Assay Detail
Binding
CHEMBL1027398
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of europium-labeled NDP-alpha-MSH from human MC4R 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 |
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 | 7.68 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL443396 | — | — | 1 | 8.85 |
| CHEMBL506272 | — | — | 1 | 8.40 |
| CHEMBL449131 | — | — | 1 | 8.40 |
| CHEMBL452710 | — | — | 1 | 8.30 |
| CHEMBL448410 | — | — | 1 | 8.30 |
| CHEMBL506762 | — | — | 1 | 8.28 |
| CHEMBL446757 | — | — | 1 | 8.26 |
| CHEMBL463047 | — | — | 1 | 8.22 |
| CHEMBL504349 | — | — | 1 | 8.22 |
| CHEMBL466380 | — | — | 1 | 8.10 |
| CHEMBL453734 | — | — | 1 | 8.05 |
| CHEMBL213566 | — | — | 1 | 7.96 |
| CHEMBL447117 | — | — | 1 | 7.96 |
| CHEMBL442829 | — | — | 1 | 7.92 |
| CHEMBL450236 | — | — | 1 | 7.85 |
| CHEMBL449050 | — | — | 1 | 7.85 |
| CHEMBL507876 | — | — | 1 | 7.72 |
| CHEMBL451694 | — | — | 1 | 7.58 |
| CHEMBL448337 | — | — | 1 | 7.46 |
| CHEMBL453300 | — | — | 1 | 7.44 |
| CHEMBL460138 | — | — | 1 | 7.12 |
| CHEMBL517108 | — | — | 1 | 7.01 |
| CHEMBL460349 | — | — | 1 | 6.75 |
| CHEMBL214770 | — | — | 1 | 6.72 |
| CHEMBL445009 | — | — | 1 | 6.25 |
| CHEMBL468252 | — | — | 1 | 6.21 |
| CHEMBL460142 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL443396 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL506272 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL449131 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL452710 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL448410 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL506762 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL446757 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL463047 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL504349 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL466380 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL453734 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL213566 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL447117 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL442829 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL450236 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL449050 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL507876 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL451694 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL448337 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL453300 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL460138 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL517108 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL460349 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL214770 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL445009 | — | Ki | = | 556.0 | nM | 6.25 |
| CHEMBL468252 | — | Ki | = | 624.0 | nM | 6.21 |
| CHEMBL460142 | — | Ki | = | 714.0 | nM | 6.15 |