Assay Detail
Functional
CHEMBL853038
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 8.47 | 8.92 |
| Activity | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 2 | 8.92 |
| CHEMBL339053 | — | — | 2 | 8.92 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 2 | 8.54 |
| CHEMBL380691 | — | — | 2 | 8.02 |
| CHEMBL438596 | — | — | 2 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL339053 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL380691 | — | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL438596 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL441738 | AFAMELANOTIDE | Activity | = | 89.0 | % | - |
| CHEMBL380691 | — | Activity | = | 111.0 | % | - |
| CHEMBL339053 | — | Activity | = | 110.0 | % | - |
| CHEMBL438596 | — | Activity | = | 90.0 | % | - |
| CHEMBL214332 | INTERMEDINE | Activity | = | 100.0 | % | - |