Assay Detail
Functional
CHEMBL1769659
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Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 5 | 9.00 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL639 | AZELASTINE | 4.0 | 1 | 9.70 |
| CHEMBL1767164 | GSK-1004723 | 2.0 | 1 | 9.10 |
| CHEMBL1767165 | — | — | 1 | 8.90 |
| CHEMBL1767167 | — | — | 1 | 8.90 |
| CHEMBL1767166 | — | — | 1 | 8.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL639 | AZELASTINE | Kd | = | 0.1995 | nM | 9.70 |
| CHEMBL1767164 | GSK-1004723 | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL1767165 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL1767167 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL1767166 | — | Kd | = | 3.981 | nM | 8.40 |