Assay Detail
Binding
CHEMBL2169535
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Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Shape-based reprofiling of FDA-approved drugs for the H₁ histamine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.04 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL908 | CHLORPROTHIXENE | 4.0 | 1 | 8.97 |
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 8.24 |
| CHEMBL900 | ORPHENADRINE | 4.0 | 1 | 6.79 |
| CHEMBL564 | PROMAZINE | 4.0 | 1 | 5.90 |
| CHEMBL86715 | PROCYCLIDINE | 4.0 | 1 | 5.17 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 4.95 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 4.90 |
| CHEMBL353846 | ADIPHENINE | 2.0 | 1 | 4.77 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL908 | CHLORPROTHIXENE | IC50 | = | 1.072 | nM | 8.97 |
| CHEMBL511 | PYRILAMINE | IC50 | = | 5.754 | nM | 8.24 |
| CHEMBL900 | ORPHENADRINE | IC50 | = | 162.18 | nM | 6.79 |
| CHEMBL564 | PROMAZINE | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL86715 | PROCYCLIDINE | IC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL122270 | LOBELINE | IC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL597 | PHENTOLAMINE | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL353846 | ADIPHENINE | IC50 | = | 16982.44 | nM | 4.77 |
| CHEMBL596 | FENTANYL | IC50 | = | 19952.62 | nM | 4.70 |