Assay Detail
Binding
CHEMBL4356374
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NAMH from human H3R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 24 | 7.36 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4441731 | — | — | 1 | 8.50 |
| CHEMBL4466700 | — | — | 1 | 8.20 |
| CHEMBL4535316 | — | — | 1 | 8.00 |
| CHEMBL4516714 | — | — | 1 | 7.90 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.90 |
| CHEMBL4560428 | — | — | 1 | 7.80 |
| CHEMBL4459469 | — | — | 1 | 7.80 |
| CHEMBL4468740 | — | — | 1 | 7.50 |
| CHEMBL4539015 | — | — | 1 | 7.40 |
| CHEMBL4579823 | — | — | 1 | 7.40 |
| CHEMBL4476584 | — | — | 1 | 7.40 |
| CHEMBL4468827 | — | — | 1 | 7.30 |
| CHEMBL4455352 | — | — | 1 | 7.30 |
| CHEMBL4535363 | — | — | 1 | 7.30 |
| CHEMBL4555457 | — | — | 1 | 7.20 |
| CHEMBL4459723 | — | — | 1 | 7.10 |
| CHEMBL4469111 | — | — | 1 | 7.10 |
| CHEMBL4470781 | — | — | 1 | 7.00 |
| CHEMBL4439165 | — | — | 1 | 7.00 |
| CHEMBL4519616 | — | — | 1 | 6.90 |
| CHEMBL4570258 | — | — | 1 | 6.90 |
| CHEMBL4452204 | — | — | 1 | 6.70 |
| CHEMBL4461302 | — | — | 1 | 6.60 |
| CHEMBL4579385 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4441731 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL4466700 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL4535316 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4516714 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL90 | HISTAMINE | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL4560428 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL4459469 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL4468740 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL4539015 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL4579823 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL4476584 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL4468827 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL4455352 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL4535363 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL4555457 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL4459723 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL4469111 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL4470781 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4439165 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4519616 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL4570258 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL4452204 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL4461302 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL4579385 | — | Ki | = | 316.23 | nM | 6.50 |