Assay Detail
Binding
CHEMBL1048093
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Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.03 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL571390 | — | — | 1 | 7.80 |
| CHEMBL568892 | — | — | 1 | 7.70 |
| CHEMBL914 | FEXOFENADINE | 4.0 | 1 | 7.57 |
| CHEMBL571389 | — | — | 1 | 7.41 |
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 7.40 |
| CHEMBL571174 | — | — | 1 | 7.21 |
| CHEMBL571391 | — | — | 1 | 7.19 |
| CHEMBL572034 | — | — | 1 | 6.92 |
| CHEMBL570695 | — | — | 1 | 6.81 |
| CHEMBL570033 | — | — | 1 | 6.69 |
| CHEMBL127508 | AZACYCLONOL | 2.0 | 1 | 6.18 |
| CHEMBL571073 | — | — | 1 | 5.50 |
| CHEMBL571819 | — | — | 1 | - |
| CHEMBL570961 | — | — | 1 | - |
| CHEMBL570915 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL571390 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL568892 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL914 | FEXOFENADINE | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL571389 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL17157 | TERFENADINE | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL571174 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL571391 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL572034 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL570695 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL570033 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL127508 | AZACYCLONOL | Ki | = | 659.0 | nM | 6.18 |
| CHEMBL571073 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL571819 | — | Ki | - | — | - | |
| CHEMBL570961 | — | Ki | - | — | - | |
| CHEMBL570915 | — | Ki | - | — | - |