Assay Detail
ADMET
CHEMBL4032183
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Displacement of [125I]-NDP-alpha-MSH from human MC4R 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 | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 13 | 7.73 | 9.40 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4093140 | — | — | 1 | 9.40 |
| CHEMBL503229 | — | — | 1 | 8.92 |
| CHEMBL4079302 | — | — | 1 | 8.30 |
| CHEMBL4072387 | — | — | 1 | 8.30 |
| CHEMBL2370964 | — | — | 1 | 8.22 |
| CHEMBL4081900 | — | — | 1 | 8.17 |
| CHEMBL4089770 | — | — | 1 | 7.70 |
| CHEMBL4104092 | — | — | 1 | 7.35 |
| CHEMBL4090684 | — | — | 1 | 7.17 |
| CHEMBL4088516 | — | — | 1 | 6.68 |
| CHEMBL4068654 | — | — | 1 | 6.44 |
| CHEMBL437050 | — | — | 1 | 6.12 |
| CHEMBL4103570 | — | — | 1 | - |
| CHEMBL4068475 | — | — | 1 | - |
| CHEMBL4060000 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4093140 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL503229 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4079302 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4072387 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2370964 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4081900 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4089770 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4104092 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4090684 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4088516 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4068654 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL437050 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4103570 | — | Inhibition | = | - | % | - |
| CHEMBL4068475 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4060000 | — | Inhibition | = | - | % | - |