Assay Detail
Binding
CHEMBL716494
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Inhibitory concentration against human Melanocortin 1 receptor (hMC1R)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.57 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 9.60 |
| CHEMBL2115441 | — | — | 1 | 9.46 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.29 |
| CHEMBL3350396 | — | — | 1 | 9.04 |
| CHEMBL410217 | — | — | 1 | 8.71 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 8.22 |
| CHEMBL217584 | — | — | 1 | 7.65 |
| CHEMBL413260 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL2115441 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL441738 | AFAMELANOTIDE | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL3350396 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL410217 | — | IC50 | = | 1.94 | nM | 8.71 |
| CHEMBL214332 | INTERMEDINE | IC50 | = | 5.97 | nM | 8.22 |
| CHEMBL217584 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL413260 | — | IC50 | = | 264.0 | nM | 6.58 |