Assay Detail
Binding
CHEMBL981878
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Displacement of [3H]N-alpha-methylhistamine from rat recombinant histamine H3 receptor expressed in HEK293 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.53 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL484946 | — | — | 1 | 8.74 |
| CHEMBL485543 | — | — | 1 | 8.64 |
| CHEMBL483400 | — | — | 1 | 8.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL484946 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL485543 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL483400 | — | Ki | = | 6.0 | nM | 8.22 |