Assay Detail
Functional
CHEMBL3297366
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
9
Total Activities
9
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 | Autocuration |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 8.21 | 10.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.06 |
| CHEMBL3287324 | — | — | 1 | 8.57 |
| CHEMBL3287322 | — | — | 1 | 8.54 |
| CHEMBL3287326 | — | — | 1 | 8.40 |
| CHEMBL3287323 | — | — | 1 | 7.92 |
| CHEMBL3287327 | — | — | 1 | 7.72 |
| CHEMBL3287328 | — | — | 1 | 7.66 |
| CHEMBL3287329 | — | — | 1 | 7.62 |
| CHEMBL3287325 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.088 | nM | 10.06 |
| CHEMBL3287324 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3287322 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3287326 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3287323 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3287327 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3287328 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3287329 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3287325 | — | EC50 | = | 40.0 | nM | 7.40 |