Assay Detail
Binding
CHEMBL828399
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Inhibition of [125I]NDP-MSH binding to Melanocortin 1 receptor expressed in HEK293 cells; (N = 4)
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.61 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL414778 | — | — | 1 | 9.80 |
| CHEMBL413439 | — | — | 1 | 9.52 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.40 |
| CHEMBL443071 | — | — | 1 | 9.30 |
| CHEMBL438920 | — | — | 1 | 9.15 |
| CHEMBL2096759 | — | — | 1 | 9.00 |
| CHEMBL437050 | — | — | 2 | 8.92 |
| CHEMBL2371712 | — | — | 1 | 8.70 |
| CHEMBL2310901 | — | — | 1 | 7.70 |
| CHEMBL411359 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL414778 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL413439 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL214332 | INTERMEDINE | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL443071 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL438920 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2096759 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL437050 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2371712 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2310901 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL411359 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL437050 | — | IC50 | = | 1000.0 | nM | 6.00 |