Assay Detail
Binding
CHEMBL4154392
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Displacement of [3H]Nalpha-methylhistamine from recombinant human H3 receptor expressed in HEK293 cells after 90 mins by liquid scintillation counting method
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 6.13 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4173079 | — | — | 1 | 8.08 |
| CHEMBL4173854 | — | — | 1 | 7.80 |
| CHEMBL4159018 | — | — | 1 | 7.66 |
| CHEMBL4165880 | — | — | 1 | 7.51 |
| CHEMBL4162433 | — | — | 1 | 7.42 |
| CHEMBL4160557 | — | — | 1 | 6.92 |
| CHEMBL4163949 | — | — | 1 | 6.32 |
| CHEMBL4170784 | — | — | 1 | 6.17 |
| CHEMBL4166945 | — | — | 1 | 6.05 |
| CHEMBL4162840 | — | — | 1 | 5.64 |
| CHEMBL4163913 | — | — | 1 | 5.53 |
| CHEMBL4170350 | — | — | 1 | 5.47 |
| CHEMBL4173801 | — | — | 1 | 5.44 |
| CHEMBL4166262 | — | — | 1 | 5.42 |
| CHEMBL4165061 | — | — | 1 | 5.28 |
| CHEMBL4175250 | — | — | 1 | 5.27 |
| CHEMBL4159046 | — | — | 1 | 5.26 |
| CHEMBL4167380 | — | — | 1 | 5.21 |
| CHEMBL4163474 | — | — | 1 | 5.09 |
| CHEMBL4174172 | — | — | 1 | 5.06 |
| CHEMBL4159479 | — | — | 1 | - |
| CHEMBL4171151 | — | — | 1 | - |
| CHEMBL4174596 | — | — | 1 | - |
| CHEMBL4175362 | — | — | 1 | - |
| CHEMBL4174564 | — | — | 1 | - |
| CHEMBL4161040 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4173079 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL4173854 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4159018 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4165880 | — | Ki | = | 30.6 | nM | 7.51 |
| CHEMBL4162433 | — | Ki | = | 37.8 | nM | 7.42 |
| CHEMBL4160557 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4163949 | — | Ki | = | 482.0 | nM | 6.32 |
| CHEMBL4170784 | — | Ki | = | 683.0 | nM | 6.17 |
| CHEMBL4166945 | — | Ki | = | 883.0 | nM | 6.05 |
| CHEMBL4162840 | — | Ki | = | 2264.0 | nM | 5.64 |
| CHEMBL4163913 | — | Ki | = | 2957.0 | nM | 5.53 |
| CHEMBL4170350 | — | Ki | = | 3420.0 | nM | 5.47 |
| CHEMBL4173801 | — | Ki | = | 3654.0 | nM | 5.44 |
| CHEMBL4166262 | — | Ki | = | 3827.0 | nM | 5.42 |
| CHEMBL4165061 | — | Ki | = | 5196.0 | nM | 5.28 |
| CHEMBL4175250 | — | Ki | = | 5405.0 | nM | 5.27 |
| CHEMBL4159046 | — | Ki | = | 5477.0 | nM | 5.26 |
| CHEMBL4167380 | — | Ki | = | 6212.0 | nM | 5.21 |
| CHEMBL4163474 | — | Ki | = | 8156.0 | nM | 5.09 |
| CHEMBL4174172 | — | Ki | = | 8740.0 | nM | 5.06 |
| CHEMBL4159479 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4171151 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4174596 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4175362 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4174564 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4161040 | — | Ki | > | 10000.0 | nM | - |