Assay Detail
Binding
CHEMBL830379
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Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.44 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1172 | DESLORATADINE | 4.0 | 1 | 9.01 |
| CHEMBL187264 | — | — | 1 | 8.05 |
| CHEMBL188021 | — | — | 1 | 7.85 |
| CHEMBL1000 | CETIRIZINE | 4.0 | 1 | 7.85 |
| CHEMBL185905 | — | — | 1 | 7.72 |
| CHEMBL444083 | — | — | 1 | 7.58 |
| CHEMBL186125 | — | — | 1 | 7.52 |
| CHEMBL360202 | — | — | 1 | 7.30 |
| CHEMBL185825 | — | — | 1 | 6.96 |
| CHEMBL187637 | — | — | 1 | 6.53 |
| CHEMBL425358 | — | — | 1 | 6.52 |
| CHEMBL998 | LORATADINE | 4.0 | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1172 | DESLORATADINE | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL187264 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL188021 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1000 | CETIRIZINE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL185905 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL444083 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL186125 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL360202 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL185825 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL187637 | — | Ki | = | 295.0 | nM | 6.53 |
| CHEMBL425358 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL998 | LORATADINE | Ki | = | 414.0 | nM | 6.38 |