Assay Detail
Binding
CHEMBL692990
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Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.84 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL564226 | (S)-(+)-DIMETHINDENE | — | 1 | 9.36 |
| CHEMBL22108 | DIMETHINDENE | 3.0 | 1 | 9.16 |
| CHEMBL167223 | — | — | 1 | 9.09 |
| CHEMBL172233 | — | — | 1 | 8.14 |
| CHEMBL434684 | — | — | 1 | 7.54 |
| CHEMBL1493369 | — | — | 1 | 7.16 |
| CHEMBL352375 | — | — | 2 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL564226 | (S)-(+)-DIMETHINDENE | Ki | = | 0.4365 | nM | 9.36 |
| CHEMBL22108 | DIMETHINDENE | Ki | = | 0.6918 | nM | 9.16 |
| CHEMBL167223 | — | Ki | = | 0.8128 | nM | 9.09 |
| CHEMBL172233 | — | Ki | = | 7.244 | nM | 8.14 |
| CHEMBL434684 | — | Ki | = | 28.84 | nM | 7.54 |
| CHEMBL1493369 | — | Ki | = | 69.18 | nM | 7.16 |
| CHEMBL352375 | — | Ki | = | 218.78 | nM | 6.66 |
| CHEMBL352375 | — | Ki | = | 2454.71 | nM | 5.61 |