Assay Detail
Functional
CHEMBL698419
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Rat Histamine H3 receptor antagonism determined by [K+] - evoked depolarization-induced release of [3H]histamine from rat cerebral cortex synaptosomes
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
A novel series of (phenoxyalkyl)imidazoles as potent H3-receptor histamine antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 7.58 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL340196 | — | — | 1 | 8.43 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.40 |
| CHEMBL112504 | — | — | 1 | 8.32 |
| CHEMBL127404 | — | — | 1 | 8.29 |
| CHEMBL420892 | — | — | 1 | 8.22 |
| CHEMBL123857 | — | — | 1 | 8.05 |
| CHEMBL125320 | — | — | 1 | 8.05 |
| CHEMBL338887 | — | — | 1 | 7.96 |
| CHEMBL127575 | — | — | 1 | 7.92 |
| CHEMBL113030 | — | — | 1 | 7.92 |
| CHEMBL320970 | — | — | 1 | 7.85 |
| CHEMBL125775 | — | — | 1 | 7.72 |
| CHEMBL419574 | — | — | 1 | 7.70 |
| CHEMBL124187 | — | — | 1 | 7.68 |
| CHEMBL124270 | — | — | 1 | 7.64 |
| CHEMBL435383 | — | — | 1 | 7.64 |
| CHEMBL124864 | — | — | 1 | 7.62 |
| CHEMBL341499 | — | — | 1 | 7.46 |
| CHEMBL125056 | — | — | 1 | 7.42 |
| CHEMBL127405 | — | — | 1 | 7.41 |
| CHEMBL125751 | — | — | 1 | 7.27 |
| CHEMBL125947 | — | — | 1 | 7.25 |
| CHEMBL264817 | — | — | 1 | 7.17 |
| CHEMBL340298 | — | — | 1 | 7.10 |
| CHEMBL125022 | — | — | 1 | 7.05 |
| CHEMBL332730 | — | — | 1 | 6.86 |
| CHEMBL125261 | — | — | 1 | 6.50 |
| CHEMBL339606 | — | — | 1 | 6.47 |
| CHEMBL127195 | — | — | 1 | 6.32 |
| CHEMBL331836 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL340196 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL112504 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL127404 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL420892 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL123857 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL125320 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL338887 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL127575 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL113030 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL320970 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL125775 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL419574 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL124187 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL124270 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL435383 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL124864 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL341499 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL125056 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL127405 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL125751 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL125947 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL264817 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL340298 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL125022 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL332730 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL125261 | — | Ki | = | 313.0 | nM | 6.50 |
| CHEMBL339606 | — | Ki | = | 338.0 | nM | 6.47 |
| CHEMBL127195 | — | Ki | = | 483.0 | nM | 6.32 |
| CHEMBL331836 | — | Ki | > | 500.0 | nM | - |
| CHEMBL338851 | — | Ki | > | 500.0 | nM | - |