Assay Detail
Binding
CHEMBL907693
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Displacement of [3H]rauwolscine from human ADRA2B expressed in S115 cells
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | S115 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 5.76 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384925 | — | — | 1 | 7.02 |
| CHEMBL216464 | — | — | 1 | 6.38 |
| CHEMBL217203 | — | — | 1 | 6.24 |
| CHEMBL217567 | — | — | 1 | 6.22 |
| CHEMBL1689423 | — | — | 1 | 6.06 |
| CHEMBL218730 | — | — | 1 | 6.04 |
| CHEMBL217177 | — | — | 1 | 5.96 |
| CHEMBL217568 | — | — | 1 | 5.95 |
| CHEMBL383978 | — | — | 1 | 5.94 |
| CHEMBL217366 | — | — | 1 | 5.92 |
| CHEMBL218679 | — | — | 1 | 5.90 |
| CHEMBL262901 | — | — | 1 | 5.89 |
| CHEMBL216674 | — | — | 1 | 5.88 |
| CHEMBL425983 | — | — | 1 | 5.88 |
| CHEMBL218675 | — | — | 1 | 5.83 |
| CHEMBL106525 | — | — | 1 | 5.82 |
| CHEMBL440594 | — | — | 1 | 5.78 |
| CHEMBL218457 | — | — | 1 | 5.77 |
| CHEMBL424917 | — | — | 1 | 5.76 |
| CHEMBL217254 | — | — | 1 | 5.75 |
| CHEMBL268217 | — | — | 1 | 5.72 |
| CHEMBL217452 | — | — | 1 | 5.69 |
| CHEMBL216072 | — | — | 1 | 5.60 |
| CHEMBL217278 | — | — | 1 | 5.58 |
| CHEMBL217542 | — | — | 1 | 5.58 |
| CHEMBL386169 | — | — | 1 | 5.58 |
| CHEMBL216197 | — | — | 1 | 5.54 |
| CHEMBL217768 | — | — | 1 | 5.53 |
| CHEMBL214661 | — | — | 1 | 5.50 |
| CHEMBL216727 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384925 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL216464 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL217203 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL217567 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL1689423 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL218730 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL217177 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL217568 | — | Ki | = | 1120.0 | nM | 5.95 |
| CHEMBL383978 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL217366 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL218679 | — | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL262901 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL216674 | — | Ki | = | 1320.0 | nM | 5.88 |
| CHEMBL425983 | — | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL218675 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL106525 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL440594 | — | Ki | = | 1680.0 | nM | 5.78 |
| CHEMBL218457 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL424917 | — | Ki | = | 1750.0 | nM | 5.76 |
| CHEMBL217254 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL268217 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL217452 | — | Ki | = | 2030.0 | nM | 5.69 |
| CHEMBL216072 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL217278 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL217542 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL386169 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL216197 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL217768 | — | Ki | = | 2980.0 | nM | 5.53 |
| CHEMBL214661 | — | Ki | = | 3150.0 | nM | 5.50 |
| CHEMBL216727 | — | Ki | = | 3470.0 | nM | 5.46 |
| CHEMBL217202 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL384318 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL216399 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL217665 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL425622 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL217253 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL385722 | — | Ki | = | 17600.0 | nM | 4.75 |
| CHEMBL217180 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL216290 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL276417 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL425803 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL267464 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL214996 | — | Ki | > | 10000.0 | nM | - |