Assay Detail
Binding
CHEMBL694915
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Potency against histamine H1 receptor on guinea pig ileum
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 5 | 8.64 | 9.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL855 | TRIPROLIDINE | 4.0 | 1 | 9.90 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 1 | 9.00 |
| CHEMBL278398 | PHENINDAMINE | 2.0 | 1 | 8.80 |
| CHEMBL609131 | — | — | 1 | 8.70 |
| CHEMBL612084 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL855 | TRIPROLIDINE | Kd | = | 0.1259 | nM | 9.90 |
| CHEMBL516 | CYPROHEPTADINE | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL278398 | PHENINDAMINE | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL609131 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL612084 | — | Kd | = | 158.49 | nM | 6.80 |