Assay Detail
Functional
CHEMBL717328
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Evaluated for agonist activity against mouse Melanocortin 1 receptor using mMC1R assay
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 |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 9.90 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL428615 | — | — | 1 | 10.59 |
| CHEMBL266417 | — | — | 1 | 10.41 |
| CHEMBL428801 | — | — | 1 | 9.72 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 8.89 |
| CHEMBL413212 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL428615 | — | EC50 | = | 0.026 | nM | 10.59 |
| CHEMBL266417 | — | EC50 | = | 0.039 | nM | 10.41 |
| CHEMBL428801 | — | EC50 | = | 0.19 | nM | 9.72 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL413212 | — | EC50 | = | 0.0095 | nM | - |