| CHEMBL5409227 | — | — | 1 | 6.89 |
| CHEMBL5398291 | — | — | 1 | 6.87 |
| CHEMBL5422196 | — | — | 1 | 6.84 |
| CHEMBL5432478 | — | — | 1 | 6.82 |
| CHEMBL5435580 | — | — | 1 | 6.77 |
| CHEMBL5404031 | — | — | 1 | 6.75 |
| CHEMBL5429491 | — | — | 1 | 6.74 |
| CHEMBL5411002 | — | — | 1 | 6.61 |
| CHEMBL5412886 | — | — | 1 | 6.50 |
| CHEMBL5415412 | — | — | 1 | 6.49 |
| CHEMBL5395668 | — | — | 1 | 6.40 |
| CHEMBL5418283 | — | — | 1 | 6.15 |
| CHEMBL5424052 | — | — | 1 | 5.92 |
| CHEMBL5439203 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL5431642 | — | Ki | = | 66.7 | nM | 7.18 |
| CHEMBL5409227 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL5398291 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL5422196 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL5432478 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL5435580 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL5404031 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL5429491 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL5411002 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL5412886 | — | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL5415412 | — | Ki | = | 321.0 | nM | 6.49 |
| CHEMBL5395668 | — | Ki | = | 401.0 | nM | 6.40 |
| CHEMBL5418283 | — | Ki | = | 706.0 | nM | 6.15 |
| CHEMBL5424052 | — | Ki | = | 1189.0 | nM | 5.92 |
| CHEMBL5439203 | — | Ki | = | 2917.0 | nM | 5.54 |