Assay Detail
Binding
CHEMBL3293222
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ketanserin from human 5HT2A receptor expressed in HEK293 cells by competitive binding assay
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Functionally selective dopamine D₂, D₃ receptor partial agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.58 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.40 |
| CHEMBL3287403 | — | — | 2 | 8.40 |
| CHEMBL3287404 | — | — | 1 | 8.10 |
| CHEMBL3287396 | — | — | 1 | 7.80 |
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 1 | 7.66 |
| CHEMBL3287395 | — | — | 1 | 7.66 |
| CHEMBL3287402 | — | — | 1 | 7.25 |
| CHEMBL3287406 | — | — | 1 | 7.09 |
| CHEMBL3287397 | — | — | 1 | 6.62 |
| CHEMBL3287405 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3287403 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3287403 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL3287404 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3287396 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2028019 | CARIPRAZINE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3287395 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3287402 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL3287406 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL3287397 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL3287405 | — | Ki | = | 490.0 | nM | 6.31 |