Assay Detail
Binding
CHEMBL853033
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 7 | 7.91 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.20 |
| CHEMBL267492 | — | — | 1 | 9.15 |
| CHEMBL339053 | — | — | 1 | 8.49 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 8.03 |
| CHEMBL438596 | — | — | 1 | 7.54 |
| CHEMBL380691 | — | — | 1 | 6.94 |
| CHEMBL40711 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL267492 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL339053 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL214332 | INTERMEDINE | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL438596 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL380691 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL40711 | — | Ki | = | 890.0 | nM | 6.05 |