Assay Detail
Binding
CHEMBL1785144
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Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 8.00 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1783890 | — | — | 1 | 9.68 |
| CHEMBL351231 | — | — | 1 | 9.35 |
| CHEMBL129542 | JNJ-5207852 | — | 1 | 9.22 |
| CHEMBL1783910 | — | — | 1 | 9.15 |
| CHEMBL268229 | — | — | 1 | 9.10 |
| CHEMBL1783889 | — | — | 1 | 9.10 |
| CHEMBL1783895 | — | — | 1 | 9.05 |
| CHEMBL237087 | — | — | 1 | 9.00 |
| CHEMBL1783893 | — | — | 1 | 8.96 |
| CHEMBL1783891 | — | — | 1 | 8.96 |
| CHEMBL97170 | — | — | 1 | 8.92 |
| CHEMBL1783905 | — | — | 1 | 8.82 |
| CHEMBL194092 | — | — | 1 | 8.68 |
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | 8.57 |
| CHEMBL1783877 | — | — | 1 | 8.49 |
| CHEMBL1783897 | — | — | 1 | 8.47 |
| CHEMBL1783909 | — | — | 1 | 8.39 |
| CHEMBL1783915 | — | — | 1 | 8.36 |
| CHEMBL1783906 | — | — | 1 | 8.24 |
| CHEMBL1783896 | — | — | 1 | 8.16 |
| CHEMBL1783913 | — | — | 1 | 7.92 |
| CHEMBL1783894 | — | — | 1 | 7.82 |
| CHEMBL1783892 | — | — | 1 | 7.64 |
| CHEMBL1783914 | — | — | 1 | 7.58 |
| CHEMBL380697 | APLYSAMINE | — | 1 | 7.52 |
| CHEMBL1783916 | — | — | 1 | 7.50 |
| CHEMBL1783912 | — | — | 1 | 7.46 |
| CHEMBL1783898 | — | — | 1 | 7.43 |
| CHEMBL1783911 | — | — | 1 | 7.27 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1783890 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL351231 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL129542 | JNJ-5207852 | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1783910 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL268229 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL1783889 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL1783895 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL237087 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1783893 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1783891 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL97170 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1783905 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL194092 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL462605 | PITOLISANT | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1783877 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL1783897 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL1783909 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL1783915 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL1783906 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL1783896 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL1783913 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1783894 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1783892 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL1783914 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL380697 | APLYSAMINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1783916 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL1783912 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL1783898 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL1783911 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL1783907 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL1783908 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL1783901 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL1783917 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL1783904 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL1783899 | — | Ki | = | 356.0 | nM | 6.45 |
| CHEMBL1783902 | — | Ki | = | 458.0 | nM | 6.34 |
| CHEMBL1783900 | — | Ki | = | 679.0 | nM | 6.17 |
| CHEMBL1783903 | — | Ki | = | 692.0 | nM | 6.16 |