Assay Detail
Functional
CHEMBL4151400
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
15
Total Activities
15
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 |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Synergistic Multiresidue Substitutions of a Macrocyclic c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Agouti-Related Protein (AGRP) Scaffold Yield Potent and >600-Fold MC4R versus MC3R Selective Melanocortin Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 7.03 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 11.00 |
| CHEMBL4170160 | — | — | 1 | 6.72 |
| CHEMBL4163787 | — | — | 1 | 6.40 |
| CHEMBL4173301 | — | — | 1 | 6.25 |
| CHEMBL4172753 | — | — | 1 | 6.22 |
| CHEMBL4159541 | — | — | 1 | 5.58 |
| CHEMBL4164846 | — | — | 1 | - |
| CHEMBL4169872 | — | — | 1 | - |
| CHEMBL4159229 | — | — | 1 | - |
| CHEMBL4166449 | — | — | 1 | - |
| CHEMBL4174361 | — | — | 1 | - |
| CHEMBL4166050 | — | — | 1 | - |
| CHEMBL4162603 | — | — | 1 | - |
| CHEMBL4164111 | — | — | 1 | - |
| CHEMBL4167239 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.01 | nM | 11.00 |
| CHEMBL4170160 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4163787 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4173301 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4172753 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4159541 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4164846 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4169872 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4159229 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4166449 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4174361 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4166050 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4162603 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4164111 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4167239 | — | EC50 | > | 100000.0 | nM | - |