Assay Detail
ADMET
CHEMBL2328668
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Agonist activity at human 5-HT2B receptor transfected in CHO cell assessed as IP1 production incubated for 30 mins measured by HTRF detection method
9
Total Activities
6
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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 |
|---|---|---|---|
| Emax | 4 | - | - |
| EC50 | 3 | 7.86 | 7.89 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2323578 | — | — | 2 | 7.89 |
| CHEMBL1201087 | CABERGOLINE | 4.0 | 2 | 7.89 |
| CHEMBL14022 | — | — | 2 | 7.80 |
| CHEMBL2323581 | — | — | 1 | - |
| CHEMBL2323580 | — | — | 1 | - |
| CHEMBL2323579 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201087 | CABERGOLINE | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2323578 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL14022 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL14022 | — | Emax | = | 38.0 | % | - |
| CHEMBL2323578 | — | Emax | = | 106.0 | % | - |
| CHEMBL1201087 | CABERGOLINE | Emax | = | 103.0 | % | - |
| CHEMBL2323581 | — | Activity | - | — | - | |
| CHEMBL2323580 | — | Emax | < | 12.0 | % | - |
| CHEMBL2323579 | — | Activity | - | — | - |