Assay Detail
Binding
CHEMBL4402771
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CGP12177 from human beta2 adrenoceptor H2.64C mutant expressed in HEK293T cell membranes
19
Total Activities
16
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Development of covalent antagonists for β1- and β2-adrenergic receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.83 | 10.08 |
| KiH | 3 | - | - |
| KiL | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4537221 | — | — | 1 | 10.08 |
| CHEMBL4456301 | — | — | 1 | 9.74 |
| CHEMBL4437569 | — | — | 1 | 9.59 |
| CHEMBL4463246 | — | — | 1 | 9.12 |
| CHEMBL4463925 | — | — | 1 | 8.92 |
| CHEMBL4566666 | — | — | 1 | 8.82 |
| CHEMBL4553747 | — | — | 1 | 8.42 |
| CHEMBL4473272 | — | — | 1 | 7.58 |
| CHEMBL4456505 | — | — | 1 | 7.18 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | - |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | - |
| CHEMBL645 | BISOPROLOL | 4.0 | 1 | - |
| CHEMBL280822 | CGP-20712A | — | 1 | - |
| CHEMBL4450085 | — | — | 2 | - |
| CHEMBL4443911 | — | — | 2 | - |
| CHEMBL4576034 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4537221 | — | Ki | = | 0.083 | nM | 10.08 |
| CHEMBL4456301 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL4437569 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL4463246 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL4463925 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4566666 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4553747 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL4473272 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4456505 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL4576034 | — | KiL | = | 3600.0 | nM | - |
| CHEMBL4443911 | — | KiL | = | 8400.0 | nM | - |
| CHEMBL4450085 | — | KiL | = | 2500.0 | nM | - |
| CHEMBL4576034 | — | KiH | = | 77.0 | nM | - |
| CHEMBL4443911 | — | KiH | = | 36.0 | nM | - |
| CHEMBL4450085 | — | KiH | = | 3.6 | nM | - |
| CHEMBL280822 | CGP-20712A | Ki | - | — | - | |
| CHEMBL13 | METOPROLOL | Ki | - | — | - | |
| CHEMBL645 | BISOPROLOL | Ki | - | — | - | |
| CHEMBL27 | PROPRANOLOL | Ki | - | — | - |