Assay Detail
Binding
CHEMBL698090
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In vitro binding affinity was measured against Histamine H3 receptor on rat cerebral cortex.
3
Total Activities
3
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
Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)- and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.19 | 8.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13795 | VUF-5297 | — | 1 | 8.76 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 8.20 |
| CHEMBL13559 | VUF-5296 | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13795 | VUF-5297 | Ki | = | 1.738 | nM | 8.76 |
| CHEMBL90 | HISTAMINE | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL13559 | VUF-5296 | Ki | = | 25.12 | nM | 7.60 |