Assay Detail
Binding
CHEMBL3755807
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Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 5.28 | 7.37 |
| pKi | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL452847 | — | — | 1 | 7.37 |
| CHEMBL213912 | — | — | 1 | 6.99 |
| CHEMBL494093 | — | — | 1 | 6.73 |
| CHEMBL3752085 | — | — | 1 | 6.02 |
| CHEMBL3752270 | — | — | 1 | 5.80 |
| CHEMBL3752195 | — | — | 1 | 5.76 |
| CHEMBL3752225 | — | — | 1 | 5.37 |
| CHEMBL3753985 | — | — | 1 | 5.17 |
| CHEMBL3753705 | — | — | 1 | 5.11 |
| CHEMBL3753962 | — | — | 1 | 5.04 |
| CHEMBL3752383 | — | — | 1 | 5.01 |
| CHEMBL3753334 | — | — | 1 | 4.96 |
| CHEMBL3752972 | — | — | 1 | 4.86 |
| CHEMBL3752885 | — | — | 1 | 4.84 |
| CHEMBL3753621 | — | — | 1 | 4.82 |
| CHEMBL3753784 | — | — | 1 | 4.71 |
| CHEMBL3754176 | — | — | 1 | 4.70 |
| CHEMBL3753967 | — | — | 1 | 4.58 |
| CHEMBL3753849 | — | — | 1 | 4.50 |
| CHEMBL3752978 | — | — | 1 | 4.44 |
| CHEMBL3754008 | — | — | 1 | 4.14 |
| CHEMBL3752407 | — | — | 1 | - |
| CHEMBL3753031 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL452847 | — | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL213912 | — | Ki | = | 102.33 | nM | 6.99 |
| CHEMBL494093 | — | Ki | = | 186.21 | nM | 6.73 |
| CHEMBL3752085 | — | Ki | = | 954.99 | nM | 6.02 |
| CHEMBL3752270 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL3752195 | — | Ki | = | 1737.8 | nM | 5.76 |
| CHEMBL3752225 | — | Ki | = | 4265.8 | nM | 5.37 |
| CHEMBL3753985 | — | Ki | = | 6760.83 | nM | 5.17 |
| CHEMBL3753705 | — | Ki | = | 7762.47 | nM | 5.11 |
| CHEMBL3753962 | — | Ki | = | 9120.11 | nM | 5.04 |
| CHEMBL3752383 | — | Ki | = | 9772.37 | nM | 5.01 |
| CHEMBL3753334 | — | Ki | = | 10964.78 | nM | 4.96 |
| CHEMBL3752972 | — | Ki | = | 13803.84 | nM | 4.86 |
| CHEMBL3752885 | — | Ki | = | 14454.4 | nM | 4.84 |
| CHEMBL3753621 | — | Ki | = | 15135.61 | nM | 4.82 |
| CHEMBL3753784 | — | Ki | = | 19498.45 | nM | 4.71 |
| CHEMBL3754176 | — | Ki | = | 19952.62 | nM | 4.70 |
| CHEMBL3753967 | — | Ki | = | 26302.68 | nM | 4.58 |
| CHEMBL3753849 | — | Ki | = | 31622.78 | nM | 4.50 |
| CHEMBL3752978 | — | Ki | = | 36307.81 | nM | 4.44 |
| CHEMBL3754008 | — | Ki | = | 72443.6 | nM | 4.14 |
| CHEMBL3752407 | — | pKi | - | — | - | |
| CHEMBL3753031 | — | pKi | - | — | - |