Assay Detail
Functional
CHEMBL698406
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Histamine H3 receptor affinity of compound was determined in rat cortical membranes using the H3 selective agonist ligand, [3H]N-alpha-methylhistamine
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Diastereoselective synthesis of trans-2-(1-triphenylmethyl-1H-imidazol-4-yl)cyclopropanecarboxylic acids: key intermediates for the preparation of potent and chiral histamine H3 receptor agents
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.76 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 9.74 |
| CHEMBL19010 | IODOPROXYFAN | — | 1 | 9.52 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.37 |
| CHEMBL14812 | GT-2016 | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL19010 | IODOPROXYFAN | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL14812 | GT-2016 | Ki | = | 40.0 | nM | 7.40 |