Assay Detail
Functional
CHEMBL4356375
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
24
Total Activities
24
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 | 24 | 8.06 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4441731 | — | — | 1 | 9.50 |
| CHEMBL4535316 | — | — | 1 | 9.20 |
| CHEMBL4560428 | — | — | 1 | 9.10 |
| CHEMBL4466700 | — | — | 1 | 8.90 |
| CHEMBL4516714 | — | — | 1 | 8.70 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 8.60 |
| CHEMBL4476584 | — | — | 1 | 8.50 |
| CHEMBL4455352 | — | — | 1 | 8.40 |
| CHEMBL4579823 | — | — | 1 | 8.30 |
| CHEMBL4459469 | — | — | 1 | 8.30 |
| CHEMBL4539015 | — | — | 1 | 8.10 |
| CHEMBL4555457 | — | — | 1 | 8.10 |
| CHEMBL4468740 | — | — | 1 | 8.00 |
| CHEMBL4469111 | — | — | 1 | 7.90 |
| CHEMBL4470781 | — | — | 1 | 7.90 |
| CHEMBL4468827 | — | — | 1 | 7.80 |
| CHEMBL4535363 | — | — | 1 | 7.60 |
| CHEMBL4570258 | — | — | 1 | 7.50 |
| CHEMBL4459723 | — | — | 1 | 7.50 |
| CHEMBL4579385 | — | — | 1 | 7.40 |
| CHEMBL4461302 | — | — | 1 | 7.20 |
| CHEMBL4452204 | — | — | 1 | 7.10 |
| CHEMBL4519616 | — | — | 1 | 7.00 |
| CHEMBL4439165 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4441731 | — | EC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL4535316 | — | EC50 | = | 0.631 | nM | 9.20 |
| CHEMBL4560428 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4466700 | — | EC50 | = | 1.259 | nM | 8.90 |
| CHEMBL4516714 | — | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL90 | HISTAMINE | EC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4476584 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4455352 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4579823 | — | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL4459469 | — | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL4539015 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4555457 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4468740 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4469111 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4470781 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4468827 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4535363 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4570258 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4459723 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4579385 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4461302 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4452204 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4519616 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4439165 | — | EC50 | = | 158.49 | nM | 6.80 |