Assay Detail
Binding
CHEMBL840219
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Displacement of [3H]N-R-methylhistamine binding to SK-N-MC cell membranes expressing human H3 receptor
22
Total Activities
22
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 | Expert |
Publication
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.56 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | — | 1 | 9.30 |
| CHEMBL175782 | METHIMEPIP | — | 1 | 9.00 |
| CHEMBL356666 | — | — | 1 | 8.20 |
| CHEMBL179302 | — | — | 1 | 8.20 |
| CHEMBL179873 | — | — | 1 | 8.00 |
| CHEMBL176269 | — | — | 1 | 7.80 |
| CHEMBL176178 | — | — | 1 | 7.80 |
| CHEMBL150701 | — | — | 1 | 7.70 |
| CHEMBL177612 | — | — | 1 | 7.50 |
| CHEMBL369096 | — | — | 1 | 7.40 |
| CHEMBL176018 | — | — | 1 | 7.40 |
| CHEMBL175741 | — | — | 1 | 7.30 |
| CHEMBL175800 | — | — | 1 | 7.30 |
| CHEMBL369819 | — | — | 1 | 7.30 |
| CHEMBL176105 | — | — | 1 | 7.20 |
| CHEMBL368774 | — | — | 1 | 7.20 |
| CHEMBL176608 | — | — | 1 | 7.20 |
| CHEMBL179479 | — | — | 1 | 7.20 |
| CHEMBL175771 | — | — | 1 | 7.10 |
| CHEMBL180061 | — | — | 1 | 7.00 |
| CHEMBL369158 | — | — | 1 | 6.80 |
| CHEMBL179747 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL175782 | METHIMEPIP | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL356666 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL179302 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL179873 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL176269 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL176178 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL150701 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL177612 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL369096 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL176018 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL175741 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL175800 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL369819 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL176105 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL368774 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL176608 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL179479 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL175771 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL180061 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL369158 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL179747 | — | Ki | = | 398.11 | nM | 6.40 |