Assay Detail
Functional
CHEMBL1785146
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Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
19
Total Activities
19
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| Kd | 16 | 8.94 | 9.84 |
| pKb | 2 | - | - |
| pA2 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | — | 1 | 9.84 |
| CHEMBL1783889 | — | — | 1 | 9.62 |
| CHEMBL1783910 | — | — | 1 | 9.46 |
| CHEMBL1783895 | — | — | 1 | 9.38 |
| CHEMBL194092 | — | — | 1 | 9.32 |
| CHEMBL1783905 | — | — | 1 | 9.31 |
| CHEMBL1783890 | — | — | 1 | 9.26 |
| CHEMBL1783891 | — | — | 1 | 9.25 |
| CHEMBL1783897 | — | — | 1 | 9.24 |
| CHEMBL237087 | — | — | 1 | 9.22 |
| CHEMBL1783893 | — | — | 1 | 9.09 |
| CHEMBL1783877 | — | — | 1 | 8.54 |
| CHEMBL1783909 | — | — | 1 | 8.31 |
| CHEMBL1783915 | — | — | 1 | 8.16 |
| CHEMBL351231 | — | — | 1 | 7.89 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 7.20 |
| CHEMBL380697 | APLYSAMINE | — | 1 | - |
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | - |
| CHEMBL97170 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | Kd | = | 0.1445 | nM | 9.84 |
| CHEMBL1783889 | — | Kd | = | 0.2399 | nM | 9.62 |
| CHEMBL1783910 | — | Kd | = | 0.3467 | nM | 9.46 |
| CHEMBL1783895 | — | Kd | = | 0.4169 | nM | 9.38 |
| CHEMBL194092 | — | Kd | = | 0.4786 | nM | 9.32 |
| CHEMBL1783905 | — | Kd | = | 0.4898 | nM | 9.31 |
| CHEMBL1783890 | — | Kd | = | 0.5495 | nM | 9.26 |
| CHEMBL1783891 | — | Kd | = | 0.5623 | nM | 9.25 |
| CHEMBL1783897 | — | Kd | = | 0.5754 | nM | 9.24 |
| CHEMBL237087 | — | Kd | = | 0.6026 | nM | 9.22 |
| CHEMBL1783893 | — | Kd | = | 0.8128 | nM | 9.09 |
| CHEMBL1783877 | — | Kd | = | 2.884 | nM | 8.54 |
| CHEMBL1783909 | — | Kd | = | 4.898 | nM | 8.31 |
| CHEMBL1783915 | — | Kd | = | 6.918 | nM | 8.16 |
| CHEMBL351231 | — | Kd | = | 12.88 | nM | 7.89 |
| CHEMBL260374 | THIOPERAMIDE | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL380697 | APLYSAMINE | pA2 | - | — | - | |
| CHEMBL462605 | PITOLISANT | pKb | = | 9.5 | — | - |
| CHEMBL97170 | — | pKb | = | 8.64 | — | - |