Assay Detail
Binding
CHEMBL871434
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
36
Total Activities
36
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 | Expert |
Publication
Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally restricted dipeptide mimic approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 6.57 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214347 | — | — | 1 | 8.00 |
| CHEMBL213747 | — | — | 1 | 7.85 |
| CHEMBL379508 | — | — | 1 | 7.77 |
| CHEMBL209789 | — | — | 1 | 7.75 |
| CHEMBL377620 | — | — | 1 | 7.68 |
| CHEMBL211699 | — | — | 1 | 7.54 |
| CHEMBL213956 | — | — | 1 | 7.51 |
| CHEMBL375440 | — | — | 1 | 7.34 |
| CHEMBL377465 | — | — | 1 | 7.24 |
| CHEMBL378446 | — | — | 1 | 7.23 |
| CHEMBL212766 | — | — | 1 | 7.05 |
| CHEMBL379168 | — | — | 1 | 7.01 |
| CHEMBL202699 | — | — | 1 | 6.98 |
| CHEMBL210011 | — | — | 1 | 6.92 |
| CHEMBL212976 | — | — | 1 | 6.86 |
| CHEMBL209622 | — | — | 1 | 6.73 |
| CHEMBL50056 | — | — | 1 | 6.61 |
| CHEMBL380051 | — | — | 1 | 6.61 |
| CHEMBL379879 | — | — | 1 | 6.52 |
| CHEMBL375775 | — | — | 1 | 6.39 |
| CHEMBL379490 | — | — | 1 | 6.31 |
| CHEMBL375559 | — | — | 1 | 6.25 |
| CHEMBL377779 | — | — | 1 | 6.20 |
| CHEMBL210008 | — | — | 1 | 6.17 |
| CHEMBL209587 | — | — | 1 | 6.12 |
| CHEMBL377778 | — | — | 1 | 5.99 |
| CHEMBL387246 | — | — | 1 | 5.90 |
| CHEMBL211798 | — | — | 1 | 5.86 |
| CHEMBL378293 | — | — | 1 | 5.80 |
| CHEMBL213752 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214347 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL213747 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL379508 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL209789 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL377620 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL211699 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL213956 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL375440 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL377465 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL378446 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL212766 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL379168 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL202699 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL210011 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL212976 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL209622 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL50056 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL380051 | — | Ki | = | 248.0 | nM | 6.61 |
| CHEMBL379879 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL375775 | — | Ki | = | 411.0 | nM | 6.39 |
| CHEMBL379490 | — | Ki | = | 492.0 | nM | 6.31 |
| CHEMBL375559 | — | Ki | = | 559.0 | nM | 6.25 |
| CHEMBL377779 | — | Ki | = | 632.0 | nM | 6.20 |
| CHEMBL210008 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL209587 | — | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL377778 | — | Ki | = | 1016.0 | nM | 5.99 |
| CHEMBL387246 | — | Ki | = | 1248.0 | nM | 5.90 |
| CHEMBL211798 | — | Ki | = | 1376.0 | nM | 5.86 |
| CHEMBL378293 | — | Ki | = | 1578.0 | nM | 5.80 |
| CHEMBL213752 | — | Ki | = | 1712.0 | nM | 5.77 |
| CHEMBL210009 | — | Ki | = | 2258.0 | nM | 5.65 |
| CHEMBL213026 | — | Ki | = | 2353.0 | nM | 5.63 |
| CHEMBL211419 | — | Ki | = | 2879.0 | nM | 5.54 |
| CHEMBL213751 | — | Ki | = | 4390.0 | nM | 5.36 |
| CHEMBL378571 | — | Ki | = | 6666.0 | nM | 5.18 |
| CHEMBL377210 | — | Ki | = | 8158.0 | nM | 5.09 |