Assay Detail
Functional
CHEMBL4041390
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at the Melanocortin-5 Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 6.98 | 10.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.68 |
| CHEMBL4072797 | — | — | 1 | 5.58 |
| CHEMBL4098651 | — | — | 1 | 4.69 |
| CHEMBL4083137 | — | — | 1 | - |
| CHEMBL4077783 | — | — | 1 | - |
| CHEMBL4065443 | — | — | 1 | - |
| CHEMBL4066514 | — | — | 1 | - |
| CHEMBL4075125 | — | — | 1 | - |
| CHEMBL4089149 | — | — | 1 | - |
| CHEMBL4066929 | — | — | 1 | - |
| CHEMBL4086679 | — | — | 1 | - |
| CHEMBL4104582 | — | — | 1 | - |
| CHEMBL4071633 | — | — | 1 | - |
| CHEMBL4093379 | — | — | 1 | - |
| CHEMBL4072662 | — | — | 1 | - |
| CHEMBL4101128 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.021 | nM | 10.68 |
| CHEMBL4072797 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4098651 | — | EC50 | = | 20500.0 | nM | 4.69 |
| CHEMBL4083137 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4077783 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4065443 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4066514 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4075125 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4089149 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4066929 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4086679 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4104582 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4071633 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4093379 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4072662 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4101128 | — | EC50 | > | 100000.0 | nM | - |