Assay Detail
Binding
CHEMBL4032175
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Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by gamma counting method
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design of MC1R Selective γ-MSH Analogues with Canonical Amino Acids Leads to Potency and Pigmentation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.27 | 11.00 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4093140 | — | — | 1 | 11.00 |
| CHEMBL2370964 | — | — | 1 | 9.52 |
| CHEMBL4072387 | — | — | 1 | 9.40 |
| CHEMBL503229 | — | — | 1 | 9.30 |
| CHEMBL4081900 | — | — | 1 | 8.96 |
| CHEMBL4104092 | — | — | 1 | 8.92 |
| CHEMBL4060000 | — | — | 1 | 7.80 |
| CHEMBL4089770 | — | — | 1 | 7.64 |
| CHEMBL4088516 | — | — | 1 | 7.62 |
| CHEMBL4090684 | — | — | 1 | 7.38 |
| CHEMBL4079302 | — | — | 1 | 7.09 |
| CHEMBL4068475 | — | — | 1 | 6.86 |
| CHEMBL437050 | — | — | 1 | 6.00 |
| CHEMBL4103570 | — | — | 1 | - |
| CHEMBL4068654 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4093140 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL2370964 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4072387 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL503229 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4081900 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4104092 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4060000 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4089770 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4088516 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4090684 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4079302 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4068475 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL437050 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4103570 | — | Inhibition | = | - | % | - |
| CHEMBL4068654 | — | IC50 | > | 1000.0 | nM | - |