Assay Detail
Binding
CHEMBL5350658
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Displacement of [3H] mepyramine from human FLAG-tagged histamine H1 receptor stably expressed in HEK293T cells assessed as inhibition constant by competitive binding based radioligand depletion assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dual Piperidine-Based Histamine H<sub>3</sub> and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 5.65 | 6.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5433976 | — | — | 1 | 6.18 |
| CHEMBL5421122 | — | — | 1 | 5.12 |
| CHEMBL5413694 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5433976 | — | Ki | = | 653.0 | nM | 6.18 |
| CHEMBL5421122 | — | Ki | = | 7615.0 | nM | 5.12 |
| CHEMBL5413694 | — | Ki | > | 10000.0 | nM | - |