Assay Detail
Binding
CHEMBL693985
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity for histamine H3 receptor was determined in guinea-pig cerebral cortex using [3H](R)-alpha-methylhistamine
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H(3) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.69 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL311578 | — | — | 1 | 9.03 |
| CHEMBL75625 | — | — | 1 | 8.97 |
| CHEMBL308633 | — | — | 1 | 8.85 |
| CHEMBL80582 | — | — | 1 | 8.70 |
| CHEMBL76256 | — | — | 1 | 8.45 |
| CHEMBL77925 | — | — | 1 | 8.45 |
| CHEMBL76807 | — | — | 1 | 8.38 |
| CHEMBL75912 | — | — | 1 | 8.33 |
| CHEMBL307850 | — | — | 1 | 8.33 |
| CHEMBL80422 | — | — | 1 | 8.29 |
| CHEMBL440689 | — | — | 1 | 8.27 |
| CHEMBL80253 | — | — | 1 | 8.20 |
| CHEMBL76556 | — | — | 1 | 8.17 |
| CHEMBL308085 | — | — | 1 | 8.12 |
| CHEMBL76002 | — | — | 1 | 8.10 |
| CHEMBL274490 | — | — | 1 | 8.10 |
| CHEMBL78272 | — | — | 1 | 7.97 |
| CHEMBL76521 | — | — | 1 | 7.70 |
| CHEMBL75911 | — | — | 1 | 7.59 |
| CHEMBL76944 | — | — | 1 | 7.52 |
| CHEMBL77244 | — | — | 1 | 7.37 |
| CHEMBL12344 | DIMAPRIT | — | 1 | 7.32 |
| CHEMBL80475 | — | — | 1 | 7.27 |
| CHEMBL77774 | — | — | 1 | 7.27 |
| CHEMBL307875 | — | — | 1 | 7.25 |
| CHEMBL79709 | — | — | 1 | 7.08 |
| CHEMBL80547 | — | — | 1 | 7.00 |
| CHEMBL309269 | — | — | 1 | 6.64 |
| CHEMBL75871 | — | — | 1 | 6.49 |
| CHEMBL77249 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL311578 | — | Ki | = | 0.9333 | nM | 9.03 |
| CHEMBL75625 | — | Ki | = | 1.072 | nM | 8.97 |
| CHEMBL308633 | — | Ki | = | 1.413 | nM | 8.85 |
| CHEMBL80582 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL76256 | — | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL77925 | — | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL76807 | — | Ki | = | 4.169 | nM | 8.38 |
| CHEMBL75912 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL307850 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL80422 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL440689 | — | Ki | = | 5.37 | nM | 8.27 |
| CHEMBL80253 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL76556 | — | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL308085 | — | Ki | = | 7.586 | nM | 8.12 |
| CHEMBL274490 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL76002 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL78272 | — | Ki | = | 10.72 | nM | 7.97 |
| CHEMBL76521 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL75911 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL76944 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL77244 | — | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL12344 | DIMAPRIT | Ki | = | 47.86 | nM | 7.32 |
| CHEMBL80475 | — | Ki | = | 53.7 | nM | 7.27 |
| CHEMBL77774 | — | Ki | = | 53.7 | nM | 7.27 |
| CHEMBL307875 | — | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL79709 | — | Ki | = | 83.18 | nM | 7.08 |
| CHEMBL80547 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL309269 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL75871 | — | Ki | = | 323.59 | nM | 6.49 |
| CHEMBL77249 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL420757 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL77594 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL307146 | — | Ki | = | 1698.24 | nM | 5.77 |