Assay Detail
Binding
CHEMBL694088
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Ability to displace [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortex
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.61 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45369 | — | — | 1 | 9.74 |
| CHEMBL1160082 | — | — | 1 | 9.40 |
| CHEMBL73053 | — | — | 1 | 8.15 |
| CHEMBL16496 | — | — | 1 | 7.92 |
| CHEMBL45370 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45369 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL1160082 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL73053 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL16496 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL45370 | — | Ki | = | 14.0 | nM | 7.85 |