Assay Detail
Functional
CHEMBL3591120
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Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 17 | 4.96 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL761 | NAPHAZOLINE | 4.0 | 1 | 7.26 |
| CHEMBL3588902 | — | — | 1 | 6.76 |
| CHEMBL286080 | SKF-38393 | — | 1 | 5.86 |
| CHEMBL2087646 | — | — | 1 | 5.50 |
| CHEMBL3588904 | — | — | 1 | 5.46 |
| CHEMBL3588911 | — | — | 1 | 3.83 |
| CHEMBL1327 | — | — | 1 | 3.47 |
| CHEMBL3588905 | — | — | 1 | 3.32 |
| CHEMBL3588909 | — | — | 1 | 3.20 |
| CHEMBL3588907 | — | — | 1 | - |
| CHEMBL3588906 | — | — | 1 | - |
| CHEMBL598391 | — | — | 1 | - |
| CHEMBL3588908 | — | — | 1 | - |
| CHEMBL3588903 | — | — | 1 | - |
| CHEMBL3588910 | — | — | 1 | - |
| CHEMBL3590203 | — | — | 1 | - |
| CHEMBL341473 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL761 | NAPHAZOLINE | EC50 | = | 54.95 | nM | 7.26 |
| CHEMBL3588902 | — | EC50 | = | 173.78 | nM | 6.76 |
| CHEMBL286080 | SKF-38393 | EC50 | = | 1380.38 | nM | 5.86 |
| CHEMBL2087646 | — | EC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL3588904 | — | EC50 | = | 3467.37 | nM | 5.46 |
| CHEMBL3588911 | — | EC50 | = | 147910.84 | nM | 3.83 |
| CHEMBL1327 | — | EC50 | = | 338844.16 | nM | 3.47 |
| CHEMBL3588905 | — | EC50 | = | 478630.09 | nM | 3.32 |
| CHEMBL3588909 | — | EC50 | = | 630957.34 | nM | 3.20 |
| CHEMBL3588907 | — | EC50 | > | 501187.23 | nM | - |
| CHEMBL3588906 | — | EC50 | > | 501187.23 | nM | - |
| CHEMBL598391 | — | EC50 | > | 501187.23 | nM | - |
| CHEMBL3588908 | — | EC50 | > | 501187.23 | nM | - |
| CHEMBL3588903 | — | EC50 | > | 501187.23 | nM | - |
| CHEMBL3588910 | — | EC50 | > | 501187.23 | nM | - |
| CHEMBL3590203 | — | EC50 | > | 501187.23 | nM | - |
| CHEMBL341473 | — | EC50 | > | 501187.23 | nM | - |