Assay Detail
Functional
CHEMBL699051
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonism of the histamine H3-receptor in the rat cerebral cortex.
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design of potent non-thiourea H3-receptor histamine antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 7.11 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.37 |
| CHEMBL112504 | — | — | 1 | 8.32 |
| CHEMBL74293 | — | — | 1 | 7.89 |
| CHEMBL116126 | — | — | 1 | 7.77 |
| CHEMBL71597 | — | — | 1 | 7.70 |
| CHEMBL419574 | — | — | 1 | 7.54 |
| CHEMBL115212 | — | — | 1 | 7.38 |
| CHEMBL112349 | — | — | 1 | 7.38 |
| CHEMBL324605 | — | — | 1 | 7.28 |
| CHEMBL12160 | BURIMAMIDE | — | 1 | 7.16 |
| CHEMBL112577 | — | — | 1 | 7.04 |
| CHEMBL112013 | — | — | 1 | 6.80 |
| CHEMBL112503 | — | — | 1 | 6.77 |
| CHEMBL330926 | — | — | 1 | 6.73 |
| CHEMBL324890 | — | — | 1 | 6.70 |
| CHEMBL323855 | — | — | 1 | 6.70 |
| CHEMBL326797 | — | — | 1 | 6.62 |
| CHEMBL112390 | — | — | 1 | 6.48 |
| CHEMBL419206 | — | — | 1 | 6.47 |
| CHEMBL326940 | — | — | 1 | 6.40 |
| CHEMBL112391 | — | — | 1 | 5.89 |
| CHEMBL112178 | — | — | 1 | - |
| CHEMBL115289 | — | — | 1 | - |
| CHEMBL112377 | — | — | 1 | - |
| CHEMBL113210 | — | — | 1 | - |
| CHEMBL112576 | — | — | 1 | - |
| CHEMBL323415 | — | — | 1 | - |
| CHEMBL72881 | — | — | 1 | - |
| CHEMBL114907 | — | — | 1 | - |
| CHEMBL325089 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL112504 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL74293 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL116126 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL71597 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL419574 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL115212 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL112349 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL324605 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL12160 | BURIMAMIDE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL112577 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL112013 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL112503 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL330926 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL324890 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL323855 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL326797 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL112390 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL419206 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL326940 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL112391 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL112178 | — | Ki | ~ | 11000.0 | nM | - |
| CHEMBL115289 | — | Ki | ~ | 1300.0 | nM | - |
| CHEMBL112377 | — | Ki | ~ | 1000.0 | nM | - |
| CHEMBL113210 | — | Ki | ~ | 1300.0 | nM | - |
| CHEMBL112576 | — | Ki | ~ | 600.0 | nM | - |
| CHEMBL323415 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL72881 | — | Ki | ~ | 200.0 | nM | - |
| CHEMBL114907 | — | Ki | ~ | 500.0 | nM | - |
| CHEMBL325089 | — | Ki | ~ | 2500.0 | nM | - |
| CHEMBL325683 | — | Ki | ~ | 3100.0 | nM | - |