Assay Detail
Functional
CHEMBL2379696
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| pKb | 5 | - | - |
| IC50 | 5 | 7.06 | 7.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1915540 | ADRIFORANT | 2.0 | 2 | 7.27 |
| CHEMBL2376804 | — | — | 2 | 7.15 |
| CHEMBL2376803 | — | — | 2 | 7.01 |
| CHEMBL2376800 | — | — | 2 | 6.95 |
| CHEMBL2376801 | — | — | 2 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1915540 | ADRIFORANT | IC50 | = | 53.7 | nM | 7.27 |
| CHEMBL2376804 | — | IC50 | = | 70.79 | nM | 7.15 |
| CHEMBL2376803 | — | IC50 | = | 97.72 | nM | 7.01 |
| CHEMBL2376800 | — | IC50 | = | 112.2 | nM | 6.95 |
| CHEMBL2376801 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL2376804 | — | pKb | = | 8.33 | — | - |
| CHEMBL2376803 | — | pKb | = | 8.2 | — | - |
| CHEMBL2376801 | — | pKb | = | 8.08 | — | - |
| CHEMBL2376800 | — | pKb | = | 8.14 | — | - |
| CHEMBL1915540 | ADRIFORANT | pKb | = | 8.46 | — | - |