Assay Detail
Functional
CHEMBL900877
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Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
14
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK239 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 8.93 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237394 | — | — | 2 | 9.23 |
| CHEMBL237191 | — | — | 2 | 9.11 |
| CHEMBL392573 | — | — | 2 | 8.95 |
| CHEMBL351231 | — | — | 2 | 8.89 |
| CHEMBL393581 | — | — | 2 | 8.85 |
| CHEMBL263101 | — | — | 2 | 8.80 |
| CHEMBL442242 | — | — | 2 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237394 | — | EC50 | = | 0.5888 | nM | 9.23 |
| CHEMBL237394 | — | EC50 | = | 0.59 | nM | 9.23 |
| CHEMBL237191 | — | EC50 | = | 0.7762 | nM | 9.11 |
| CHEMBL237191 | — | EC50 | = | 0.78 | nM | 9.11 |
| CHEMBL392573 | — | EC50 | = | 1.122 | nM | 8.95 |
| CHEMBL392573 | — | EC50 | = | 1.12 | nM | 8.95 |
| CHEMBL351231 | — | EC50 | = | 1.288 | nM | 8.89 |
| CHEMBL351231 | — | EC50 | = | 1.29 | nM | 8.89 |
| CHEMBL393581 | — | EC50 | = | 1.413 | nM | 8.85 |
| CHEMBL393581 | — | EC50 | = | 1.41 | nM | 8.85 |
| CHEMBL263101 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL263101 | — | EC50 | = | 1.58 | nM | 8.80 |
| CHEMBL442242 | — | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL442242 | — | EC50 | = | 2.0 | nM | 8.70 |