Assay Detail
Binding
CHEMBL2379701
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 5.30 | 5.55 |
| pKi | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2376803 | — | — | 1 | 5.55 |
| CHEMBL2376801 | — | — | 1 | 5.50 |
| CHEMBL2376800 | — | — | 1 | 4.85 |
| CHEMBL2376804 | — | — | 1 | - |
| CHEMBL1915540 | ADRIFORANT | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2376803 | — | Ki | = | 2818.38 | nM | 5.55 |
| CHEMBL2376801 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL2376800 | — | Ki | = | 14125.38 | nM | 4.85 |
| CHEMBL2376804 | — | pKi | - | — | - | |
| CHEMBL1915540 | ADRIFORANT | pKi | - | — | - |