Assay Detail
Binding
CHEMBL4357485
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin-5 Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.79 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 8.89 |
| CHEMBL4102048 | — | — | 1 | 8.72 |
| CHEMBL4565367 | — | — | 1 | 8.09 |
| CHEMBL4538274 | — | — | 1 | 7.42 |
| CHEMBL3577981 | — | — | 1 | 7.16 |
| CHEMBL4566163 | — | — | 1 | 6.87 |
| CHEMBL4531291 | — | — | 1 | 6.00 |
| CHEMBL4474215 | — | — | 1 | 5.72 |
| CHEMBL4466724 | — | — | 1 | 5.70 |
| CHEMBL4587214 | — | — | 1 | 5.17 |
| CHEMBL4541505 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4102048 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4565367 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4538274 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3577981 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4566163 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4531291 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4474215 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4466724 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4587214 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4541505 | — | IC50 | = | 10000.0 | nM | 5.00 |