Assay Detail
Binding
CHEMBL695758
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Binding affinity towards histamine H3 receptor using [3H](R)-alpha-methylhistamine as radioligand in guinea pig cortical homogenates
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| 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 | 16 | 7.60 | 10.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL268229 | — | — | 1 | 10.07 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 9.84 |
| CHEMBL299589 | — | — | 1 | 8.99 |
| CHEMBL301176 | — | — | 1 | 7.85 |
| CHEMBL55836 | — | — | 1 | 7.85 |
| CHEMBL53361 | — | — | 1 | 7.83 |
| CHEMBL300704 | — | — | 1 | 7.79 |
| CHEMBL55018 | — | — | 1 | 7.64 |
| CHEMBL417017 | — | — | 1 | 7.60 |
| CHEMBL52090 | — | — | 1 | 7.30 |
| CHEMBL54858 | — | — | 1 | 7.07 |
| CHEMBL52080 | — | — | 1 | 6.94 |
| CHEMBL53412 | — | — | 1 | 6.86 |
| CHEMBL301838 | — | — | 1 | 6.31 |
| CHEMBL298581 | — | — | 1 | 5.99 |
| CHEMBL53056 | — | — | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL268229 | — | Ki | = | 0.08511 | nM | 10.07 |
| CHEMBL90 | HISTAMINE | Ki | = | 0.1445 | nM | 9.84 |
| CHEMBL299589 | — | Ki | = | 1.023 | nM | 8.99 |
| CHEMBL301176 | — | Ki | = | 14.13 | nM | 7.85 |
| CHEMBL55836 | — | Ki | = | 14.13 | nM | 7.85 |
| CHEMBL53361 | — | Ki | = | 14.79 | nM | 7.83 |
| CHEMBL300704 | — | Ki | = | 16.22 | nM | 7.79 |
| CHEMBL55018 | — | Ki | = | 22.91 | nM | 7.64 |
| CHEMBL417017 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL52090 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL54858 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL52080 | — | Ki | = | 114.82 | nM | 6.94 |
| CHEMBL53412 | — | Ki | = | 138.04 | nM | 6.86 |
| CHEMBL301838 | — | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL298581 | — | Ki | = | 1023.29 | nM | 5.99 |
| CHEMBL53056 | — | Ki | = | 1862.09 | nM | 5.73 |