Assay Detail
Binding
CHEMBL827545
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Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
15
Total Activities
14
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 |
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 | 15 | 7.72 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL443071 | — | — | 1 | 8.70 |
| CHEMBL2371712 | — | — | 1 | 8.52 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 8.48 |
| CHEMBL413439 | — | — | 1 | 8.30 |
| CHEMBL414778 | — | — | 1 | 8.22 |
| CHEMBL438920 | — | — | 1 | 8.22 |
| CHEMBL405282 | — | — | 1 | 8.17 |
| CHEMBL2096759 | — | — | 1 | 7.60 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 7.52 |
| CHEMBL2310901 | — | — | 1 | 7.50 |
| CHEMBL437050 | — | — | 2 | 7.40 |
| CHEMBL439691 | — | — | 1 | 7.35 |
| CHEMBL411359 | — | — | 1 | 7.21 |
| CHEMBL408509 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL443071 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2371712 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL441738 | AFAMELANOTIDE | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL413439 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL414778 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL438920 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL405282 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL2096759 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL214332 | INTERMEDINE | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2310901 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL437050 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL439691 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL411359 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL437050 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL408509 | — | IC50 | = | 3000.0 | nM | 5.52 |