Assay Detail
Functional
CHEMBL5034982
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 28 | 8.80 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2070241 | BREMELANOTIDE | 4.0 | 1 | 9.92 |
| CHEMBL5090946 | — | — | 1 | 9.88 |
| CHEMBL5083551 | — | — | 1 | 9.75 |
| CHEMBL5080489 | — | — | 1 | 9.66 |
| CHEMBL5087839 | — | — | 1 | 9.56 |
| CHEMBL5090285 | — | — | 1 | 9.52 |
| CHEMBL5090670 | — | — | 1 | 9.34 |
| CHEMBL5080784 | — | — | 1 | 9.27 |
| CHEMBL5077095 | — | — | 1 | 9.05 |
| CHEMBL5087859 | — | — | 1 | 9.01 |
| CHEMBL5076315 | — | — | 1 | 8.98 |
| CHEMBL5077144 | — | — | 1 | 8.92 |
| CHEMBL5091236 | — | — | 1 | 8.89 |
| CHEMBL5087814 | — | — | 1 | 8.80 |
| CHEMBL5078687 | — | — | 1 | 8.66 |
| CHEMBL5085972 | — | — | 1 | 8.59 |
| CHEMBL5094168 | — | — | 1 | 8.56 |
| CHEMBL4099889 | — | — | 1 | 8.51 |
| CHEMBL5094215 | — | — | 1 | 8.50 |
| CHEMBL5075712 | — | — | 1 | 8.47 |
| CHEMBL5091245 | — | — | 1 | 8.41 |
| CHEMBL5092761 | — | — | 1 | 8.37 |
| CHEMBL5081077 | — | — | 1 | 7.98 |
| CHEMBL5075506 | — | — | 1 | 7.64 |
| CHEMBL5093939 | — | — | 1 | 7.23 |
| CHEMBL5077811 | — | — | 1 | 7.20 |
| CHEMBL3301624 | SETMELANOTIDE | 4.0 | 1 | - |
| CHEMBL430239 | MELATONAN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2070241 | BREMELANOTIDE | EC50 | = | 0.1202 | nM | 9.92 |
| CHEMBL5090946 | — | EC50 | = | 0.1318 | nM | 9.88 |
| CHEMBL5083551 | — | EC50 | = | 0.1778 | nM | 9.75 |
| CHEMBL5080489 | — | EC50 | = | 0.2188 | nM | 9.66 |
| CHEMBL5087839 | — | EC50 | = | 0.2754 | nM | 9.56 |
| CHEMBL5090285 | — | EC50 | = | 0.302 | nM | 9.52 |
| CHEMBL5090670 | — | EC50 | = | 0.4571 | nM | 9.34 |
| CHEMBL5080784 | — | EC50 | = | 0.537 | nM | 9.27 |
| CHEMBL5077095 | — | EC50 | = | 0.8913 | nM | 9.05 |
| CHEMBL5087859 | — | EC50 | = | 0.9772 | nM | 9.01 |
| CHEMBL5076315 | — | EC50 | = | 1.047 | nM | 8.98 |
| CHEMBL5077144 | — | EC50 | = | 1.202 | nM | 8.92 |
| CHEMBL5091236 | — | EC50 | = | 1.288 | nM | 8.89 |
| CHEMBL5087814 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL5078687 | — | EC50 | = | 2.188 | nM | 8.66 |
| CHEMBL5085972 | — | EC50 | = | 2.57 | nM | 8.59 |
| CHEMBL5094168 | — | EC50 | = | 2.754 | nM | 8.56 |
| CHEMBL4099889 | — | EC50 | = | 3.09 | nM | 8.51 |
| CHEMBL5094215 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL5075712 | — | EC50 | = | 3.388 | nM | 8.47 |
| CHEMBL5091245 | — | EC50 | = | 3.89 | nM | 8.41 |
| CHEMBL5092761 | — | EC50 | = | 4.266 | nM | 8.37 |
| CHEMBL5081077 | — | EC50 | = | 10.47 | nM | 7.98 |
| CHEMBL5075506 | — | EC50 | = | 22.91 | nM | 7.64 |
| CHEMBL5093939 | — | EC50 | = | 58.88 | nM | 7.23 |
| CHEMBL5077811 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3301624 | SETMELANOTIDE | EC50 | < | 0.05012 | nM | - |
| CHEMBL430239 | MELATONAN | EC50 | < | 0.05012 | nM | - |