Assay Detail
Binding
CHEMBL5107058
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK2936E |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 7.11 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175981 | — | — | 1 | 9.04 |
| CHEMBL430239 | MELATONAN | — | 1 | 8.90 |
| CHEMBL3301624 | SETMELANOTIDE | 4.0 | 1 | 8.37 |
| CHEMBL5185945 | — | — | 1 | 7.70 |
| CHEMBL2070241 | BREMELANOTIDE | 4.0 | 1 | 7.70 |
| CHEMBL5203986 | — | — | 1 | 7.65 |
| CHEMBL5181812 | — | — | 1 | 7.51 |
| CHEMBL5185775 | — | — | 1 | 7.51 |
| CHEMBL5176443 | — | — | 1 | 7.48 |
| CHEMBL5192329 | — | — | 1 | 7.48 |
| CHEMBL5191309 | — | — | 1 | 7.47 |
| CHEMBL5175487 | — | — | 1 | 7.45 |
| CHEMBL5190042 | — | — | 1 | 7.36 |
| CHEMBL5170533 | — | — | 1 | 7.35 |
| CHEMBL5178164 | — | — | 1 | 7.34 |
| CHEMBL5172738 | — | — | 1 | 7.21 |
| CHEMBL5195641 | — | — | 1 | 7.09 |
| CHEMBL5185405 | — | — | 1 | 7.09 |
| CHEMBL5204285 | — | — | 1 | 7.04 |
| CHEMBL5207936 | — | — | 1 | 6.78 |
| CHEMBL5179373 | — | — | 1 | 6.77 |
| CHEMBL5179081 | — | — | 1 | 6.58 |
| CHEMBL5182345 | — | — | 1 | 6.53 |
| CHEMBL5187932 | — | — | 1 | 6.52 |
| CHEMBL5199932 | — | — | 1 | 6.46 |
| CHEMBL5196407 | — | — | 1 | 6.34 |
| CHEMBL5177494 | — | — | 1 | 6.12 |
| CHEMBL5181752 | — | — | 1 | 6.05 |
| CHEMBL5195937 | — | — | 1 | 5.93 |
| CHEMBL5175444 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175981 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL430239 | MELATONAN | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL3301624 | SETMELANOTIDE | Ki | = | 4.266 | nM | 8.37 |
| CHEMBL5185945 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL2070241 | BREMELANOTIDE | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL5203986 | — | Ki | = | 22.39 | nM | 7.65 |
| CHEMBL5181812 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL5185775 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL5176443 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL5192329 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL5191309 | — | Ki | = | 33.88 | nM | 7.47 |
| CHEMBL5175487 | — | Ki | = | 35.48 | nM | 7.45 |
| CHEMBL5190042 | — | Ki | = | 43.65 | nM | 7.36 |
| CHEMBL5170533 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL5178164 | — | Ki | = | 45.71 | nM | 7.34 |
| CHEMBL5172738 | — | Ki | = | 61.66 | nM | 7.21 |
| CHEMBL5195641 | — | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL5185405 | — | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL5204285 | — | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL5207936 | — | Ki | = | 165.96 | nM | 6.78 |
| CHEMBL5179373 | — | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL5179081 | — | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL5182345 | — | Ki | = | 295.12 | nM | 6.53 |
| CHEMBL5187932 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL5199932 | — | Ki | = | 346.74 | nM | 6.46 |
| CHEMBL5196407 | — | Ki | = | 457.09 | nM | 6.34 |
| CHEMBL5177494 | — | Ki | = | 758.58 | nM | 6.12 |
| CHEMBL5181752 | — | Ki | = | 891.25 | nM | 6.05 |
| CHEMBL5195937 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL5175444 | — | Ki | = | 1288.25 | nM | 5.89 |
| CHEMBL5208830 | — | Ki | = | 2137.96 | nM | 5.67 |