Assay Detail
Functional
CHEMBL716486
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Evaluated for agonist activity at cloned mammalian human MSH1 receptor
6
Total Activities
6
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 (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6 | 10.44 | 10.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL428615 | — | — | 1 | 10.80 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.64 |
| CHEMBL266417 | — | — | 1 | 10.44 |
| CHEMBL428801 | — | — | 1 | 10.26 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 10.04 |
| CHEMBL413212 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL428615 | — | EC50 | = | 0.016 | nM | 10.80 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.023 | nM | 10.64 |
| CHEMBL266417 | — | EC50 | = | 0.036 | nM | 10.44 |
| CHEMBL428801 | — | EC50 | = | 0.055 | nM | 10.26 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.091 | nM | 10.04 |
| CHEMBL413212 | — | EC50 | = | 0.005 | nM | - |