Assay Detail
Binding
CHEMBL698418
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In vitro inhibitory activity against histamine H3 receptor using [3H]histamine as radioligand from rat cerebral cortex synaptosomes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.64 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.40 |
| CHEMBL322039 | — | — | 1 | 8.08 |
| CHEMBL110957 | — | — | 1 | 8.03 |
| CHEMBL113030 | — | — | 1 | 7.92 |
| CHEMBL320970 | — | — | 1 | 7.85 |
| CHEMBL113077 | — | — | 1 | 7.82 |
| CHEMBL113738 | — | — | 1 | 7.75 |
| CHEMBL110258 | — | — | 1 | 7.72 |
| CHEMBL2112499 | — | — | 1 | 7.70 |
| CHEMBL112850 | — | — | 1 | 7.66 |
| CHEMBL109761 | — | — | 1 | 7.64 |
| CHEMBL332268 | — | — | 1 | 7.54 |
| CHEMBL110414 | — | — | 1 | 7.43 |
| CHEMBL109498 | — | — | 1 | 7.42 |
| CHEMBL326846 | — | — | 1 | 7.42 |
| CHEMBL112951 | — | — | 1 | 7.26 |
| CHEMBL110582 | — | — | 1 | 6.97 |
| CHEMBL322145 | — | — | 1 | 6.94 |
| CHEMBL110741 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL322039 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL110957 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL113030 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL320970 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL113077 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL113738 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL110258 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2112499 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL112850 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL109761 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL332268 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL110414 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL109498 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL326846 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL112951 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL110582 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL322145 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL110741 | — | Ki | ~ | 500.0 | nM | - |