Assay Detail
Binding
CHEMBL2345299
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Biophysical fragment screening of the β1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.25 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200234 | — | — | 1 | 7.17 |
| CHEMBL2335158 | — | — | 1 | 7.07 |
| CHEMBL1424807 | — | — | 1 | 6.97 |
| CHEMBL2335166 | — | — | 1 | 6.70 |
| CHEMBL2335159 | — | — | 1 | 6.67 |
| CHEMBL1559535 | — | — | 1 | 6.65 |
| CHEMBL2335164 | — | — | 1 | 6.60 |
| CHEMBL2335161 | — | — | 1 | 6.27 |
| CHEMBL2335167 | — | — | 1 | 6.17 |
| CHEMBL2335160 | — | — | 1 | 6.13 |
| CHEMBL2335162 | — | — | 1 | 5.90 |
| CHEMBL9434 | PHENYLPIPERAZINE | — | 1 | 5.87 |
| CHEMBL2335163 | — | — | 1 | 5.80 |
| CHEMBL2335165 | — | — | 1 | 5.80 |
| CHEMBL2335156 | — | — | 1 | 5.63 |
| CHEMBL2335157 | — | — | 1 | 5.60 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200234 | — | Ki | = | 67.61 | nM | 7.17 |
| CHEMBL2335158 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL1424807 | — | Ki | = | 107.15 | nM | 6.97 |
| CHEMBL2335166 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL2335159 | — | Ki | = | 213.8 | nM | 6.67 |
| CHEMBL1559535 | — | Ki | = | 223.87 | nM | 6.65 |
| CHEMBL2335164 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL2335161 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL2335167 | — | Ki | = | 676.08 | nM | 6.17 |
| CHEMBL2335160 | — | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL2335162 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL9434 | PHENYLPIPERAZINE | Ki | = | 1348.96 | nM | 5.87 |
| CHEMBL2335163 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL2335165 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL2335156 | — | Ki | = | 2344.23 | nM | 5.63 |
| CHEMBL2335157 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL18772 | QUIPAZINE | Ki | = | 6309.57 | nM | 5.20 |