Assay Detail
Binding
CHEMBL997222
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Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC1R expressed in HEK293 cells
15
Total Activities
15
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 |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 15 | 7.69 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 9.70 |
| CHEMBL503229 | — | — | 1 | 9.30 |
| CHEMBL2096742 | — | — | 1 | 9.00 |
| CHEMBL524861 | — | — | 1 | 8.96 |
| CHEMBL502300 | — | — | 1 | 8.92 |
| CHEMBL501592 | — | — | 1 | 8.64 |
| CHEMBL500743 | — | — | 1 | 8.57 |
| CHEMBL526334 | — | — | 1 | 6.72 |
| CHEMBL508501 | — | — | 1 | 6.40 |
| CHEMBL194552 | — | — | 1 | 6.22 |
| CHEMBL510270 | — | — | 1 | 6.08 |
| CHEMBL525399 | — | — | 1 | 6.00 |
| CHEMBL455070 | — | — | 1 | 5.46 |
| CHEMBL509582 | — | — | 1 | - |
| CHEMBL501642 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL503229 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2096742 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL524861 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL502300 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL501592 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL500743 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL526334 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL508501 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL194552 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL510270 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL525399 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL455070 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL509582 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL501642 | — | IC50 | > | 4800.0 | nM | - |