Assay Detail
Binding
CHEMBL856624
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]rauwolscine from human ADRA2A 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 | 5.86 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216399 | — | — | 1 | 6.30 |
| CHEMBL384925 | — | — | 1 | 6.24 |
| CHEMBL217768 | — | — | 1 | 6.20 |
| CHEMBL218730 | — | — | 1 | 6.19 |
| CHEMBL217452 | — | — | 1 | 6.17 |
| CHEMBL425983 | — | — | 1 | 6.15 |
| CHEMBL217665 | — | — | 1 | 6.14 |
| CHEMBL217568 | — | — | 1 | 6.11 |
| CHEMBL217567 | — | — | 1 | 6.10 |
| CHEMBL262901 | — | — | 1 | 6.08 |
| CHEMBL216674 | — | — | 1 | 6.07 |
| CHEMBL216197 | — | — | 1 | 6.05 |
| CHEMBL218679 | — | — | 1 | 6.05 |
| CHEMBL383978 | — | — | 1 | 6.04 |
| CHEMBL216464 | — | — | 1 | 6.02 |
| CHEMBL214661 | — | — | 1 | 6.01 |
| CHEMBL440594 | — | — | 1 | 6.00 |
| CHEMBL217278 | — | — | 1 | 5.98 |
| CHEMBL425803 | — | — | 1 | 5.96 |
| CHEMBL218675 | — | — | 1 | 5.93 |
| CHEMBL216727 | — | — | 1 | 5.91 |
| CHEMBL424917 | — | — | 1 | 5.88 |
| CHEMBL276417 | — | — | 1 | 5.86 |
| CHEMBL217202 | — | — | 1 | 5.85 |
| CHEMBL218457 | — | — | 1 | 5.85 |
| CHEMBL1689423 | — | — | 1 | 5.84 |
| CHEMBL425622 | — | — | 1 | 5.77 |
| CHEMBL216290 | — | — | 1 | 5.77 |
| CHEMBL217203 | — | — | 1 | 5.73 |
| CHEMBL217254 | — | — | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216399 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL384925 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL217768 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL218730 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL217452 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL425983 | — | Ki | = | 715.0 | nM | 6.15 |
| CHEMBL217665 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL217568 | — | Ki | = | 775.0 | nM | 6.11 |
| CHEMBL217567 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL262901 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL216674 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL218679 | — | Ki | = | 895.0 | nM | 6.05 |
| CHEMBL216197 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL383978 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL216464 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL214661 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL440594 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL217278 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL425803 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL218675 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL216727 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL424917 | — | Ki | = | 1320.0 | nM | 5.88 |
| CHEMBL276417 | — | Ki | = | 1380.0 | nM | 5.86 |
| CHEMBL217202 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL218457 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL1689423 | — | Ki | = | 1430.0 | nM | 5.84 |
| CHEMBL425622 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL216290 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL217203 | — | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL217254 | — | Ki | = | 1870.0 | nM | 5.73 |
| CHEMBL268217 | — | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL217177 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL217542 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL267464 | — | Ki | = | 2210.0 | nM | 5.66 |
| CHEMBL384318 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL217253 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL214996 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL106525 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL217180 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL217366 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL386169 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL385722 | — | Ki | = | 9600.0 | nM | 5.02 |
| CHEMBL216072 | — | Ki | > | 10000.0 | nM | - |