Assay Detail
Functional
CHEMBL4406077
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 15 mins followed by 5-HT addition and measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.18 | 6.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4593394 | — | — | 1 | 6.07 |
| CHEMBL4443039 | — | — | 1 | 5.00 |
| CHEMBL4475406 | — | — | 1 | 4.84 |
| CHEMBL4454380 | — | — | 1 | 4.79 |
| CHEMBL4439544 | — | — | 1 | - |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | - |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4593394 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4443039 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL4475406 | — | IC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL4454380 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL4439544 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL240773 | QUINPIROLE | IC50 | - | — | - | |
| CHEMBL59 | DOPAMINE | IC50 | - | — | - |