Assay Detail
Functional
CHEMBL871436
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Agonist activity at human MC3R 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 |
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 | 6.14 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL377465 | — | — | 1 | 8.89 |
| CHEMBL209622 | — | — | 1 | 8.00 |
| CHEMBL379508 | — | — | 1 | 7.82 |
| CHEMBL209789 | — | — | 1 | 7.38 |
| CHEMBL380051 | — | — | 1 | 7.17 |
| CHEMBL377620 | — | — | 1 | 7.07 |
| CHEMBL379168 | — | — | 1 | 6.67 |
| CHEMBL214347 | — | — | 1 | 6.63 |
| CHEMBL50056 | — | — | 1 | 6.61 |
| CHEMBL209587 | — | — | 1 | 6.58 |
| CHEMBL213956 | — | — | 1 | 6.58 |
| CHEMBL210011 | — | — | 1 | 6.54 |
| CHEMBL378446 | — | — | 1 | 6.50 |
| CHEMBL378293 | — | — | 1 | 6.47 |
| CHEMBL211699 | — | — | 1 | 6.27 |
| CHEMBL377779 | — | — | 1 | 6.25 |
| CHEMBL375440 | — | — | 1 | 6.23 |
| CHEMBL375775 | — | — | 1 | 6.08 |
| CHEMBL379879 | — | — | 1 | 6.06 |
| CHEMBL213747 | — | — | 1 | 5.95 |
| CHEMBL379490 | — | — | 1 | 5.93 |
| CHEMBL375559 | — | — | 1 | 5.91 |
| CHEMBL212766 | — | — | 1 | 5.86 |
| CHEMBL213751 | — | — | 1 | 5.83 |
| CHEMBL211798 | — | — | 1 | 5.75 |
| CHEMBL212976 | — | — | 1 | 5.69 |
| CHEMBL377778 | — | — | 1 | 5.61 |
| CHEMBL377210 | — | — | 1 | 5.53 |
| CHEMBL210008 | — | — | 1 | 5.50 |
| CHEMBL211419 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL377465 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL209622 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL379508 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL209789 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL380051 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL377620 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL379168 | — | EC50 | = | 214.0 | nM | 6.67 |
| CHEMBL214347 | — | EC50 | = | 232.0 | nM | 6.63 |
| CHEMBL50056 | — | EC50 | = | 248.0 | nM | 6.61 |
| CHEMBL213956 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL209587 | — | EC50 | = | 266.0 | nM | 6.58 |
| CHEMBL210011 | — | EC50 | = | 286.0 | nM | 6.54 |
| CHEMBL378446 | — | EC50 | = | 313.0 | nM | 6.50 |
| CHEMBL378293 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL211699 | — | EC50 | = | 541.0 | nM | 6.27 |
| CHEMBL377779 | — | EC50 | = | 563.0 | nM | 6.25 |
| CHEMBL375440 | — | EC50 | = | 593.0 | nM | 6.23 |
| CHEMBL375775 | — | EC50 | = | 825.0 | nM | 6.08 |
| CHEMBL379879 | — | EC50 | = | 871.0 | nM | 6.06 |
| CHEMBL213747 | — | EC50 | = | 1134.0 | nM | 5.95 |
| CHEMBL379490 | — | EC50 | = | 1171.0 | nM | 5.93 |
| CHEMBL375559 | — | EC50 | = | 1218.0 | nM | 5.91 |
| CHEMBL212766 | — | EC50 | = | 1384.0 | nM | 5.86 |
| CHEMBL213751 | — | EC50 | = | 1474.0 | nM | 5.83 |
| CHEMBL211798 | — | EC50 | = | 1774.0 | nM | 5.75 |
| CHEMBL212976 | — | EC50 | = | 2051.0 | nM | 5.69 |
| CHEMBL377778 | — | EC50 | = | 2474.0 | nM | 5.61 |
| CHEMBL377210 | — | EC50 | = | 2986.0 | nM | 5.53 |
| CHEMBL210008 | — | EC50 | = | 3152.0 | nM | 5.50 |
| CHEMBL211419 | — | EC50 | = | 3720.0 | nM | 5.43 |
| CHEMBL387246 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL213026 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL213752 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL378571 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL202699 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL210009 | — | EC50 | = | 20000.0 | nM | 4.70 |