Assay Detail
Binding
CHEMBL2379705
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Displacement of [3H]histamine from human histamine H3 receptor expressed in HEK cells
21
Total Activities
21
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 | 21 | 6.30 | 6.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2376807 | — | — | 1 | 6.84 |
| CHEMBL2376803 | — | — | 1 | 6.82 |
| CHEMBL2376793 | — | — | 1 | 6.81 |
| CHEMBL2376790 | — | — | 1 | 6.80 |
| CHEMBL2376798 | — | — | 1 | 6.75 |
| CHEMBL1915540 | ADRIFORANT | 2.0 | 1 | 6.73 |
| CHEMBL2376799 | — | — | 1 | 6.67 |
| CHEMBL2376795 | — | — | 1 | 6.66 |
| CHEMBL2376789 | — | — | 1 | 6.48 |
| CHEMBL2376792 | — | — | 1 | 6.31 |
| CHEMBL2376797 | — | — | 1 | 6.22 |
| CHEMBL2376796 | — | — | 1 | 6.21 |
| CHEMBL2376804 | — | — | 1 | 6.20 |
| CHEMBL2376794 | — | — | 1 | 6.16 |
| CHEMBL2376800 | — | — | 1 | 6.11 |
| CHEMBL2376805 | — | — | 1 | 6.08 |
| CHEMBL2376791 | — | — | 1 | 6.07 |
| CHEMBL2376806 | — | — | 1 | 6.00 |
| CHEMBL2376801 | — | — | 1 | 5.82 |
| CHEMBL1935574 | — | — | 1 | 5.47 |
| CHEMBL2376802 | — | — | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2376807 | — | Ki | = | 144.54 | nM | 6.84 |
| CHEMBL2376803 | — | Ki | = | 151.36 | nM | 6.82 |
| CHEMBL2376793 | — | Ki | = | 154.88 | nM | 6.81 |
| CHEMBL2376790 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL2376798 | — | Ki | = | 177.83 | nM | 6.75 |
| CHEMBL1915540 | ADRIFORANT | Ki | = | 186.21 | nM | 6.73 |
| CHEMBL2376799 | — | Ki | = | 213.8 | nM | 6.67 |
| CHEMBL2376795 | — | Ki | = | 218.78 | nM | 6.66 |
| CHEMBL2376789 | — | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL2376792 | — | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL2376797 | — | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL2376796 | — | Ki | = | 616.6 | nM | 6.21 |
| CHEMBL2376804 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL2376794 | — | Ki | = | 691.83 | nM | 6.16 |
| CHEMBL2376800 | — | Ki | = | 776.25 | nM | 6.11 |
| CHEMBL2376805 | — | Ki | = | 831.76 | nM | 6.08 |
| CHEMBL2376791 | — | Ki | = | 851.14 | nM | 6.07 |
| CHEMBL2376806 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL2376801 | — | Ki | = | 1513.56 | nM | 5.82 |
| CHEMBL1935574 | — | Ki | = | 3388.44 | nM | 5.47 |
| CHEMBL2376802 | — | Ki | = | 9549.93 | nM | 5.02 |