Assay Detail
Binding
CHEMBL3590965
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
37
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Cell-based and virtual fragment screening for adrenergic α2C receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 5.91 | 8.64 |
| Emax | 17 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL761 | NAPHAZOLINE | 4.0 | 2 | 8.64 |
| CHEMBL3590203 | — | — | 2 | 7.93 |
| CHEMBL3588902 | — | — | 2 | 7.14 |
| CHEMBL286080 | SKF-38393 | — | 2 | 7.08 |
| CHEMBL1879790 | — | — | 1 | 6.62 |
| CHEMBL3588903 | — | — | 2 | 6.27 |
| CHEMBL129399 | — | — | 1 | 6.25 |
| CHEMBL2087646 | — | — | 2 | 6.19 |
| CHEMBL3588904 | — | — | 2 | 5.97 |
| CHEMBL598391 | — | — | 2 | 5.93 |
| CHEMBL341473 | — | — | 2 | 5.82 |
| CHEMBL3588905 | — | — | 2 | 5.28 |
| CHEMBL3588906 | — | — | 2 | 5.14 |
| CHEMBL3588907 | — | — | 2 | 5.08 |
| CHEMBL3588908 | — | — | 2 | 4.98 |
| CHEMBL3588912 | — | — | 1 | 4.86 |
| CHEMBL1327 | — | — | 2 | 4.82 |
| CHEMBL3588909 | — | — | 2 | 4.81 |
| CHEMBL3588910 | — | — | 2 | 4.81 |
| CHEMBL3588911 | — | — | 2 | 4.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL761 | NAPHAZOLINE | Ki | = | 2.291 | nM | 8.64 |
| CHEMBL3590203 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL3588902 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL286080 | SKF-38393 | Ki | = | 83.18 | nM | 7.08 |
| CHEMBL1879790 | — | Ki | = | 239.88 | nM | 6.62 |
| CHEMBL3588903 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL129399 | — | Ki | = | 562.34 | nM | 6.25 |
| CHEMBL2087646 | — | Ki | = | 645.65 | nM | 6.19 |
| CHEMBL3588904 | — | Ki | = | 1071.52 | nM | 5.97 |
| CHEMBL598391 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL341473 | — | Ki | = | 1513.56 | nM | 5.82 |
| CHEMBL3588905 | — | Ki | = | 5248.07 | nM | 5.28 |
| CHEMBL3588906 | — | Ki | = | 7244.36 | nM | 5.14 |
| CHEMBL3588907 | — | Ki | = | 8317.64 | nM | 5.08 |
| CHEMBL3588908 | — | Ki | = | 10471.29 | nM | 4.98 |
| CHEMBL3588912 | — | Ki | = | 13803.84 | nM | 4.86 |
| CHEMBL1327 | — | Ki | = | 15135.61 | nM | 4.82 |
| CHEMBL3588910 | — | Ki | = | 15488.17 | nM | 4.81 |
| CHEMBL3588909 | — | Ki | = | 15488.17 | nM | 4.81 |
| CHEMBL3588911 | — | Ki | = | 22387.21 | nM | 4.65 |
| CHEMBL761 | NAPHAZOLINE | Emax | = | 102.0 | % | - |
| CHEMBL3590203 | — | Emax | = | 100.0 | % | - |
| CHEMBL3588902 | — | Emax | = | 100.0 | % | - |
| CHEMBL286080 | SKF-38393 | Emax | = | 92.0 | % | - |
| CHEMBL3588903 | — | Emax | = | 92.0 | % | - |
| CHEMBL2087646 | — | Emax | = | 92.0 | % | - |
| CHEMBL3588904 | — | Emax | = | 98.0 | % | - |
| CHEMBL598391 | — | Emax | = | 97.0 | % | - |
| CHEMBL3588905 | — | Emax | = | 102.0 | % | - |
| CHEMBL3588906 | — | Emax | = | 99.0 | % | - |
| CHEMBL3588907 | — | Emax | = | 104.0 | % | - |
| CHEMBL3588908 | — | Emax | = | 81.0 | % | - |
| CHEMBL1327 | — | Emax | = | 78.0 | % | - |
| CHEMBL3588909 | — | Emax | = | 81.0 | % | - |
| CHEMBL3588910 | — | Emax | = | 81.0 | % | - |
| CHEMBL3588911 | — | Emax | = | 102.0 | % | - |
| CHEMBL341473 | — | Emax | = | 100.0 | % | - |