Assay Detail
Binding
CHEMBL4197754
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Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel indanone derivatives as MAO B/H3R dual-targeting ligands for treatment of Parkinson's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.34 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4209497 | — | — | 1 | 8.68 |
| CHEMBL4218833 | — | — | 1 | 8.66 |
| CHEMBL4212330 | — | — | 1 | 8.41 |
| CHEMBL4205653 | — | — | 1 | 8.19 |
| CHEMBL4214411 | — | — | 1 | 7.96 |
| CHEMBL2297871 | — | — | 1 | 7.96 |
| CHEMBL4217355 | — | — | 1 | 7.50 |
| CHEMBL4204965 | — | — | 1 | 7.48 |
| CHEMBL4216392 | — | — | 1 | 7.41 |
| CHEMBL4215163 | — | — | 1 | 6.80 |
| CHEMBL4204031 | — | — | 1 | 6.69 |
| CHEMBL4207429 | — | — | 1 | 6.52 |
| CHEMBL4208908 | — | — | 1 | 6.46 |
| CHEMBL4216240 | — | — | 1 | 6.16 |
| CHEMBL4212333 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4209497 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4218833 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL4212330 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4205653 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4214411 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2297871 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4217355 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4204965 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4216392 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL4215163 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL4204031 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL4207429 | — | Ki | = | 304.0 | nM | 6.52 |
| CHEMBL4208908 | — | Ki | = | 345.0 | nM | 6.46 |
| CHEMBL4216240 | — | Ki | = | 696.0 | nM | 6.16 |
| CHEMBL4212333 | — | Ki | = | 6118.0 | nM | 5.21 |