Assay Detail
Binding
CHEMBL5034977
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 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
28
Total Activities
28
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
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.31 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 8.90 |
| CHEMBL3301624 | SETMELANOTIDE | 4.0 | 1 | 8.39 |
| CHEMBL5076315 | — | — | 1 | 8.10 |
| CHEMBL5087839 | — | — | 1 | 8.09 |
| CHEMBL5090670 | — | — | 1 | 7.99 |
| CHEMBL5090285 | — | — | 1 | 7.97 |
| CHEMBL5083551 | — | — | 1 | 7.87 |
| CHEMBL5080489 | — | — | 1 | 7.82 |
| CHEMBL2070241 | BREMELANOTIDE | 4.0 | 1 | 7.66 |
| CHEMBL5077095 | — | — | 1 | 7.59 |
| CHEMBL5090946 | — | — | 1 | 7.59 |
| CHEMBL5087814 | — | — | 1 | 7.52 |
| CHEMBL5087859 | — | — | 1 | 7.52 |
| CHEMBL5080784 | — | — | 1 | 7.44 |
| CHEMBL5077144 | — | — | 1 | 7.30 |
| CHEMBL5094168 | — | — | 1 | 7.19 |
| CHEMBL5094215 | — | — | 1 | 7.14 |
| CHEMBL5078687 | — | — | 1 | 7.04 |
| CHEMBL5075712 | — | — | 1 | 6.94 |
| CHEMBL5091236 | — | — | 1 | 6.86 |
| CHEMBL5081077 | — | — | 1 | 6.80 |
| CHEMBL5091245 | — | — | 1 | 6.51 |
| CHEMBL5085972 | — | — | 1 | 6.46 |
| CHEMBL5092761 | — | — | 1 | 6.45 |
| CHEMBL5075506 | — | — | 1 | 6.23 |
| CHEMBL4099889 | — | — | 1 | 6.21 |
| CHEMBL5077811 | — | — | 1 | 5.69 |
| CHEMBL5093939 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL3301624 | SETMELANOTIDE | Ki | = | 4.074 | nM | 8.39 |
| CHEMBL5076315 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL5087839 | — | Ki | = | 8.128 | nM | 8.09 |
| CHEMBL5090670 | — | Ki | = | 10.23 | nM | 7.99 |
| CHEMBL5090285 | — | Ki | = | 10.72 | nM | 7.97 |
| CHEMBL5083551 | — | Ki | = | 13.49 | nM | 7.87 |
| CHEMBL5080489 | — | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL2070241 | BREMELANOTIDE | Ki | = | 21.88 | nM | 7.66 |
| CHEMBL5077095 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL5090946 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL5087814 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL5087859 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL5080784 | — | Ki | = | 36.31 | nM | 7.44 |
| CHEMBL5077144 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5094168 | — | Ki | = | 64.57 | nM | 7.19 |
| CHEMBL5094215 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL5078687 | — | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL5075712 | — | Ki | = | 114.82 | nM | 6.94 |
| CHEMBL5091236 | — | Ki | = | 138.04 | nM | 6.86 |
| CHEMBL5081077 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL5091245 | — | Ki | = | 309.03 | nM | 6.51 |
| CHEMBL5085972 | — | Ki | = | 346.74 | nM | 6.46 |
| CHEMBL5092761 | — | Ki | = | 354.81 | nM | 6.45 |
| CHEMBL5075506 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL4099889 | — | Ki | = | 616.6 | nM | 6.21 |
| CHEMBL5077811 | — | Ki | = | 2041.74 | nM | 5.69 |
| CHEMBL5093939 | — | Ki | > | 1000.0 | nM | - |