Assay Detail
Binding
CHEMBL695765
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Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| EC50 | 11 | 7.17 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19439 | IMETIT | — | 1 | 8.72 |
| CHEMBL60716 | — | — | 1 | 8.00 |
| CHEMBL13795 | VUF-5297 | — | 1 | 7.38 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.11 |
| CHEMBL305135 | — | — | 1 | 7.02 |
| CHEMBL13559 | VUF-5296 | — | 1 | 6.14 |
| CHEMBL418470 | — | — | 1 | 5.85 |
| CHEMBL294061 | — | — | 1 | - |
| CHEMBL302231 | — | — | 1 | - |
| CHEMBL292924 | — | — | 1 | - |
| CHEMBL292558 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19439 | IMETIT | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL60716 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL13795 | VUF-5297 | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL90 | HISTAMINE | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL305135 | — | EC50 | = | 96.0 | nM | 7.02 |
| CHEMBL13559 | VUF-5296 | EC50 | = | 724.0 | nM | 6.14 |
| CHEMBL418470 | — | EC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL294061 | — | EC50 | > | 0.0001 | nM | - |
| CHEMBL302231 | — | EC50 | > | 0.0001 | nM | - |
| CHEMBL292924 | — | EC50 | > | 0.0001 | nM | - |
| CHEMBL292558 | — | EC50 | > | 0.0001 | nM | - |