Assay Detail
Functional
CHEMBL5034972
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human melanocortin receptor 1 expressed in human T-Rex-293 cells 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 | T-REx-293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 9.23 | 10.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5083551 | — | — | 1 | 10.25 |
| CHEMBL5092761 | — | — | 1 | 10.19 |
| CHEMBL2070241 | BREMELANOTIDE | 4.0 | 1 | 10.11 |
| CHEMBL5094168 | — | — | 1 | 10.08 |
| CHEMBL5090946 | — | — | 1 | 10.04 |
| CHEMBL5091236 | — | — | 1 | 9.96 |
| CHEMBL5077095 | — | — | 1 | 9.87 |
| CHEMBL5075712 | — | — | 1 | 9.86 |
| CHEMBL5075506 | — | — | 1 | 9.85 |
| CHEMBL3301624 | SETMELANOTIDE | 4.0 | 1 | 9.80 |
| CHEMBL5077144 | — | — | 1 | 9.37 |
| CHEMBL5080784 | — | — | 1 | 9.16 |
| CHEMBL5093939 | — | — | 1 | 9.12 |
| CHEMBL5090285 | — | — | 1 | 9.10 |
| CHEMBL5081077 | — | — | 1 | 9.09 |
| CHEMBL5094215 | — | — | 1 | 9.08 |
| CHEMBL5080489 | — | — | 1 | 8.97 |
| CHEMBL5087814 | — | — | 1 | 8.88 |
| CHEMBL5076315 | — | — | 1 | 8.81 |
| CHEMBL5078687 | — | — | 1 | 8.65 |
| CHEMBL5090670 | — | — | 1 | 8.44 |
| CHEMBL5091245 | — | — | 1 | 8.44 |
| CHEMBL5077811 | — | — | 1 | 8.26 |
| CHEMBL5085972 | — | — | 1 | 8.06 |
| CHEMBL4099889 | — | — | 1 | 7.19 |
| CHEMBL5087839 | — | — | 1 | - |
| CHEMBL5087859 | — | — | 1 | - |
| CHEMBL430239 | MELATONAN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5083551 | — | EC50 | = | 0.05623 | nM | 10.25 |
| CHEMBL5092761 | — | EC50 | = | 0.06457 | nM | 10.19 |
| CHEMBL2070241 | BREMELANOTIDE | EC50 | = | 0.07762 | nM | 10.11 |
| CHEMBL5094168 | — | EC50 | = | 0.08318 | nM | 10.08 |
| CHEMBL5090946 | — | EC50 | = | 0.0912 | nM | 10.04 |
| CHEMBL5091236 | — | EC50 | = | 0.1096 | nM | 9.96 |
| CHEMBL5077095 | — | EC50 | = | 0.1349 | nM | 9.87 |
| CHEMBL5075712 | — | EC50 | = | 0.138 | nM | 9.86 |
| CHEMBL5075506 | — | EC50 | = | 0.1413 | nM | 9.85 |
| CHEMBL3301624 | SETMELANOTIDE | EC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL5077144 | — | EC50 | = | 0.4266 | nM | 9.37 |
| CHEMBL5080784 | — | EC50 | = | 0.6918 | nM | 9.16 |
| CHEMBL5093939 | — | EC50 | = | 0.7586 | nM | 9.12 |
| CHEMBL5090285 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL5081077 | — | EC50 | = | 0.8128 | nM | 9.09 |
| CHEMBL5094215 | — | EC50 | = | 0.8318 | nM | 9.08 |
| CHEMBL5080489 | — | EC50 | = | 1.072 | nM | 8.97 |
| CHEMBL5087814 | — | EC50 | = | 1.318 | nM | 8.88 |
| CHEMBL5076315 | — | EC50 | = | 1.549 | nM | 8.81 |
| CHEMBL5078687 | — | EC50 | = | 2.239 | nM | 8.65 |
| CHEMBL5090670 | — | EC50 | = | 3.631 | nM | 8.44 |
| CHEMBL5091245 | — | EC50 | = | 3.631 | nM | 8.44 |
| CHEMBL5077811 | — | EC50 | = | 5.495 | nM | 8.26 |
| CHEMBL5085972 | — | EC50 | = | 8.71 | nM | 8.06 |
| CHEMBL4099889 | — | EC50 | = | 64.57 | nM | 7.19 |
| CHEMBL5087839 | — | EC50 | > | 0.05012 | nM | - |
| CHEMBL5087859 | — | EC50 | < | 0.05012 | nM | - |
| CHEMBL430239 | MELATONAN | EC50 | < | 0.05012 | nM | - |