Assay Detail
Functional
CHEMBL866474
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against histamine H3 receptor in guinea pig ileum
34
Total Activities
34
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
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 |
|---|---|---|---|
| Kd | 17 | 7.89 | 8.80 |
| pA2 | 17 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL379445 | — | — | 1 | 8.80 |
| CHEMBL424675 | — | — | 1 | 8.60 |
| CHEMBL205129 | — | — | 1 | 8.50 |
| CHEMBL380525 | — | — | 1 | 8.40 |
| CHEMBL200267 | — | — | 1 | 8.30 |
| CHEMBL204235 | — | — | 1 | 8.10 |
| CHEMBL425765 | — | — | 1 | 7.80 |
| CHEMBL204301 | — | — | 1 | 7.80 |
| CHEMBL204742 | — | — | 1 | 7.70 |
| CHEMBL203805 | — | — | 1 | 7.70 |
| CHEMBL203983 | — | — | 1 | 7.70 |
| CHEMBL378821 | — | — | 1 | 7.60 |
| CHEMBL203604 | — | — | 1 | 7.60 |
| CHEMBL377500 | — | — | 1 | 7.60 |
| CHEMBL381717 | — | — | 1 | 7.50 |
| CHEMBL439689 | — | — | 1 | 7.30 |
| CHEMBL203910 | — | — | 1 | 7.10 |
| CHEMBL204640 | — | — | 1 | - |
| CHEMBL381741 | — | — | 1 | - |
| CHEMBL203696 | — | — | 1 | - |
| CHEMBL204606 | — | — | 1 | - |
| CHEMBL380139 | — | — | 1 | - |
| CHEMBL379885 | — | — | 1 | - |
| CHEMBL204951 | — | — | 1 | - |
| CHEMBL437500 | — | — | 1 | - |
| CHEMBL204639 | — | — | 1 | - |
| CHEMBL382677 | — | — | 1 | - |
| CHEMBL204587 | — | — | 1 | - |
| CHEMBL204705 | — | — | 1 | - |
| CHEMBL203912 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL379445 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL424675 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL205129 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL380525 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL200267 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL204235 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL425765 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL204301 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL204742 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL203805 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL203983 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL203604 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL377500 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL378821 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL381717 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL439689 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL203910 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL204193 | — | pA2 | - | — | - | |
| CHEMBL426487 | — | pA2 | - | — | - | |
| CHEMBL377278 | — | pA2 | - | — | - | |
| CHEMBL381070 | — | pA2 | - | — | - | |
| CHEMBL203912 | — | pA2 | - | — | - | |
| CHEMBL204705 | — | pA2 | - | — | - | |
| CHEMBL204587 | — | pA2 | - | — | - | |
| CHEMBL382677 | — | pA2 | - | — | - | |
| CHEMBL204639 | — | pA2 | - | — | - | |
| CHEMBL437500 | — | pA2 | - | — | - | |
| CHEMBL204951 | — | pA2 | - | — | - | |
| CHEMBL379885 | — | pA2 | - | — | - | |
| CHEMBL380139 | — | pA2 | - | — | - | |
| CHEMBL204606 | — | pA2 | - | — | - | |
| CHEMBL203696 | — | pA2 | - | — | - | |
| CHEMBL381741 | — | pA2 | - | — | - | |
| CHEMBL204640 | — | pA2 | - | — | - |