Assay Detail
Binding
CHEMBL1027396
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of europium-labeled NDP-alpha-MSH from human MC1R expressed in HEK293 cells
27
Total Activities
27
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
Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.10 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL506762 | — | — | 1 | 7.77 |
| CHEMBL443396 | — | — | 1 | 7.20 |
| CHEMBL448410 | — | — | 1 | 7.00 |
| CHEMBL504349 | — | — | 1 | 7.00 |
| CHEMBL447117 | — | — | 1 | 6.84 |
| CHEMBL453734 | — | — | 1 | 6.76 |
| CHEMBL446757 | — | — | 1 | 6.71 |
| CHEMBL450236 | — | — | 1 | 6.65 |
| CHEMBL452710 | — | — | 1 | 6.57 |
| CHEMBL442829 | — | — | 1 | 6.52 |
| CHEMBL506272 | — | — | 1 | 6.44 |
| CHEMBL463047 | — | — | 1 | 6.44 |
| CHEMBL448337 | — | — | 1 | 6.20 |
| CHEMBL449131 | — | — | 1 | 6.10 |
| CHEMBL449050 | — | — | 1 | 6.05 |
| CHEMBL507876 | — | — | 1 | 6.00 |
| CHEMBL213566 | — | — | 1 | 5.95 |
| CHEMBL466380 | — | — | 1 | 5.86 |
| CHEMBL453300 | — | — | 1 | 5.80 |
| CHEMBL451694 | — | — | 1 | 5.78 |
| CHEMBL445009 | — | — | 1 | 5.35 |
| CHEMBL214770 | — | — | 1 | 5.24 |
| CHEMBL460138 | — | — | 1 | 5.00 |
| CHEMBL460349 | — | — | 1 | 5.00 |
| CHEMBL460142 | — | — | 1 | 5.00 |
| CHEMBL468252 | — | — | 1 | 4.77 |
| CHEMBL517108 | — | — | 1 | 4.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL506762 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL443396 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL448410 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL504349 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL447117 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL453734 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL446757 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL450236 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL452710 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL442829 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL506272 | — | Ki | = | 361.0 | nM | 6.44 |
| CHEMBL463047 | — | Ki | = | 364.0 | nM | 6.44 |
| CHEMBL448337 | — | Ki | = | 637.0 | nM | 6.20 |
| CHEMBL449131 | — | Ki | = | 798.0 | nM | 6.10 |
| CHEMBL449050 | — | Ki | = | 889.0 | nM | 6.05 |
| CHEMBL507876 | — | Ki | = | 994.0 | nM | 6.00 |
| CHEMBL213566 | — | Ki | = | 1120.0 | nM | 5.95 |
| CHEMBL466380 | — | Ki | = | 1389.0 | nM | 5.86 |
| CHEMBL453300 | — | Ki | = | 1594.0 | nM | 5.80 |
| CHEMBL451694 | — | Ki | = | 1655.0 | nM | 5.78 |
| CHEMBL445009 | — | Ki | = | 4469.0 | nM | 5.35 |
| CHEMBL214770 | — | Ki | = | 5820.0 | nM | 5.24 |
| CHEMBL460138 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL460349 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL460142 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL468252 | — | Ki | = | 16832.0 | nM | 4.77 |
| CHEMBL517108 | — | Ki | = | 23400.0 | nM | 4.63 |