Assay Detail
Binding
CHEMBL1247347
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Displacement of [3H](R)-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells by liquid scintillation counting
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.47 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | — | 1 | 9.52 |
| CHEMBL1098230 | — | — | 1 | 9.37 |
| CHEMBL82298 | IMMETHRIDINE | — | 1 | 9.11 |
| CHEMBL1243394 | — | — | 1 | 7.85 |
| CHEMBL1243335 | — | — | 1 | 7.80 |
| CHEMBL1243305 | — | — | 1 | 7.75 |
| CHEMBL1243366 | — | — | 1 | 7.19 |
| CHEMBL78838 | — | — | 1 | 7.12 |
| CHEMBL1243334 | — | — | 1 | 7.12 |
| CHEMBL1243365 | — | — | 1 | 6.92 |
| CHEMBL1243393 | — | — | 1 | 6.89 |
| CHEMBL1243395 | — | — | 1 | 6.75 |
| CHEMBL1243367 | — | — | 1 | 6.70 |
| CHEMBL1243333 | — | — | 1 | 6.28 |
| CHEMBL81644 | — | — | 1 | 5.75 |
| CHEMBL1243303 | — | — | 1 | - |
| CHEMBL1243304 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1098230 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL82298 | IMMETHRIDINE | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL1243394 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1243335 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1243305 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1243366 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL78838 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL1243334 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL1243365 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1243393 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL1243395 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL1243367 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL1243333 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL81644 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL1243303 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1243304 | — | Ki | > | 1000.0 | nM | - |