Assay Detail
Binding
CHEMBL997225
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.34 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL501592 | — | — | 1 | 9.15 |
| CHEMBL2096742 | — | — | 1 | 9.05 |
| CHEMBL524861 | — | — | 1 | 8.96 |
| CHEMBL502300 | — | — | 1 | 8.66 |
| CHEMBL503229 | — | — | 1 | 8.62 |
| CHEMBL500743 | — | — | 1 | 8.60 |
| CHEMBL430239 | MELATONAN | — | 1 | 8.12 |
| CHEMBL509582 | — | — | 1 | 7.66 |
| CHEMBL455070 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL501592 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2096742 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL524861 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL502300 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL503229 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL500743 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL430239 | MELATONAN | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL509582 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL455070 | — | IC50 | = | 590.0 | nM | 6.23 |