Assay Detail
Functional
CHEMBL900876
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as inhibition of RAMH-stimulated [35S]GTP-gamma-S binding
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| 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 |
|---|---|---|---|
| pKb | 7 | - | - |
| Ki | 7 | 8.60 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392573 | — | — | 2 | 9.04 |
| CHEMBL237394 | — | — | 2 | 9.00 |
| CHEMBL237191 | — | — | 2 | 8.71 |
| CHEMBL442242 | — | — | 2 | 8.51 |
| CHEMBL263101 | — | — | 2 | 8.45 |
| CHEMBL351231 | — | — | 2 | 8.34 |
| CHEMBL393581 | — | — | 2 | 8.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392573 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL237394 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL237191 | — | Ki | = | 1.95 | nM | 8.71 |
| CHEMBL442242 | — | Ki | = | 3.09 | nM | 8.51 |
| CHEMBL263101 | — | Ki | = | 3.55 | nM | 8.45 |
| CHEMBL351231 | — | Ki | = | 4.57 | nM | 8.34 |
| CHEMBL393581 | — | Ki | = | 7.08 | nM | 8.15 |
| CHEMBL351231 | — | pKb | = | 8.34 | — | - |
| CHEMBL263101 | — | pKb | = | 8.45 | — | - |
| CHEMBL442242 | — | pKb | = | 8.51 | — | - |
| CHEMBL392573 | — | pKb | = | 9.04 | — | - |
| CHEMBL237191 | — | pKb | = | 8.71 | — | - |
| CHEMBL393581 | — | pKb | = | 8.15 | — | - |
| CHEMBL237394 | — | pKb | = | 9.0 | — | - |