Assay Detail
Binding
CHEMBL3388263
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Displacement of [3H]histamine from human recombinant histamine H4 receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The effect of pK(a) on pyrimidine/pyridine-derived histamine H4 ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.55 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3236553 | — | — | 1 | 9.00 |
| CHEMBL3354820 | — | — | 1 | 8.70 |
| CHEMBL1770969 | — | — | 1 | 8.51 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 8.30 |
| CHEMBL3354815 | — | — | 1 | 8.22 |
| CHEMBL1770990 | — | — | 1 | 8.22 |
| CHEMBL3354811 | — | — | 1 | 7.96 |
| CHEMBL3354812 | — | — | 1 | 7.80 |
| CHEMBL3354816 | — | — | 1 | 7.72 |
| CHEMBL3236568 | — | — | 1 | 7.68 |
| CHEMBL3354819 | — | — | 1 | 7.30 |
| CHEMBL3354808 | — | — | 1 | 7.04 |
| CHEMBL3354809 | — | — | 1 | 6.90 |
| CHEMBL3354813 | — | — | 1 | 6.50 |
| CHEMBL3354814 | — | — | 1 | 6.34 |
| CHEMBL3354807 | — | — | 1 | 6.34 |
| CHEMBL3354817 | — | — | 1 | 5.81 |
| CHEMBL3354821 | — | — | 1 | - |
| CHEMBL3236584 | — | — | 1 | - |
| CHEMBL3354810 | — | — | 1 | - |
| CHEMBL3354818 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3236553 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3354820 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1770969 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3354815 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL1770990 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3354811 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3354812 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3354816 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3236568 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL3354819 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL3354808 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL3354809 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL3354813 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL3354814 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL3354807 | — | Ki | = | 456.0 | nM | 6.34 |
| CHEMBL3354817 | — | Ki | = | 1547.0 | nM | 5.81 |
| CHEMBL3354821 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3236584 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3354810 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3354818 | — | Ki | > | 1000.0 | nM | - |