Assay Detail
Functional
CHEMBL997229
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Agonist activity at human MC5R 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 |
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 | 7.82 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL501592 | — | — | 1 | 9.52 |
| CHEMBL2096742 | — | — | 1 | 8.92 |
| CHEMBL500743 | — | — | 1 | 8.80 |
| CHEMBL503229 | — | — | 1 | 8.72 |
| CHEMBL430239 | MELATONAN | — | 1 | 8.48 |
| CHEMBL524861 | — | — | 1 | 7.68 |
| CHEMBL502300 | — | — | 1 | 7.07 |
| CHEMBL509582 | — | — | 1 | 5.62 |
| CHEMBL455070 | — | — | 1 | 5.60 |
| CHEMBL501642 | — | — | 1 | - |
| CHEMBL444493 | — | — | 1 | - |
| CHEMBL194552 | — | — | 1 | - |
| CHEMBL508501 | — | — | 1 | - |
| CHEMBL526334 | — | — | 1 | - |
| CHEMBL510270 | — | — | 1 | - |
| CHEMBL525399 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL501592 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL2096742 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL500743 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL503229 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL430239 | MELATONAN | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL524861 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL502300 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL509582 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL455070 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL501642 | — | EC50 | = | - | nM | - |
| CHEMBL444493 | — | EC50 | = | - | nM | - |
| CHEMBL194552 | — | EC50 | = | - | nM | - |
| CHEMBL508501 | — | EC50 | = | - | nM | - |
| CHEMBL526334 | — | EC50 | = | - | nM | - |
| CHEMBL510270 | — | EC50 | = | - | nM | - |
| CHEMBL525399 | — | EC50 | = | - | nM | - |