Assay Detail
Binding
CHEMBL4396180
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Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Multi-targeting protein-protein interaction inhibitors: Evolution of macrocyclic ligands with embedded carbohydrates (MECs) to improve selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 6.57 | 8.55 |
| IC50 | 3 | 6.30 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12314 | MESULERGINE | 2.0 | 2 | 8.55 |
| CHEMBL4579120 | — | — | 2 | 6.06 |
| CHEMBL4562303 | — | — | 2 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12314 | MESULERGINE | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL12314 | MESULERGINE | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4579120 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL4579120 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4562303 | — | Ki | = | 8200.0 | nM | 5.09 |
| CHEMBL4562303 | — | IC50 | = | 15000.0 | nM | 4.82 |