Assay Detail
Functional
CHEMBL861795
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
31
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| 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 |
|---|---|---|---|
| Kd | 19 | 8.47 | 10.10 |
| pA2 | 12 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL371730 | — | — | 1 | 10.10 |
| CHEMBL200382 | — | — | 1 | 9.90 |
| CHEMBL373000 | — | — | 1 | 9.80 |
| CHEMBL383825 | — | — | 1 | 8.90 |
| CHEMBL373263 | — | — | 1 | 8.80 |
| CHEMBL373010 | — | — | 1 | 8.80 |
| CHEMBL200941 | — | — | 1 | 8.80 |
| CHEMBL424847 | — | — | 1 | 8.60 |
| CHEMBL200643 | — | — | 1 | 8.40 |
| CHEMBL200453 | — | — | 1 | 8.30 |
| CHEMBL200267 | — | — | 1 | 8.30 |
| CHEMBL200139 | — | — | 1 | 8.20 |
| CHEMBL200189 | — | — | 1 | 8.20 |
| CHEMBL200519 | — | — | 1 | 7.90 |
| CHEMBL200268 | — | — | 1 | 7.90 |
| CHEMBL380584 | — | — | 1 | 7.80 |
| CHEMBL200853 | — | — | 1 | 7.80 |
| CHEMBL200244 | — | — | 1 | 7.40 |
| CHEMBL200540 | — | — | 1 | 7.10 |
| CHEMBL199972 | — | — | 1 | - |
| CHEMBL200842 | — | — | 1 | - |
| CHEMBL200173 | — | — | 1 | - |
| CHEMBL200907 | — | — | 1 | - |
| CHEMBL382295 | — | — | 1 | - |
| CHEMBL200806 | — | — | 1 | - |
| CHEMBL200740 | — | — | 1 | - |
| CHEMBL372772 | — | — | 1 | - |
| CHEMBL200930 | — | — | 1 | - |
| CHEMBL200542 | — | — | 1 | - |
| CHEMBL199520 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL371730 | — | Kd | = | 0.07943 | nM | 10.10 |
| CHEMBL200382 | — | Kd | = | 0.1259 | nM | 9.90 |
| CHEMBL373000 | — | Kd | = | 0.1585 | nM | 9.80 |
| CHEMBL383825 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL373263 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL373010 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL200941 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL424847 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL200643 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL200453 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL200267 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL200139 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL200189 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL200519 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL200268 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL380584 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL200853 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL200244 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL200540 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL199972 | — | pA2 | - | — | - | |
| CHEMBL200842 | — | pA2 | - | — | - | |
| CHEMBL200173 | — | pA2 | - | — | - | |
| CHEMBL200907 | — | pA2 | - | — | - | |
| CHEMBL382295 | — | pA2 | - | — | - | |
| CHEMBL200806 | — | pA2 | - | — | - | |
| CHEMBL200740 | — | pA2 | - | — | - | |
| CHEMBL372772 | — | pA2 | - | — | - | |
| CHEMBL200930 | — | pA2 | - | — | - | |
| CHEMBL200542 | — | pA2 | - | — | - | |
| CHEMBL199520 | — | pA2 | - | — | - | |
| CHEMBL200155 | — | pA2 | - | — | - |