Assay Detail
Functional
CHEMBL871435
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MC1R transfected in HEK293 cells
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 36 | 6.95 | 10.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL377465 | — | — | 1 | 10.35 |
| CHEMBL379508 | — | — | 1 | 9.52 |
| CHEMBL378293 | — | — | 1 | 8.52 |
| CHEMBL209622 | — | — | 1 | 8.37 |
| CHEMBL211419 | — | — | 1 | 8.10 |
| CHEMBL50056 | — | — | 1 | 7.85 |
| CHEMBL211699 | — | — | 1 | 7.85 |
| CHEMBL213751 | — | — | 1 | 7.72 |
| CHEMBL209587 | — | — | 1 | 7.62 |
| CHEMBL210011 | — | — | 1 | 7.55 |
| CHEMBL213956 | — | — | 1 | 7.52 |
| CHEMBL209789 | — | — | 1 | 7.35 |
| CHEMBL375440 | — | — | 1 | 7.28 |
| CHEMBL380051 | — | — | 1 | 7.15 |
| CHEMBL379168 | — | — | 1 | 7.14 |
| CHEMBL377620 | — | — | 1 | 7.06 |
| CHEMBL214347 | — | — | 1 | 7.01 |
| CHEMBL377778 | — | — | 1 | 6.98 |
| CHEMBL379879 | — | — | 1 | 6.82 |
| CHEMBL378446 | — | — | 1 | 6.70 |
| CHEMBL212766 | — | — | 1 | 6.63 |
| CHEMBL377779 | — | — | 1 | 6.48 |
| CHEMBL211798 | — | — | 1 | 6.41 |
| CHEMBL378571 | — | — | 1 | 6.40 |
| CHEMBL213752 | — | — | 1 | 6.35 |
| CHEMBL377210 | — | — | 1 | 6.28 |
| CHEMBL375775 | — | — | 1 | 6.27 |
| CHEMBL212976 | — | — | 1 | 6.23 |
| CHEMBL210009 | — | — | 1 | 5.97 |
| CHEMBL213747 | — | — | 1 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL377465 | — | EC50 | = | 0.045 | nM | 10.35 |
| CHEMBL379508 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL378293 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL209622 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL211419 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL50056 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL211699 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL213751 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL209587 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL210011 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL213956 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL209789 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL375440 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL380051 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL379168 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL377620 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL214347 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL377778 | — | EC50 | = | 104.0 | nM | 6.98 |
| CHEMBL379879 | — | EC50 | = | 151.0 | nM | 6.82 |
| CHEMBL378446 | — | EC50 | = | 201.0 | nM | 6.70 |
| CHEMBL212766 | — | EC50 | = | 232.0 | nM | 6.63 |
| CHEMBL377779 | — | EC50 | = | 328.0 | nM | 6.48 |
| CHEMBL211798 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL378571 | — | EC50 | = | 402.0 | nM | 6.40 |
| CHEMBL213752 | — | EC50 | = | 449.0 | nM | 6.35 |
| CHEMBL377210 | — | EC50 | = | 521.0 | nM | 6.28 |
| CHEMBL375775 | — | EC50 | = | 539.0 | nM | 6.27 |
| CHEMBL212976 | — | EC50 | = | 585.0 | nM | 6.23 |
| CHEMBL210009 | — | EC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL213747 | — | EC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL375559 | — | EC50 | = | 1337.0 | nM | 5.87 |
| CHEMBL210008 | — | EC50 | = | 1362.0 | nM | 5.87 |
| CHEMBL213026 | — | EC50 | = | 1751.0 | nM | 5.76 |
| CHEMBL379490 | — | EC50 | = | 1815.0 | nM | 5.74 |
| CHEMBL202699 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL387246 | — | EC50 | = | 20000.0 | nM | 4.70 |