Assay Detail
Binding
CHEMBL4052188
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa1-Arg-(pI)DPhe-Xaa4-NH2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.04 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 8.70 |
| CHEMBL4083717 | — | — | 1 | 7.89 |
| CHEMBL4078495 | — | — | 1 | 7.37 |
| CHEMBL4063911 | — | — | 1 | 7.08 |
| CHEMBL4071063 | — | — | 1 | 7.03 |
| CHEMBL264190 | — | — | 1 | 6.92 |
| CHEMBL4079298 | — | — | 1 | 6.87 |
| CHEMBL4072129 | — | — | 1 | 6.66 |
| CHEMBL4091894 | — | — | 1 | 6.56 |
| CHEMBL4102774 | — | — | 1 | 6.34 |
| CHEMBL4092424 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4083717 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4078495 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4063911 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4071063 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL264190 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4079298 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4072129 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4091894 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL4102774 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL4092424 | — | IC50 | = | 850.0 | nM | 6.07 |