Assay Detail
Binding
CHEMBL853374
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
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 |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.75 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL379508 | — | — | 1 | 9.19 |
| CHEMBL377465 | — | — | 1 | 8.89 |
| CHEMBL211419 | — | — | 1 | 8.33 |
| CHEMBL211699 | — | — | 1 | 7.89 |
| CHEMBL378293 | — | — | 1 | 7.89 |
| CHEMBL209587 | — | — | 1 | 7.82 |
| CHEMBL213751 | — | — | 1 | 7.72 |
| CHEMBL50056 | — | — | 1 | 7.46 |
| CHEMBL209789 | — | — | 1 | 7.46 |
| CHEMBL213956 | — | — | 1 | 7.40 |
| CHEMBL214347 | — | — | 1 | 7.38 |
| CHEMBL375440 | — | — | 1 | 7.26 |
| CHEMBL377620 | — | — | 1 | 7.07 |
| CHEMBL209622 | — | — | 1 | 6.99 |
| CHEMBL377778 | — | — | 1 | 6.92 |
| CHEMBL210011 | — | — | 1 | 6.90 |
| CHEMBL380051 | — | — | 1 | 6.86 |
| CHEMBL378446 | — | — | 1 | 6.74 |
| CHEMBL213752 | — | — | 1 | 6.47 |
| CHEMBL379879 | — | — | 1 | 6.42 |
| CHEMBL378571 | — | — | 1 | 6.35 |
| CHEMBL212766 | — | — | 1 | 6.33 |
| CHEMBL379168 | — | — | 1 | 6.25 |
| CHEMBL212976 | — | — | 1 | 6.21 |
| CHEMBL211798 | — | — | 1 | 6.20 |
| CHEMBL377779 | — | — | 1 | 6.05 |
| CHEMBL210008 | — | — | 1 | 5.85 |
| CHEMBL377210 | — | — | 1 | 5.80 |
| CHEMBL375775 | — | — | 1 | 5.79 |
| CHEMBL213026 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL379508 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL377465 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL211419 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL211699 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL378293 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL209587 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL213751 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL50056 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL209789 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL213956 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL214347 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL375440 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL377620 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL209622 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL377778 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL210011 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL380051 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL378446 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL213752 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL379879 | — | Ki | = | 381.0 | nM | 6.42 |
| CHEMBL378571 | — | Ki | = | 443.0 | nM | 6.35 |
| CHEMBL212766 | — | Ki | = | 463.0 | nM | 6.33 |
| CHEMBL379168 | — | Ki | = | 562.0 | nM | 6.25 |
| CHEMBL212976 | — | Ki | = | 611.0 | nM | 6.21 |
| CHEMBL211798 | — | Ki | = | 631.0 | nM | 6.20 |
| CHEMBL377779 | — | Ki | = | 893.0 | nM | 6.05 |
| CHEMBL210008 | — | Ki | = | 1403.0 | nM | 5.85 |
| CHEMBL377210 | — | Ki | = | 1572.0 | nM | 5.80 |
| CHEMBL375775 | — | Ki | = | 1615.0 | nM | 5.79 |
| CHEMBL213026 | — | Ki | = | 1687.0 | nM | 5.77 |
| CHEMBL210009 | — | Ki | = | 1793.0 | nM | 5.75 |
| CHEMBL375559 | — | Ki | = | 2047.0 | nM | 5.69 |
| CHEMBL379490 | — | Ki | = | 2454.0 | nM | 5.61 |
| CHEMBL213747 | — | Ki | = | 2968.0 | nM | 5.53 |
| CHEMBL387246 | — | Ki | = | 4384.0 | nM | 5.36 |
| CHEMBL202699 | — | Ki | = | 4520.0 | nM | 5.34 |