Assay Detail
Functional
CHEMBL997226
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 16 | 6.77 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 9.52 |
| CHEMBL2096742 | — | — | 1 | 8.82 |
| CHEMBL503229 | — | — | 1 | 8.82 |
| CHEMBL526334 | — | — | 1 | 6.92 |
| CHEMBL194552 | — | — | 1 | 6.80 |
| CHEMBL501592 | — | — | 1 | 6.21 |
| CHEMBL444493 | — | — | 1 | 6.12 |
| CHEMBL500743 | — | — | 1 | 6.09 |
| CHEMBL510270 | — | — | 1 | 5.85 |
| CHEMBL502300 | — | — | 1 | 5.77 |
| CHEMBL524861 | — | — | 1 | 5.57 |
| CHEMBL508501 | — | — | 1 | 4.72 |
| CHEMBL455070 | — | — | 1 | - |
| CHEMBL509582 | — | — | 1 | - |
| CHEMBL501642 | — | — | 1 | - |
| CHEMBL525399 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL2096742 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL503229 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL526334 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL194552 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL501592 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL444493 | — | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL500743 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL510270 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL502300 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL524861 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL508501 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL455070 | — | EC50 | = | - | nM | - |
| CHEMBL509582 | — | EC50 | = | - | nM | - |
| CHEMBL501642 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL525399 | — | EC50 | > | 5000.0 | nM | - |