Assay Detail
Functional
CHEMBL853046
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Agonist activity at the mutant MC4R I129A 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 | 7.27 | 8.96 |
| Activity | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 2 | 8.96 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 2 | 7.57 |
| CHEMBL339053 | — | — | 2 | 7.39 |
| CHEMBL438596 | — | — | 2 | 6.60 |
| CHEMBL380691 | — | — | 2 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL339053 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL438596 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL380691 | — | EC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL441738 | AFAMELANOTIDE | Activity | = | 77.0 | % | - |
| CHEMBL380691 | — | Activity | = | 87.0 | % | - |
| CHEMBL339053 | — | Activity | = | 79.0 | % | - |
| CHEMBL438596 | — | Activity | = | 62.0 | % | - |
| CHEMBL214332 | INTERMEDINE | Activity | = | 73.0 | % | - |