Assay Detail
Functional
CHEMBL5513836
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Antagonist activity at human H1 receptor expressed in PathHunter CHO-K1 HRH1 beta-arrestin cells preincubated for 30 mins followed by agonist addition at 6 times EC80 and measured after 90 to 180 mins by PathHunter assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PathHunter CHO-K1 HRH1 beta-arrestin |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of the novel and potent histamine H1 receptor antagonists for treatment of allergic diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.63 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1172 | DESLORATADINE | 4.0 | 1 | 9.19 |
| CHEMBL5557294 | — | — | 1 | 8.71 |
| CHEMBL5565071 | — | — | 1 | 7.91 |
| CHEMBL5560560 | — | — | 1 | 7.74 |
| CHEMBL5556597 | — | — | 1 | 7.72 |
| CHEMBL5568499 | — | — | 1 | 7.66 |
| CHEMBL5559786 | — | — | 1 | 7.62 |
| CHEMBL5542993 | — | — | 1 | 7.47 |
| CHEMBL5567709 | — | — | 1 | 7.36 |
| CHEMBL5555844 | — | — | 1 | 7.24 |
| CHEMBL5558681 | — | — | 1 | 7.19 |
| CHEMBL5554991 | — | — | 1 | 7.17 |
| CHEMBL5532329 | — | — | 1 | 6.90 |
| CHEMBL5555858 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1172 | DESLORATADINE | IC50 | = | 0.644 | nM | 9.19 |
| CHEMBL5557294 | — | IC50 | = | 1.97 | nM | 8.71 |
| CHEMBL5565071 | — | IC50 | = | 12.21 | nM | 7.91 |
| CHEMBL5560560 | — | IC50 | = | 18.36 | nM | 7.74 |
| CHEMBL5556597 | — | IC50 | = | 19.25 | nM | 7.72 |
| CHEMBL5568499 | — | IC50 | = | 21.81 | nM | 7.66 |
| CHEMBL5559786 | — | IC50 | = | 24.12 | nM | 7.62 |
| CHEMBL5542993 | — | IC50 | = | 33.91 | nM | 7.47 |
| CHEMBL5567709 | — | IC50 | = | 44.18 | nM | 7.36 |
| CHEMBL5555844 | — | IC50 | = | 57.23 | nM | 7.24 |
| CHEMBL5558681 | — | IC50 | = | 64.51 | nM | 7.19 |
| CHEMBL5554991 | — | IC50 | = | 66.93 | nM | 7.17 |
| CHEMBL5532329 | — | IC50 | = | 125.7 | nM | 6.90 |
| CHEMBL5555858 | — | IC50 | = | 125.7 | nM | 6.90 |