Assay Detail
Binding
CHEMBL972322
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 1 receptor expressed in HEK293 cells
11
Total Activities
11
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 |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 11 | 6.83 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL504986 | — | — | 1 | 8.43 |
| CHEMBL506274 | — | — | 1 | 6.75 |
| CHEMBL448081 | — | — | 1 | 6.12 |
| CHEMBL508068 | — | — | 1 | 6.00 |
| CHEMBL449124 | — | — | 1 | - |
| CHEMBL499491 | — | — | 1 | - |
| CHEMBL451535 | — | — | 1 | - |
| CHEMBL508816 | — | — | 1 | - |
| CHEMBL552520 | — | — | 1 | - |
| CHEMBL553202 | — | — | 1 | - |
| CHEMBL510234 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL504986 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL506274 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL448081 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL508068 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL449124 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL499491 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL451535 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL508816 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL552520 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL553202 | — | IC50 | > | 1500.0 | nM | - |
| CHEMBL510234 | — | IC50 | > | 2000.0 | nM | - |