Assay Detail
Binding
CHEMBL4145116
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting
21
Total Activities
21
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
Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 5.61 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL499 | TIMOLOL | 4.0 | 1 | 8.27 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 7.93 |
| CHEMBL24 | ATENOLOL | 4.0 | 1 | 5.82 |
| CHEMBL4170519 | — | — | 1 | 5.18 |
| CHEMBL4174345 | — | — | 1 | 4.98 |
| CHEMBL4161638 | — | — | 1 | 4.87 |
| CHEMBL4163665 | — | — | 1 | 4.81 |
| CHEMBL4162590 | — | — | 1 | 4.57 |
| CHEMBL4170536 | — | — | 1 | 4.10 |
| CHEMBL4167473 | — | — | 1 | - |
| CHEMBL4159562 | — | — | 1 | - |
| CHEMBL4170860 | — | — | 1 | - |
| CHEMBL4162920 | — | — | 1 | - |
| CHEMBL4174295 | — | — | 1 | - |
| CHEMBL4166379 | — | — | 1 | - |
| CHEMBL4167532 | — | — | 1 | - |
| CHEMBL4175397 | — | — | 1 | - |
| CHEMBL4170908 | — | — | 1 | - |
| CHEMBL4174691 | — | — | 1 | - |
| CHEMBL4173735 | — | — | 1 | - |
| CHEMBL4160295 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL499 | TIMOLOL | Ki | = | 5.37 | nM | 8.27 |
| CHEMBL27 | PROPRANOLOL | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL24 | ATENOLOL | Ki | = | 1513.56 | nM | 5.82 |
| CHEMBL4170519 | — | Ki | = | 6606.93 | nM | 5.18 |
| CHEMBL4174345 | — | Ki | = | 10471.29 | nM | 4.98 |
| CHEMBL4161638 | — | Ki | = | 13489.63 | nM | 4.87 |
| CHEMBL4163665 | — | Ki | = | 15488.17 | nM | 4.81 |
| CHEMBL4162590 | — | Ki | = | 26915.35 | nM | 4.57 |
| CHEMBL4170536 | — | Ki | = | 79432.82 | nM | 4.10 |
| CHEMBL4167473 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4159562 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4170860 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4162920 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4174295 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4166379 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4167532 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4175397 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4170908 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4174691 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4173735 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4160295 | — | Ki | > | 100000.0 | nM | - |