Assay Detail
Functional
CHEMBL1247348
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Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 17 | 7.47 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | — | 1 | 9.17 |
| CHEMBL1098230 | — | — | 1 | 9.12 |
| CHEMBL82298 | IMMETHRIDINE | — | 1 | 8.96 |
| CHEMBL1243335 | — | — | 1 | 7.82 |
| CHEMBL1243366 | — | — | 1 | 7.66 |
| CHEMBL1243394 | — | — | 1 | 7.64 |
| CHEMBL1243305 | — | — | 1 | 7.42 |
| CHEMBL1243334 | — | — | 1 | 7.32 |
| CHEMBL1243365 | — | — | 1 | 7.17 |
| CHEMBL1243395 | — | — | 1 | 7.13 |
| CHEMBL1243367 | — | — | 1 | 6.85 |
| CHEMBL78838 | — | — | 1 | 6.85 |
| CHEMBL1243393 | — | — | 1 | 6.85 |
| CHEMBL1243333 | — | — | 1 | 6.27 |
| CHEMBL81644 | — | — | 1 | 5.89 |
| CHEMBL1243303 | — | — | 1 | - |
| CHEMBL1243304 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | EC50 | = | 0.67 | nM | 9.17 |
| CHEMBL1098230 | — | EC50 | = | 0.75 | nM | 9.12 |
| CHEMBL82298 | IMMETHRIDINE | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1243335 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1243366 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1243394 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1243305 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1243334 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL1243365 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL1243395 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1243367 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL78838 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1243393 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1243333 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL81644 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1243303 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL1243304 | — | EC50 | > | 1000.0 | nM | - |