Assay Detail
Functional
CHEMBL2329833
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melanocortin-4 receptor (mMC4R).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 6.27 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.64 |
| CHEMBL1688107 | — | — | 1 | 8.77 |
| CHEMBL2323795 | — | — | 1 | 7.31 |
| CHEMBL2323786 | — | — | 1 | 6.75 |
| CHEMBL2323793 | — | — | 1 | 6.72 |
| CHEMBL2323785 | — | — | 1 | 6.70 |
| CHEMBL2323787 | — | — | 1 | 6.64 |
| CHEMBL1688111 | — | — | 1 | 6.49 |
| CHEMBL2323799 | — | — | 1 | 5.74 |
| CHEMBL2323790 | — | — | 1 | 5.72 |
| CHEMBL2323529 | — | — | 1 | 5.65 |
| CHEMBL2323798 | — | — | 1 | 5.59 |
| CHEMBL2323788 | — | — | 1 | 5.40 |
| CHEMBL2323789 | — | — | 1 | 5.35 |
| CHEMBL2323800 | — | — | 1 | 5.15 |
| CHEMBL2323792 | — | — | 1 | 5.11 |
| CHEMBL2323797 | — | — | 1 | 5.09 |
| CHEMBL2323791 | — | — | 1 | 4.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.23 | nM | 9.64 |
| CHEMBL1688107 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2323795 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2323786 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2323793 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2323785 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2323787 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1688111 | — | EC50 | = | 324.0 | nM | 6.49 |
| CHEMBL2323799 | — | EC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL2323790 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2323529 | — | EC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL2323798 | — | EC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL2323788 | — | EC50 | = | 4020.0 | nM | 5.40 |
| CHEMBL2323789 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2323800 | — | EC50 | = | 7120.0 | nM | 5.15 |
| CHEMBL2323792 | — | EC50 | = | 7720.0 | nM | 5.11 |
| CHEMBL2323797 | — | EC50 | = | 8070.0 | nM | 5.09 |
| CHEMBL2323791 | — | EC50 | = | 10350.0 | nM | 4.99 |