Assay Detail
Functional
CHEMBL714608
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Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 10.23 | 10.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.77 |
| CHEMBL413212 | — | — | 1 | 10.74 |
| CHEMBL428615 | — | — | 1 | 10.72 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.68 |
| CHEMBL428801 | — | — | 1 | 9.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.017 | nM | 10.77 |
| CHEMBL413212 | — | EC50 | = | 0.018 | nM | 10.74 |
| CHEMBL428615 | — | EC50 | = | 0.019 | nM | 10.72 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.21 | nM | 9.68 |
| CHEMBL428801 | — | EC50 | = | 0.573 | nM | 9.24 |