Assay Detail
Binding
CHEMBL907694
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Displacement of [3H]rauwolscine from human ADRA2C 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 | 7.54 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL425983 | — | — | 1 | 8.64 |
| CHEMBL218675 | — | — | 1 | 8.42 |
| CHEMBL217253 | — | — | 1 | 8.31 |
| CHEMBL218457 | — | — | 1 | 8.30 |
| CHEMBL217203 | — | — | 1 | 8.30 |
| CHEMBL218679 | — | — | 1 | 8.27 |
| CHEMBL216464 | — | — | 1 | 8.23 |
| CHEMBL268217 | — | — | 1 | 8.19 |
| CHEMBL217177 | — | — | 1 | 8.16 |
| CHEMBL214996 | — | — | 1 | 8.12 |
| CHEMBL217567 | — | — | 1 | 8.11 |
| CHEMBL383978 | — | — | 1 | 8.08 |
| CHEMBL1689423 | — | — | 1 | 8.08 |
| CHEMBL386169 | — | — | 1 | 8.07 |
| CHEMBL217202 | — | — | 1 | 8.07 |
| CHEMBL217254 | — | — | 1 | 8.05 |
| CHEMBL217542 | — | — | 1 | 8.04 |
| CHEMBL262901 | — | — | 1 | 7.82 |
| CHEMBL216727 | — | — | 1 | 7.80 |
| CHEMBL425803 | — | — | 1 | 7.60 |
| CHEMBL106525 | — | — | 1 | 7.55 |
| CHEMBL267464 | — | — | 1 | 7.46 |
| CHEMBL216290 | — | — | 1 | 7.46 |
| CHEMBL384925 | — | — | 1 | 7.46 |
| CHEMBL217366 | — | — | 1 | 7.43 |
| CHEMBL214661 | — | — | 1 | 7.42 |
| CHEMBL276417 | — | — | 1 | 7.37 |
| CHEMBL424917 | — | — | 1 | 7.30 |
| CHEMBL425622 | — | — | 1 | 7.28 |
| CHEMBL217278 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL425983 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL218675 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL217253 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL218457 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL217203 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL218679 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL216464 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL268217 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL217177 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL214996 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL217567 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL383978 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL1689423 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL386169 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL217202 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL217254 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL217542 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL262901 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL216727 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL425803 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL106525 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL267464 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL384925 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL216290 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL217366 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL214661 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL276417 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL424917 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL425622 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL217278 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL216197 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL216674 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL217452 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL440594 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL217768 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL218730 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL217568 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL385722 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL384318 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL216399 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL216072 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL217665 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL217180 | — | Ki | > | 5000.0 | nM | - |