Assay Detail
Binding
CHEMBL4480596
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as effect on pyrilamine-induced inhibition of electrically evoked contraction treated 20 mins after pyrilamine stimulation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Jejunum |
| 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 | 9 | 7.57 | 8.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.98 |
| CHEMBL4585110 | — | — | 1 | 8.35 |
| CHEMBL4482871 | — | — | 1 | 8.10 |
| CHEMBL4514561 | — | — | 1 | 7.99 |
| CHEMBL4579190 | — | — | 1 | 7.97 |
| CHEMBL4546027 | — | — | 1 | 7.90 |
| CHEMBL4517581 | — | — | 1 | 7.30 |
| CHEMBL4550675 | — | — | 1 | 5.78 |
| CHEMBL4591503 | — | — | 1 | 5.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | Kd | = | 1.047 | nM | 8.98 |
| CHEMBL4585110 | — | Kd | = | 4.467 | nM | 8.35 |
| CHEMBL4482871 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL4514561 | — | Kd | = | 10.23 | nM | 7.99 |
| CHEMBL4579190 | — | Kd | = | 10.72 | nM | 7.97 |
| CHEMBL4546027 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL4517581 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL4550675 | — | Kd | = | 1659.59 | nM | 5.78 |
| CHEMBL4591503 | — | Kd | = | 1659.59 | nM | 5.78 |