Assay Detail
Binding
CHEMBL1027397
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Displacement of europium-labeled NDP-alpha-MSH from human MC3R 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 | 6.34 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL443396 | — | — | 1 | 7.12 |
| CHEMBL446757 | — | — | 1 | 7.10 |
| CHEMBL506762 | — | — | 1 | 6.90 |
| CHEMBL506272 | — | — | 1 | 6.89 |
| CHEMBL463047 | — | — | 1 | 6.84 |
| CHEMBL448410 | — | — | 1 | 6.81 |
| CHEMBL442829 | — | — | 1 | 6.78 |
| CHEMBL449050 | — | — | 1 | 6.77 |
| CHEMBL466380 | — | — | 1 | 6.70 |
| CHEMBL504349 | — | — | 1 | 6.68 |
| CHEMBL448337 | — | — | 1 | 6.67 |
| CHEMBL452710 | — | — | 1 | 6.55 |
| CHEMBL449131 | — | — | 1 | 6.51 |
| CHEMBL453734 | — | — | 1 | 6.49 |
| CHEMBL447117 | — | — | 1 | 6.42 |
| CHEMBL453300 | — | — | 1 | 6.37 |
| CHEMBL451694 | — | — | 1 | 6.36 |
| CHEMBL213566 | — | — | 1 | 6.33 |
| CHEMBL450236 | — | — | 1 | 6.33 |
| CHEMBL460138 | — | — | 1 | 6.14 |
| CHEMBL507876 | — | — | 1 | 6.08 |
| CHEMBL460349 | — | — | 1 | 6.02 |
| CHEMBL460142 | — | — | 1 | 5.73 |
| CHEMBL517108 | — | — | 1 | 5.55 |
| CHEMBL214770 | — | — | 1 | 5.38 |
| CHEMBL445009 | — | — | 1 | 5.06 |
| CHEMBL468252 | — | — | 1 | 4.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL443396 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL446757 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL506762 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL506272 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL463047 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL448410 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL442829 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL449050 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL466380 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL504349 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL448337 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL452710 | — | Ki | = | 282.0 | nM | 6.55 |
| CHEMBL449131 | — | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL453734 | — | Ki | = | 322.0 | nM | 6.49 |
| CHEMBL447117 | — | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL453300 | — | Ki | = | 428.0 | nM | 6.37 |
| CHEMBL451694 | — | Ki | = | 434.0 | nM | 6.36 |
| CHEMBL213566 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL450236 | — | Ki | = | 471.0 | nM | 6.33 |
| CHEMBL460138 | — | Ki | = | 727.0 | nM | 6.14 |
| CHEMBL507876 | — | Ki | = | 827.0 | nM | 6.08 |
| CHEMBL460349 | — | Ki | = | 947.0 | nM | 6.02 |
| CHEMBL460142 | — | Ki | = | 1862.0 | nM | 5.73 |
| CHEMBL517108 | — | Ki | = | 2832.0 | nM | 5.55 |
| CHEMBL214770 | — | Ki | = | 4122.0 | nM | 5.38 |
| CHEMBL445009 | — | Ki | = | 8734.0 | nM | 5.06 |
| CHEMBL468252 | — | Ki | = | 26323.0 | nM | 4.58 |