Assay Detail
Functional
CHEMBL915319
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.25 | 10.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 10.68 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.64 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.55 |
| CHEMBL2448525 | — | — | 1 | 7.19 |
| CHEMBL2304247 | — | — | 1 | 7.03 |
| CHEMBL3350327 | — | — | 2 | 6.92 |
| CHEMBL2304248 | — | — | 1 | 5.76 |
| CHEMBL2369131 | — | — | 1 | 5.43 |
| CHEMBL2304246 | — | — | 1 | 5.28 |
| CHEMBL2304250 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | EC50 | = | 0.021 | nM | 10.68 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.023 | nM | 10.64 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.28 | nM | 9.55 |
| CHEMBL2448525 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2304247 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3350327 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3350327 | — | EC50 | = | 960.0 | nM | 6.02 |
| CHEMBL2304248 | — | EC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL2369131 | — | EC50 | = | 3750.0 | nM | 5.43 |
| CHEMBL2304246 | — | EC50 | = | 5270.0 | nM | 5.28 |
| CHEMBL2304250 | — | EC50 | = | 6330.0 | nM | 5.20 |