Assay Detail
Binding
CHEMBL4842101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-LSD from 5HT2C receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
14
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
2-Phenylcyclopropylmethylamine Derivatives as Dopamine D<sub>2</sub> Receptor Partial Agonists: Design, Synthesis, and Biological Evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.63 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 2 | 7.02 |
| CHEMBL4862890 | — | — | 2 | 6.91 |
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 2 | 6.70 |
| CHEMBL4863832 | — | — | 2 | 6.52 |
| CHEMBL4862770 | — | — | 2 | 6.43 |
| CHEMBL4875081 | — | — | 2 | 6.22 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | - |
| CHEMBL441618 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 95.4 | nM | 7.02 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL4862890 | — | Ki | = | 122.3 | nM | 6.91 |
| CHEMBL4862890 | — | Ki | = | 123.03 | nM | 6.91 |
| CHEMBL2028019 | CARIPRAZINE | Ki | = | 198.2 | nM | 6.70 |
| CHEMBL2028019 | CARIPRAZINE | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL4863832 | — | Ki | = | 304.6 | nM | 6.52 |
| CHEMBL4863832 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL4862770 | — | Ki | = | 373.0 | nM | 6.43 |
| CHEMBL4862770 | — | Ki | = | 371.54 | nM | 6.43 |
| CHEMBL4875081 | — | Ki | = | 604.0 | nM | 6.22 |
| CHEMBL4875081 | — | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL54 | HALOPERIDOL | Ki | - | — | - | |
| CHEMBL441618 | — | Ki | - | — | - |