Assay Detail
Functional
CHEMBL717667
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
30
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 5.73 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 10.70 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.42 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.26 |
| CHEMBL264190 | — | — | 1 | 7.70 |
| CHEMBL319871 | — | — | 1 | 7.55 |
| CHEMBL322610 | — | — | 1 | 7.22 |
| CHEMBL103817 | — | — | 1 | 6.78 |
| CHEMBL321870 | — | — | 1 | 6.45 |
| CHEMBL106959 | — | — | 1 | 5.82 |
| CHEMBL102688 | — | — | 2 | 5.63 |
| CHEMBL105113 | — | — | 1 | 5.50 |
| CHEMBL430843 | — | — | 1 | 5.20 |
| CHEMBL50056 | — | — | 1 | 5.11 |
| CHEMBL421028 | — | — | 1 | 4.97 |
| CHEMBL317228 | — | — | 1 | 4.83 |
| CHEMBL319922 | — | — | 1 | 4.82 |
| CHEMBL318119 | — | — | 1 | 4.77 |
| CHEMBL432018 | — | — | 1 | 4.72 |
| CHEMBL104397 | — | — | 1 | 4.66 |
| CHEMBL104052 | — | — | 1 | 4.64 |
| CHEMBL322889 | — | — | 1 | 4.60 |
| CHEMBL317210 | — | — | 1 | 4.52 |
| CHEMBL431242 | — | — | 1 | 4.48 |
| CHEMBL102391 | — | — | 1 | 4.48 |
| CHEMBL430489 | — | — | 1 | 4.43 |
| CHEMBL607103 | — | — | 1 | 4.39 |
| CHEMBL104010 | — | — | 1 | 4.38 |
| CHEMBL607104 | — | — | 1 | 4.27 |
| CHEMBL104880 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.038 | nM | 10.42 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.55 | nM | 9.26 |
| CHEMBL264190 | — | EC50 | = | 20.1 | nM | 7.70 |
| CHEMBL319871 | — | EC50 | = | 28.4 | nM | 7.55 |
| CHEMBL322610 | — | EC50 | = | 60.4 | nM | 7.22 |
| CHEMBL103817 | — | EC50 | = | 167.0 | nM | 6.78 |
| CHEMBL321870 | — | EC50 | = | 356.0 | nM | 6.45 |
| CHEMBL106959 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL102688 | — | EC50 | = | 2350.0 | nM | 5.63 |
| CHEMBL105113 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL102688 | — | EC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL430843 | — | EC50 | = | 6250.0 | nM | 5.20 |
| CHEMBL50056 | — | EC50 | = | 7690.0 | nM | 5.11 |
| CHEMBL421028 | — | EC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL317228 | — | EC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL319922 | — | EC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL318119 | — | EC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL432018 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL104397 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL104052 | — | EC50 | = | 22900.0 | nM | 4.64 |
| CHEMBL322889 | — | EC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL317210 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL431242 | — | EC50 | = | 33400.0 | nM | 4.48 |
| CHEMBL102391 | — | EC50 | = | 33100.0 | nM | 4.48 |
| CHEMBL430489 | — | EC50 | = | 36700.0 | nM | 4.43 |
| CHEMBL607103 | — | EC50 | = | 40800.0 | nM | 4.39 |
| CHEMBL104010 | — | EC50 | = | 41700.0 | nM | 4.38 |
| CHEMBL607104 | — | EC50 | = | 53600.0 | nM | 4.27 |
| CHEMBL104880 | — | EC50 | = | 61400.0 | nM | 4.21 |