Assay Detail
Functional
CHEMBL915320
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Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
7
Total Activities
7
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 |
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 | 7 | 6.87 | 10.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.07 |
| CHEMBL430239 | MELATONAN | — | 1 | 9.77 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 9.28 |
| CHEMBL2304248 | — | — | 1 | 5.26 |
| CHEMBL3350327 | — | — | 1 | 4.86 |
| CHEMBL2369131 | — | — | 1 | 4.65 |
| CHEMBL2448525 | — | — | 1 | 4.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.085 | nM | 10.07 |
| CHEMBL430239 | MELATONAN | EC50 | = | 0.17 | nM | 9.77 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.52 | nM | 9.28 |
| CHEMBL2304248 | — | EC50 | = | 5510.0 | nM | 5.26 |
| CHEMBL3350327 | — | EC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL2369131 | — | EC50 | = | 22600.0 | nM | 4.65 |
| CHEMBL2448525 | — | EC50 | = | 63300.0 | nM | 4.20 |