Assay Detail
Binding
CHEMBL5034976
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 16-23 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 | 6.53 | 7.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3301624 | SETMELANOTIDE | 4.0 | 1 | 7.88 |
| CHEMBL430239 | MELATONAN | — | 1 | 7.73 |
| CHEMBL5087839 | — | — | 1 | 7.30 |
| CHEMBL5087859 | — | — | 1 | 7.29 |
| CHEMBL5083551 | — | — | 1 | 7.07 |
| CHEMBL5087814 | — | — | 1 | 7.00 |
| CHEMBL5094168 | — | — | 1 | 6.98 |
| CHEMBL5090946 | — | — | 1 | 6.97 |
| CHEMBL5080489 | — | — | 1 | 6.87 |
| CHEMBL5081077 | — | — | 1 | 6.83 |
| CHEMBL2070241 | BREMELANOTIDE | 4.0 | 1 | 6.70 |
| CHEMBL5075712 | — | — | 1 | 6.57 |
| CHEMBL5080784 | — | — | 1 | 6.52 |
| CHEMBL5090670 | — | — | 1 | 6.42 |
| CHEMBL5090285 | — | — | 1 | 6.41 |
| CHEMBL5077095 | — | — | 1 | 6.41 |
| CHEMBL5076315 | — | — | 1 | 6.39 |
| CHEMBL5091236 | — | — | 1 | 6.32 |
| CHEMBL5094215 | — | — | 1 | 6.15 |
| CHEMBL5077144 | — | — | 1 | 6.05 |
| CHEMBL5092761 | — | — | 1 | 6.05 |
| CHEMBL5078687 | — | — | 1 | 5.94 |
| CHEMBL5075506 | — | — | 1 | 5.76 |
| CHEMBL5077811 | — | — | 1 | 5.50 |
| CHEMBL5085972 | — | — | 1 | 5.40 |
| CHEMBL5091245 | — | — | 1 | 5.30 |
| CHEMBL4099889 | — | — | 1 | - |
| CHEMBL5093939 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3301624 | SETMELANOTIDE | Ki | = | 13.18 | nM | 7.88 |
| CHEMBL430239 | MELATONAN | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL5087839 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5087859 | — | Ki | = | 51.29 | nM | 7.29 |
| CHEMBL5083551 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL5087814 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5094168 | — | Ki | = | 104.71 | nM | 6.98 |
| CHEMBL5090946 | — | Ki | = | 107.15 | nM | 6.97 |
| CHEMBL5080489 | — | Ki | = | 134.9 | nM | 6.87 |
| CHEMBL5081077 | — | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL2070241 | BREMELANOTIDE | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL5075712 | — | Ki | = | 269.15 | nM | 6.57 |
| CHEMBL5080784 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL5090670 | — | Ki | = | 380.19 | nM | 6.42 |
| CHEMBL5090285 | — | Ki | = | 389.05 | nM | 6.41 |
| CHEMBL5077095 | — | Ki | = | 389.05 | nM | 6.41 |
| CHEMBL5076315 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL5091236 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL5094215 | — | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL5077144 | — | Ki | = | 891.25 | nM | 6.05 |
| CHEMBL5092761 | — | Ki | = | 891.25 | nM | 6.05 |
| CHEMBL5078687 | — | Ki | = | 1148.15 | nM | 5.94 |
| CHEMBL5075506 | — | Ki | = | 1737.8 | nM | 5.76 |
| CHEMBL5077811 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL5085972 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL5091245 | — | Ki | = | 5011.87 | nM | 5.30 |
| CHEMBL4099889 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5093939 | — | Ki | > | 1000.0 | nM | - |