Assay Detail
Functional
CHEMBL2328667
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Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of novel analogs of cabergoline: improving cardiovascular safety by removing 5-HT2B receptor agonism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kb | 3 | - | - |
| IC50 | 3 | 7.66 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2323581 | — | — | 2 | 7.89 |
| CHEMBL2323579 | — | — | 2 | 7.66 |
| CHEMBL2323580 | — | — | 2 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2323581 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2323579 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2323580 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2323581 | — | Kb | = | 3.3 | nM | - |
| CHEMBL2323580 | — | Kb | = | 9.3 | nM | - |
| CHEMBL2323579 | — | Kb | = | 5.6 | nM | - |