Assay Detail
Binding
CHEMBL693829
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Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Optical isomers of rocastine and close analogues: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.29 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL505 | CHLORPHENIRAMINE | 4.0 | 1 | 8.06 |
| CHEMBL24517 | — | — | 1 | 7.62 |
| CHEMBL279907 | — | — | 1 | 6.37 |
| CHEMBL25198 | — | — | 1 | 6.06 |
| CHEMBL283760 | — | — | 1 | 4.92 |
| CHEMBL25622 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL505 | CHLORPHENIRAMINE | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL24517 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL279907 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL25198 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL283760 | — | IC50 | = | 11900.0 | nM | 4.92 |
| CHEMBL25622 | — | IC50 | = | 21000.0 | nM | 4.68 |