Assay Detail
Binding
CHEMBL694918
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Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 8.58 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 1 | 9.27 |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 9.07 |
| CHEMBL1106 | EPINASTINE | 4.0 | 1 | 8.85 |
| CHEMBL855 | TRIPROLIDINE | 4.0 | 1 | 8.78 |
| CHEMBL278398 | PHENINDAMINE | 2.0 | 1 | 8.20 |
| CHEMBL73451 | MEQUITAZINE | 2.0 | 1 | 8.00 |
| CHEMBL609131 | — | — | 1 | 7.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 0.537 | nM | 9.27 |
| CHEMBL6437 | MIANSERIN | Ki | = | 0.8511 | nM | 9.07 |
| CHEMBL1106 | EPINASTINE | Ki | = | 1.413 | nM | 8.85 |
| CHEMBL855 | TRIPROLIDINE | Ki | = | 1.66 | nM | 8.78 |
| CHEMBL278398 | PHENINDAMINE | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL73451 | MEQUITAZINE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL609131 | — | Ki | = | 12.3 | nM | 7.91 |