Assay Detail
Functional
CHEMBL4356378
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H3 Receptor Agonists with in Vivo Central Nervous System Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 7.80 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4441731 | — | — | 1 | 8.40 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4441731 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL90 | HISTAMINE | EC50 | = | 63.1 | nM | 7.20 |