Assay Detail
Binding
CHEMBL5107057
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-NDP-alpha-MSH from human MC3R 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 | 7.04 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175981 | — | — | 1 | 9.20 |
| CHEMBL5185945 | — | — | 1 | 8.29 |
| CHEMBL5185775 | — | — | 1 | 8.26 |
| CHEMBL5176443 | — | — | 1 | 7.99 |
| CHEMBL5191309 | — | — | 1 | 7.96 |
| CHEMBL5181812 | — | — | 1 | 7.94 |
| CHEMBL5178164 | — | — | 1 | 7.93 |
| CHEMBL3301624 | SETMELANOTIDE | 4.0 | 1 | 7.88 |
| CHEMBL5175487 | — | — | 1 | 7.87 |
| CHEMBL5203986 | — | — | 1 | 7.86 |
| CHEMBL5172738 | — | — | 1 | 7.78 |
| CHEMBL430239 | MELATONAN | — | 1 | 7.73 |
| CHEMBL5170533 | — | — | 1 | 7.71 |
| CHEMBL5195641 | — | — | 1 | 7.68 |
| CHEMBL5190042 | — | — | 1 | 7.63 |
| CHEMBL5192329 | — | — | 1 | 7.58 |
| CHEMBL5185405 | — | — | 1 | 7.55 |
| CHEMBL5179081 | — | — | 1 | 7.51 |
| CHEMBL5207936 | — | — | 1 | 7.45 |
| CHEMBL5204285 | — | — | 1 | 7.43 |
| CHEMBL5179373 | — | — | 1 | 7.29 |
| CHEMBL2070241 | BREMELANOTIDE | 4.0 | 1 | 6.70 |
| CHEMBL5187932 | — | — | 1 | 6.53 |
| CHEMBL5199932 | — | — | 1 | 5.40 |
| CHEMBL5182345 | — | — | 1 | 5.20 |
| CHEMBL5196407 | — | — | 1 | 5.08 |
| CHEMBL5175444 | — | — | 1 | 5.04 |
| CHEMBL5177494 | — | — | 1 | 5.01 |
| CHEMBL5208830 | — | — | 1 | 4.91 |
| CHEMBL5181752 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175981 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL5185945 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL5185775 | — | Ki | = | 5.495 | nM | 8.26 |
| CHEMBL5176443 | — | Ki | = | 10.23 | nM | 7.99 |
| CHEMBL5191309 | — | Ki | = | 10.96 | nM | 7.96 |
| CHEMBL5181812 | — | Ki | = | 11.48 | nM | 7.94 |
| CHEMBL5178164 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL3301624 | SETMELANOTIDE | Ki | = | 13.18 | nM | 7.88 |
| CHEMBL5175487 | — | Ki | = | 13.49 | nM | 7.87 |
| CHEMBL5203986 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL5172738 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL430239 | MELATONAN | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL5170533 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL5195641 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL5190042 | — | Ki | = | 23.44 | nM | 7.63 |
| CHEMBL5192329 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL5185405 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL5179081 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL5207936 | — | Ki | = | 35.48 | nM | 7.45 |
| CHEMBL5204285 | — | Ki | = | 37.15 | nM | 7.43 |
| CHEMBL5179373 | — | Ki | = | 51.29 | nM | 7.29 |
| CHEMBL2070241 | BREMELANOTIDE | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL5187932 | — | Ki | = | 295.12 | nM | 6.53 |
| CHEMBL5199932 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL5182345 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL5196407 | — | Ki | = | 8317.64 | nM | 5.08 |
| CHEMBL5175444 | — | Ki | = | 9120.11 | nM | 5.04 |
| CHEMBL5177494 | — | Ki | = | 9772.37 | nM | 5.01 |
| CHEMBL5208830 | — | Ki | = | 12302.69 | nM | 4.91 |
| CHEMBL5181752 | — | Ki | = | 12882.5 | nM | 4.89 |
| CHEMBL5195937 | — | Ki | = | 13182.57 | nM | 4.88 |