Assay Detail
Binding
CHEMBL972327
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Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
10
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 | Autocuration |
Publication
Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: discovery of potent and selective hMC5R receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.69 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL504986 | — | — | 1 | 7.40 |
| CHEMBL448081 | — | — | 1 | 6.72 |
| CHEMBL552520 | — | — | 1 | 6.42 |
| CHEMBL506274 | — | — | 1 | 6.21 |
| CHEMBL510234 | — | — | 1 | - |
| CHEMBL504964 | — | — | 1 | - |
| CHEMBL505536 | — | — | 1 | - |
| CHEMBL501158 | — | — | 1 | - |
| CHEMBL508816 | — | — | 1 | - |
| CHEMBL451535 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL504986 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL448081 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL552520 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL506274 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL510234 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL504964 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL505536 | — | IC50 | > | 8000.0 | nM | - |
| CHEMBL501158 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL508816 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL451535 | — | IC50 | > | 1000.0 | nM | - |