Assay Detail
Binding
CHEMBL693567
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Affinity against rat Histamine H3 receptor using [3H]N-alpha-methyl histamine
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.73 | 8.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL60716 | — | — | 1 | 8.88 |
| CHEMBL305135 | — | — | 1 | 8.60 |
| CHEMBL13795 | VUF-5297 | — | 1 | 8.37 |
| CHEMBL418470 | — | — | 1 | 8.32 |
| CHEMBL292558 | — | — | 1 | 8.00 |
| CHEMBL302231 | — | — | 1 | 7.65 |
| CHEMBL13559 | VUF-5296 | — | 1 | 7.38 |
| CHEMBL292924 | — | — | 1 | 7.19 |
| CHEMBL59389 | — | — | 1 | 7.04 |
| CHEMBL294061 | — | — | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL60716 | — | Ki | = | 1.31 | nM | 8.88 |
| CHEMBL305135 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL13795 | VUF-5297 | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL418470 | — | Ki | = | 4.78 | nM | 8.32 |
| CHEMBL292558 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL302231 | — | Ki | = | 22.6 | nM | 7.65 |
| CHEMBL13559 | VUF-5296 | Ki | = | 42.2 | nM | 7.38 |
| CHEMBL292924 | — | Ki | = | 64.7 | nM | 7.19 |
| CHEMBL59389 | — | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL294061 | — | Ki | = | 1380.0 | nM | 5.86 |