Assay Detail
Binding
CHEMBL4480597
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and <i>in vitro</i> and <i>in vivo</i> characterization of 1-{4-[4-(substituted)piperazin-1-yl]butyl}guanidines and their piperidine analogues as histamine H<sub>3</sub> receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 8 | 7.32 | 9.18 |
| pA2 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 9.18 |
| CHEMBL4514561 | — | — | 1 | 7.22 |
| CHEMBL4546027 | — | — | 1 | 7.19 |
| CHEMBL4579190 | — | — | 1 | 7.18 |
| CHEMBL4482871 | — | — | 1 | 7.10 |
| CHEMBL4517581 | — | — | 1 | 6.97 |
| CHEMBL4585110 | — | — | 1 | 6.90 |
| CHEMBL4550675 | — | — | 1 | 6.80 |
| CHEMBL4591503 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511 | PYRILAMINE | Kd | = | 0.6607 | nM | 9.18 |
| CHEMBL4514561 | — | Kd | = | 60.26 | nM | 7.22 |
| CHEMBL4546027 | — | Kd | = | 64.57 | nM | 7.19 |
| CHEMBL4579190 | — | Kd | = | 66.07 | nM | 7.18 |
| CHEMBL4482871 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL4517581 | — | Kd | = | 107.15 | nM | 6.97 |
| CHEMBL4585110 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL4550675 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL4591503 | — | pA2 | - | — | - |