Assay Detail
Functional
CHEMBL678735
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Decrease in frog skin reflectivity (metabotropic activity).
19
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | frog |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 9.12 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2114259 | — | — | 1 | 10.70 |
| CHEMBL3350329 | — | — | 2 | 10.22 |
| CHEMBL430239 | MELATONAN | — | 3 | 10.00 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 10.00 |
| CHEMBL3350299 | — | — | 2 | 9.70 |
| CHEMBL2115248 | — | — | 1 | 9.70 |
| CHEMBL2115249 | — | — | 1 | 9.36 |
| CHEMBL319752 | — | — | 1 | 9.00 |
| CHEMBL2114258 | — | — | 1 | 8.70 |
| CHEMBL320459 | — | — | 1 | 8.48 |
| CHEMBL3350298 | — | — | 2 | 8.20 |
| CHEMBL2115246 | — | — | 1 | 8.20 |
| CHEMBL2364550 | — | — | 1 | 7.54 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2114259 | — | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL3350329 | — | EC50 | = | 0.06 | nM | 10.22 |
| CHEMBL430239 | MELATONAN | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL430239 | MELATONAN | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3350299 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL2115248 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3350329 | — | EC50 | = | 0.33 | nM | 9.48 |
| CHEMBL2115249 | — | EC50 | = | 0.44 | nM | 9.36 |
| CHEMBL319752 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2114258 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL320459 | — | EC50 | = | 3.33 | nM | 8.48 |
| CHEMBL3350298 | — | EC50 | = | 6.25 | nM | 8.20 |
| CHEMBL2115246 | — | EC50 | = | 6.25 | nM | 8.20 |
| CHEMBL430239 | MELATONAN | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3350298 | — | EC50 | = | 16.67 | nM | 7.78 |
| CHEMBL2364550 | — | EC50 | = | 28.6 | nM | 7.54 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.005 | nM | - |
| CHEMBL3350299 | — | EC50 | = | 0.005 | nM | - |