Assay Detail
Binding
CHEMBL858407
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Binding affinity towards histamine H3 receptor using [3H](R)-alpha-methylhistamine as radioligand in guinea pig ileum LMMP homogenates
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.39 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL268229 | — | — | 1 | 9.82 |
| CHEMBL299589 | — | — | 1 | 8.44 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.98 |
| CHEMBL301176 | — | — | 1 | 7.77 |
| CHEMBL300704 | — | — | 1 | 7.55 |
| CHEMBL53361 | — | — | 1 | 7.50 |
| CHEMBL417017 | — | — | 1 | 7.49 |
| CHEMBL55018 | — | — | 1 | 7.42 |
| CHEMBL52090 | — | — | 1 | 7.40 |
| CHEMBL52080 | — | — | 1 | 7.26 |
| CHEMBL53412 | — | — | 1 | 7.07 |
| CHEMBL298581 | — | — | 1 | 6.97 |
| CHEMBL54858 | — | — | 1 | 6.73 |
| CHEMBL301838 | — | — | 1 | 5.94 |
| CHEMBL53056 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL268229 | — | Ki | = | 0.1514 | nM | 9.82 |
| CHEMBL299589 | — | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL90 | HISTAMINE | Ki | = | 10.47 | nM | 7.98 |
| CHEMBL301176 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL300704 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL53361 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL417017 | — | Ki | = | 32.36 | nM | 7.49 |
| CHEMBL55018 | — | Ki | = | 38.02 | nM | 7.42 |
| CHEMBL52090 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL52080 | — | Ki | = | 54.95 | nM | 7.26 |
| CHEMBL53412 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL298581 | — | Ki | = | 107.15 | nM | 6.97 |
| CHEMBL54858 | — | Ki | = | 186.21 | nM | 6.73 |
| CHEMBL301838 | — | Ki | = | 1148.15 | nM | 5.94 |
| CHEMBL53056 | — | Ki | = | 2884.03 | nM | 5.54 |