Assay Detail
Binding
CHEMBL1106977
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
29
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel benzothiophene H1-antihistamines for the treatment of insomnia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 7.46 | 8.77 |
| IC50 | 4 | 5.10 | 5.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1092765 | — | — | 1 | 8.77 |
| CHEMBL1092377 | — | — | 1 | 8.57 |
| CHEMBL1092766 | — | — | 1 | 8.54 |
| CHEMBL1093294 | — | — | 1 | 8.54 |
| CHEMBL1091775 | — | — | 1 | 8.41 |
| CHEMBL1093058 | — | — | 1 | 8.36 |
| CHEMBL1091782 | — | — | 1 | 8.34 |
| CHEMBL1091069 | — | — | 1 | 8.30 |
| CHEMBL1092118 | — | — | 1 | 8.28 |
| CHEMBL1092494 | — | — | 1 | 8.10 |
| CHEMBL1092126 | — | — | 1 | 8.03 |
| CHEMBL1090432 | — | — | 1 | 7.92 |
| CHEMBL1092495 | — | — | 1 | 7.89 |
| CHEMBL1092813 | — | — | 1 | 7.77 |
| CHEMBL1092767 | — | — | 1 | 7.46 |
| CHEMBL1091793 | — | — | 1 | 7.42 |
| CHEMBL1091792 | — | — | 1 | 7.23 |
| CHEMBL1092496 | — | — | 1 | 7.16 |
| CHEMBL1092812 | — | — | 1 | 6.92 |
| CHEMBL1093607 | — | — | 1 | 6.91 |
| CHEMBL1091791 | — | — | 1 | 6.41 |
| CHEMBL1091777 | — | — | 1 | 5.46 |
| CHEMBL1091774 | — | — | 1 | 5.21 |
| CHEMBL1091776 | — | — | 1 | 5.00 |
| CHEMBL1091790 | — | — | 1 | 4.64 |
| CHEMBL1093044 | — | — | 1 | 4.50 |
| CHEMBL1091778 | — | — | 1 | 4.10 |
| CHEMBL1090433 | — | — | 1 | - |
| CHEMBL564144 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1092765 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1092377 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1092766 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL1093294 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL1091775 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1093058 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL1091782 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL1091069 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1092118 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL1092494 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1092126 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL1090432 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1092495 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1092813 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1092767 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL1091793 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL1091792 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL1092496 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL1092812 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1093607 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL1091791 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL1091777 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1091774 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL1091776 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL1091790 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL1093044 | — | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL1091778 | — | Ki | = | 79000.0 | nM | 4.10 |
| CHEMBL1090433 | — | IC50 | = | 256000.0 | nM | - |
| CHEMBL564144 | — | Ki | = | 4000.0 | nM | - |