Assay Detail
Binding
CHEMBL1769658
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human adrenergic Alpha-1B receptor expressed in rat intact fibroblasts
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| Ki | 37 | 6.98 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1767156 | — | — | 1 | 8.20 |
| CHEMBL1767136 | — | — | 1 | 7.90 |
| CHEMBL1767141 | — | — | 1 | 7.80 |
| CHEMBL1767154 | — | — | 1 | 7.70 |
| CHEMBL1765111 | — | — | 1 | 7.50 |
| CHEMBL1767164 | GSK-1004723 | 2.0 | 1 | 7.50 |
| CHEMBL1767168 | — | — | 1 | 7.40 |
| CHEMBL1767165 | — | — | 1 | 7.30 |
| CHEMBL639 | AZELASTINE | 4.0 | 1 | 7.30 |
| CHEMBL1767167 | — | — | 1 | 7.30 |
| CHEMBL1767160 | — | — | 1 | 7.10 |
| CHEMBL1767140 | — | — | 1 | 7.10 |
| CHEMBL1767155 | — | — | 1 | 7.10 |
| CHEMBL1767161 | — | — | 1 | 7.00 |
| CHEMBL1767166 | — | — | 1 | 6.90 |
| CHEMBL1767159 | — | — | 1 | 6.90 |
| CHEMBL1767137 | — | — | 1 | 6.80 |
| CHEMBL1767158 | — | — | 1 | 6.80 |
| CHEMBL1767152 | — | — | 1 | 6.70 |
| CHEMBL1767134 | — | — | 1 | 6.70 |
| CHEMBL1767157 | — | — | 1 | 6.50 |
| CHEMBL1767162 | — | — | 1 | 6.50 |
| CHEMBL1767149 | — | — | 1 | 6.50 |
| CHEMBL1767135 | — | — | 1 | 6.50 |
| CHEMBL1767138 | — | — | 1 | 6.40 |
| CHEMBL1767145 | — | — | 1 | 6.40 |
| CHEMBL1767148 | — | — | 1 | 6.30 |
| CHEMBL1767146 | — | — | 1 | 6.20 |
| CHEMBL1767153 | — | — | 1 | 6.00 |
| CHEMBL1767139 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1767156 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL1767136 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1767141 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1767154 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1765111 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1767164 | GSK-1004723 | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1767168 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL1767165 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL639 | AZELASTINE | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1767167 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1767160 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL1767155 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL1767140 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL1767161 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1767159 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL1767166 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL1767137 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1767158 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1767152 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1767134 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1767157 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1767162 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1767149 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1767135 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1767138 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1767145 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1767148 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL1767146 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1767153 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1767139 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1767151 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1767163 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1767150 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1767147 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1767144 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1767143 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1767142 | — | Ki | > | 1995.26 | nM | - |