Assay Detail
Binding
CHEMBL861794
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Displacement of [3H]N-alpha-methylhistamine from histamine H3 receptor in guinea pig brain
32
Total Activities
32
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
Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 8.01 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200382 | — | — | 1 | 9.70 |
| CHEMBL373000 | — | — | 1 | 9.70 |
| CHEMBL18661 | IMMEPIP | — | 1 | 9.40 |
| CHEMBL371730 | — | — | 1 | 9.40 |
| CHEMBL200643 | — | — | 1 | 8.70 |
| CHEMBL424847 | — | — | 1 | 8.70 |
| CHEMBL200268 | — | — | 1 | 8.70 |
| CHEMBL383825 | — | — | 1 | 8.70 |
| CHEMBL200139 | — | — | 1 | 8.52 |
| CHEMBL373263 | — | — | 1 | 8.52 |
| CHEMBL200941 | — | — | 1 | 8.52 |
| CHEMBL200267 | — | — | 1 | 8.40 |
| CHEMBL380584 | — | — | 1 | 8.30 |
| CHEMBL200189 | — | — | 1 | 8.30 |
| CHEMBL373010 | — | — | 1 | 8.22 |
| CHEMBL200853 | — | — | 1 | 8.05 |
| CHEMBL200519 | — | — | 1 | 8.05 |
| CHEMBL200806 | — | — | 1 | 7.89 |
| CHEMBL200453 | — | — | 1 | 7.77 |
| CHEMBL200244 | — | — | 1 | 7.75 |
| CHEMBL200907 | — | — | 1 | 7.70 |
| CHEMBL382295 | — | — | 1 | 7.68 |
| CHEMBL200540 | — | — | 1 | 7.60 |
| CHEMBL200173 | — | — | 1 | 7.40 |
| CHEMBL200542 | — | — | 1 | 7.36 |
| CHEMBL372772 | — | — | 1 | 7.30 |
| CHEMBL199972 | — | — | 1 | 7.22 |
| CHEMBL200155 | — | — | 1 | 7.05 |
| CHEMBL200930 | — | — | 1 | 6.80 |
| CHEMBL200740 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200382 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL373000 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL18661 | IMMEPIP | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL371730 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL200643 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL424847 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL200268 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL383825 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL200139 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL373263 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL200941 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL200267 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL380584 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL200189 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL373010 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL200519 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL200853 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL200806 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL200453 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL200244 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL200907 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL382295 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL200540 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL200173 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL200542 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL372772 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL199972 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL200155 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL200930 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL200740 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL199520 | — | Ki | = | 625.0 | nM | 6.20 |
| CHEMBL200842 | — | Ki | = | 970.0 | nM | 6.01 |