Assay Detail
Binding
CHEMBL697095
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Affinity for displacement of [125I]iodoproxyfan from human histamine H3 receptors stably expressed in CHO cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 7.77 | 10.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14364 | — | — | 1 | 10.07 |
| CHEMBL15153 | — | — | 1 | 10.04 |
| CHEMBL15056 | — | — | 1 | 9.48 |
| CHEMBL276938 | — | — | 1 | 9.28 |
| CHEMBL14754 | — | — | 1 | 8.85 |
| CHEMBL14484 | — | — | 1 | 8.82 |
| CHEMBL277061 | — | — | 1 | 8.74 |
| CHEMBL14595 | — | — | 1 | 8.44 |
| CHEMBL14573 | — | — | 1 | 8.12 |
| CHEMBL15289 | — | — | 1 | 8.11 |
| CHEMBL15101 | — | — | 1 | 8.00 |
| CHEMBL276305 | — | — | 1 | 7.92 |
| CHEMBL15098 | — | — | 1 | 7.82 |
| CHEMBL14665 | — | — | 1 | 7.75 |
| CHEMBL14657 | — | — | 1 | 7.72 |
| CHEMBL14816 | — | — | 1 | 7.58 |
| CHEMBL14283 | — | — | 1 | 7.50 |
| CHEMBL275617 | — | — | 1 | 7.47 |
| CHEMBL14656 | — | — | 1 | 7.30 |
| CHEMBL275874 | — | — | 1 | 7.16 |
| CHEMBL14781 | — | — | 1 | 7.11 |
| CHEMBL14849 | — | — | 1 | 7.09 |
| CHEMBL14753 | — | — | 1 | 7.07 |
| CHEMBL14524 | — | — | 1 | 7.05 |
| CHEMBL277988 | — | — | 1 | 6.73 |
| CHEMBL280011 | — | — | 1 | 6.72 |
| CHEMBL14860 | — | — | 1 | 6.44 |
| CHEMBL14498 | — | — | 1 | 6.42 |
| CHEMBL14740 | — | — | 1 | 6.39 |
| CHEMBL277113 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14364 | — | Ki | = | 0.086 | nM | 10.07 |
| CHEMBL15153 | — | Ki | = | 0.091 | nM | 10.04 |
| CHEMBL15056 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL276938 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL14754 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL14484 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL277061 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL14595 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL14573 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL15289 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL15101 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL276305 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL15098 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL14665 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL14657 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL14816 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL14283 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL275617 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL14656 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL275874 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL14781 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL14849 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL14753 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL14524 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL277988 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL280011 | — | Ki | = | 191.0 | nM | 6.72 |
| CHEMBL14860 | — | Ki | = | 362.0 | nM | 6.44 |
| CHEMBL14498 | — | Ki | = | 378.0 | nM | 6.42 |
| CHEMBL14740 | — | Ki | = | 411.0 | nM | 6.39 |
| CHEMBL277113 | — | Ki | = | 1130.0 | nM | 5.95 |