Assay Detail
Binding
CHEMBL997224
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Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells
14
Total Activities
14
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 | 14 | 8.18 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2096742 | — | — | 1 | 9.22 |
| CHEMBL500743 | — | — | 1 | 9.22 |
| CHEMBL430239 | MELATONAN | — | 1 | 8.96 |
| CHEMBL503229 | — | — | 1 | 8.92 |
| CHEMBL501592 | — | — | 1 | 8.82 |
| CHEMBL502300 | — | — | 1 | 8.60 |
| CHEMBL524861 | — | — | 1 | 8.24 |
| CHEMBL509582 | — | — | 1 | 8.14 |
| CHEMBL501642 | — | — | 1 | 7.96 |
| CHEMBL508501 | — | — | 1 | 7.64 |
| CHEMBL194552 | — | — | 1 | 7.48 |
| CHEMBL444493 | — | — | 1 | 7.41 |
| CHEMBL455070 | — | — | 1 | 7.30 |
| CHEMBL526334 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2096742 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL500743 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL430239 | MELATONAN | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL503229 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL501592 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL502300 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL524861 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL509582 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL501642 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL508501 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL194552 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL444493 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL455070 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL526334 | — | IC50 | = | 270.0 | nM | 6.57 |