Assay Detail
Binding
CHEMBL4396178
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Displacement of [3H]OH-DPAT from human recombinant 5-HT1A receptor measured after 60 mins by scintillation counter method
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 | 7.54 | 9.74 |
| IC50 | 3 | 7.34 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56 | 8-OH-DPAT | — | 2 | 9.74 |
| CHEMBL4579120 | — | — | 2 | 6.51 |
| CHEMBL4562303 | — | — | 2 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56 | 8-OH-DPAT | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL56 | 8-OH-DPAT | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL4579120 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL4562303 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL4579120 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4562303 | — | IC50 | = | 680.0 | nM | 6.17 |