Assay Detail
Binding
CHEMBL693574
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Binding affinity against H3 receptor in guinea pig brain using [3H]N-alpha-methyl histamine as radioligand
19
Total Activities
19
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
Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.74 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL292909 | — | — | 1 | 9.00 |
| CHEMBL444827 | — | — | 1 | 9.00 |
| CHEMBL418653 | — | — | 1 | 9.00 |
| CHEMBL59123 | — | — | 1 | 8.40 |
| CHEMBL61437 | — | — | 1 | 8.15 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.14 |
| CHEMBL59504 | — | — | 1 | 8.10 |
| CHEMBL59512 | — | — | 1 | 8.00 |
| CHEMBL292195 | — | — | 1 | 7.82 |
| CHEMBL60524 | — | — | 1 | 7.80 |
| CHEMBL58239 | — | — | 1 | 7.64 |
| CHEMBL61348 | — | — | 1 | 7.54 |
| CHEMBL60175 | — | — | 1 | 7.48 |
| CHEMBL58973 | — | — | 1 | 7.30 |
| CHEMBL293895 | — | — | 1 | 7.25 |
| CHEMBL446147 | — | — | 1 | 6.92 |
| CHEMBL60961 | — | — | 1 | 6.62 |
| CHEMBL417951 | — | — | 1 | 6.58 |
| CHEMBL58549 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL292909 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL444827 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL418653 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL59123 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL61437 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL59504 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL59512 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL292195 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL60524 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL58239 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL61348 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL60175 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL58973 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL293895 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL446147 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL60961 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL417951 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL58549 | — | Ki | = | 510.0 | nM | 6.29 |