Assay Detail
Binding
CHEMBL694449
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Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.34 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL505 | CHLORPHENIRAMINE | 4.0 | 1 | 8.70 |
| CHEMBL58973 | — | — | 1 | 8.22 |
| CHEMBL292195 | — | — | 1 | 8.15 |
| CHEMBL446147 | — | — | 1 | 8.00 |
| CHEMBL60175 | — | — | 1 | 7.41 |
| CHEMBL61348 | — | — | 1 | 6.70 |
| CHEMBL59512 | — | — | 1 | 6.59 |
| CHEMBL293895 | — | — | 1 | 6.22 |
| CHEMBL58239 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL505 | CHLORPHENIRAMINE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL58973 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL292195 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL446147 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL60175 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL61348 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL59512 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL293895 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL58239 | — | Ki | = | 920.0 | nM | 6.04 |