Assay Detail
Binding
CHEMBL934603
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Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 52 | 6.22 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260549 | — | — | 1 | 8.25 |
| CHEMBL262859 | — | — | 1 | 7.93 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.92 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 7.80 |
| CHEMBL213912 | — | — | 1 | 7.60 |
| CHEMBL260444 | — | — | 1 | 7.58 |
| CHEMBL261551 | — | — | 1 | 7.40 |
| CHEMBL261224 | — | — | 1 | 7.24 |
| CHEMBL414183 | — | — | 1 | 7.21 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 7.20 |
| CHEMBL261519 | — | — | 1 | 7.20 |
| CHEMBL1743969 | — | — | 1 | 7.04 |
| CHEMBL259745 | — | — | 1 | 6.70 |
| CHEMBL259839 | — | — | 1 | 6.64 |
| CHEMBL261010 | — | — | 1 | 6.64 |
| CHEMBL410925 | — | — | 1 | 6.57 |
| CHEMBL402470 | — | — | 1 | 6.53 |
| CHEMBL261363 | — | — | 1 | 6.49 |
| CHEMBL405044 | — | — | 1 | 6.47 |
| CHEMBL260388 | — | — | 1 | 6.44 |
| CHEMBL259957 | — | — | 1 | 6.33 |
| CHEMBL260458 | — | — | 1 | 6.32 |
| CHEMBL261223 | — | — | 1 | 6.24 |
| CHEMBL260565 | — | — | 1 | 6.23 |
| CHEMBL428606 | — | — | 1 | 6.15 |
| CHEMBL123137 | — | — | 1 | 6.05 |
| CHEMBL406327 | — | — | 1 | 6.01 |
| CHEMBL261517 | — | — | 1 | 5.93 |
| CHEMBL260274 | — | — | 1 | 5.89 |
| CHEMBL260470 | — | — | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260549 | — | Ki | = | 5.623 | nM | 8.25 |
| CHEMBL262859 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL90 | HISTAMINE | Ki | = | 12.02 | nM | 7.92 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL213912 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL260444 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL261551 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL261224 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL414183 | — | Ki | = | 61.66 | nM | 7.21 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL261519 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL1743969 | — | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL259745 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL261010 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL259839 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL410925 | — | Ki | = | 269.15 | nM | 6.57 |
| CHEMBL402470 | — | Ki | = | 295.12 | nM | 6.53 |
| CHEMBL261363 | — | Ki | = | 323.59 | nM | 6.49 |
| CHEMBL405044 | — | Ki | = | 338.84 | nM | 6.47 |
| CHEMBL260388 | — | Ki | = | 363.08 | nM | 6.44 |
| CHEMBL259957 | — | Ki | = | 467.74 | nM | 6.33 |
| CHEMBL260458 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL261223 | — | Ki | = | 575.44 | nM | 6.24 |
| CHEMBL260565 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL428606 | — | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL123137 | — | Ki | = | 891.25 | nM | 6.05 |
| CHEMBL406327 | — | Ki | = | 977.24 | nM | 6.01 |
| CHEMBL261517 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL260274 | — | Ki | = | 1288.25 | nM | 5.89 |
| CHEMBL260470 | — | Ki | = | 1380.38 | nM | 5.86 |
| CHEMBL406345 | — | Ki | = | 1479.11 | nM | 5.83 |
| CHEMBL429691 | — | Ki | = | 1548.82 | nM | 5.81 |
| CHEMBL261222 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL259536 | — | Ki | = | 1698.24 | nM | 5.77 |
| CHEMBL405416 | — | Ki | = | 2187.76 | nM | 5.66 |
| CHEMBL260456 | — | Ki | = | 2290.87 | nM | 5.64 |
| CHEMBL261225 | — | Ki | = | 2344.23 | nM | 5.63 |
| CHEMBL260851 | — | Ki | = | 2344.23 | nM | 5.63 |
| CHEMBL406558 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL260850 | — | Ki | = | 2691.53 | nM | 5.57 |
| CHEMBL259955 | — | Ki | = | 2951.21 | nM | 5.53 |
| CHEMBL406380 | — | Ki | = | 2951.21 | nM | 5.53 |
| CHEMBL406379 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL428964 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL259956 | — | Ki | = | 4365.16 | nM | 5.36 |
| CHEMBL406123 | — | Ki | = | 5754.4 | nM | 5.24 |
| CHEMBL288591 | — | Ki | = | 6918.31 | nM | 5.16 |
| CHEMBL260371 | — | Ki | = | 7413.1 | nM | 5.13 |
| CHEMBL443764 | — | Ki | = | 7585.78 | nM | 5.12 |
| CHEMBL260372 | — | Ki | = | 10232.93 | nM | 4.99 |