Assay Detail
Binding
CHEMBL866473
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Displacement of [3H]N-alpha-methylhistamine from guinea pig histamine H3 receptor
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 7.91 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL380525 | — | — | 1 | 9.00 |
| CHEMBL381741 | — | — | 1 | 8.52 |
| CHEMBL380139 | — | — | 1 | 8.52 |
| CHEMBL205129 | — | — | 1 | 8.52 |
| CHEMBL424675 | — | — | 1 | 8.52 |
| CHEMBL200267 | — | — | 1 | 8.40 |
| CHEMBL379445 | — | — | 1 | 8.40 |
| CHEMBL203696 | — | — | 1 | 8.40 |
| CHEMBL377500 | — | — | 1 | 8.40 |
| CHEMBL204193 | — | — | 1 | 8.30 |
| CHEMBL204606 | — | — | 1 | 8.22 |
| CHEMBL378821 | — | — | 1 | 8.10 |
| CHEMBL204639 | — | — | 1 | 8.05 |
| CHEMBL204235 | — | — | 1 | 8.00 |
| CHEMBL382677 | — | — | 1 | 7.92 |
| CHEMBL437500 | — | — | 1 | 7.92 |
| CHEMBL203983 | — | — | 1 | 7.92 |
| CHEMBL439689 | — | — | 1 | 7.89 |
| CHEMBL204951 | — | — | 1 | 7.82 |
| CHEMBL379885 | — | — | 1 | 7.82 |
| CHEMBL204301 | — | — | 1 | 7.80 |
| CHEMBL203604 | — | — | 1 | 7.80 |
| CHEMBL203910 | — | — | 1 | 7.77 |
| CHEMBL425765 | — | — | 1 | 7.64 |
| CHEMBL204742 | — | — | 1 | 7.62 |
| CHEMBL203805 | — | — | 1 | 7.58 |
| CHEMBL381717 | — | — | 1 | 7.48 |
| CHEMBL204705 | — | — | 1 | 7.47 |
| CHEMBL426487 | — | — | 1 | 7.40 |
| CHEMBL204640 | — | — | 1 | 7.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL380525 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL381741 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL424675 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL205129 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL380139 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL200267 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL379445 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL203696 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL377500 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL204193 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL204606 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL378821 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL204639 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL204235 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL203983 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL382677 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL437500 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL439689 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL204951 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL379885 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL204301 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL203604 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL203910 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL425765 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL204742 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL203805 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL381717 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL204705 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL426487 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL204640 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL381070 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL377278 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL204587 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL203912 | — | Ki | = | 315.0 | nM | 6.50 |