Assay Detail
Functional
CHEMBL4344899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP AlphaScreen assay
15
Total Activities
15
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
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.46 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 10.40 |
| CHEMBL264190 | — | — | 1 | 7.80 |
| CHEMBL4437801 | — | — | 1 | 7.05 |
| CHEMBL4574756 | — | — | 1 | 6.40 |
| CHEMBL4582657 | — | — | 1 | 6.05 |
| CHEMBL3287060 | — | — | 1 | 5.92 |
| CHEMBL4465466 | — | — | 1 | 5.89 |
| CHEMBL4554278 | — | — | 1 | 5.89 |
| CHEMBL4590532 | — | — | 1 | 5.80 |
| CHEMBL4513953 | — | — | 1 | 5.80 |
| CHEMBL4590028 | — | — | 1 | 5.80 |
| CHEMBL320157 | — | — | 1 | 5.68 |
| CHEMBL50056 | — | — | 1 | 5.52 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | - |
| CHEMBL4558851 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214332 | INTERMEDINE | EC50 | = | 0.04 | nM | 10.40 |
| CHEMBL264190 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4437801 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4574756 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4582657 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3287060 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4465466 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4554278 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4590532 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4513953 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4590028 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL320157 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL50056 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.012 | nM | - |
| CHEMBL4558851 | — | EC50 | > | 100000.0 | nM | - |