Assay Detail
Binding
CHEMBL2379706
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Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
23
Total Activities
23
Compounds Tested
1
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 | 23 | 7.87 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2376790 | — | — | 1 | 8.47 |
| CHEMBL2376804 | — | — | 1 | 8.28 |
| CHEMBL2376803 | — | — | 1 | 8.19 |
| CHEMBL2376794 | — | — | 1 | 8.15 |
| CHEMBL2376801 | — | — | 1 | 8.04 |
| CHEMBL2376799 | — | — | 1 | 8.03 |
| CHEMBL2376806 | — | — | 1 | 7.99 |
| CHEMBL1915540 | ADRIFORANT | 2.0 | 1 | 7.99 |
| CHEMBL2376800 | — | — | 1 | 7.97 |
| CHEMBL2376796 | — | — | 1 | 7.95 |
| CHEMBL2376793 | — | — | 1 | 7.94 |
| CHEMBL2376789 | — | — | 1 | 7.91 |
| CHEMBL2376807 | — | — | 1 | 7.91 |
| CHEMBL2376795 | — | — | 1 | 7.83 |
| CHEMBL1935574 | — | — | 1 | 7.82 |
| CHEMBL2376792 | — | — | 1 | 7.82 |
| CHEMBL2376797 | — | — | 1 | 7.77 |
| CHEMBL2376798 | — | — | 1 | 7.66 |
| CHEMBL2376805 | — | — | 1 | 7.60 |
| CHEMBL2376788 | — | — | 1 | 7.51 |
| CHEMBL2376791 | — | — | 1 | 7.45 |
| CHEMBL281590 | — | — | 1 | 7.35 |
| CHEMBL2376802 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2376790 | — | Ki | = | 3.388 | nM | 8.47 |
| CHEMBL2376804 | — | Ki | = | 5.248 | nM | 8.28 |
| CHEMBL2376803 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL2376794 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL2376801 | — | Ki | = | 9.12 | nM | 8.04 |
| CHEMBL2376799 | — | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL2376806 | — | Ki | = | 10.23 | nM | 7.99 |
| CHEMBL1915540 | ADRIFORANT | Ki | = | 10.23 | nM | 7.99 |
| CHEMBL2376800 | — | Ki | = | 10.72 | nM | 7.97 |
| CHEMBL2376796 | — | Ki | = | 11.22 | nM | 7.95 |
| CHEMBL2376793 | — | Ki | = | 11.48 | nM | 7.94 |
| CHEMBL2376789 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL2376807 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL2376795 | — | Ki | = | 14.79 | nM | 7.83 |
| CHEMBL1935574 | — | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL2376792 | — | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL2376797 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL2376798 | — | Ki | = | 21.88 | nM | 7.66 |
| CHEMBL2376805 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL2376788 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL2376791 | — | Ki | = | 35.48 | nM | 7.45 |
| CHEMBL281590 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL2376802 | — | Ki | = | 53.7 | nM | 7.27 |