Assay Detail
Functional
CHEMBL5107059
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MC1R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
34
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK2936E |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 29 | 9.39 | 10.35 |
| pEC50 | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5191309 | — | — | 2 | 10.35 |
| CHEMBL5185775 | — | — | 1 | 10.33 |
| CHEMBL2070241 | BREMELANOTIDE | 4.0 | 1 | 10.11 |
| CHEMBL5172738 | — | — | 1 | 10.09 |
| CHEMBL5175487 | — | — | 1 | 10.06 |
| CHEMBL5207936 | — | — | 1 | 10.05 |
| CHEMBL5203986 | — | — | 1 | 10.05 |
| CHEMBL5178164 | — | — | 1 | 9.91 |
| CHEMBL5170533 | — | — | 1 | 9.85 |
| CHEMBL3301624 | SETMELANOTIDE | 4.0 | 1 | 9.80 |
| CHEMBL5192329 | — | — | 1 | 9.71 |
| CHEMBL5179081 | — | — | 2 | 9.62 |
| CHEMBL5185405 | — | — | 1 | 9.54 |
| CHEMBL5195641 | — | — | 1 | 9.47 |
| CHEMBL5187932 | — | — | 1 | 9.32 |
| CHEMBL5190042 | — | — | 1 | 9.26 |
| CHEMBL5196407 | — | — | 1 | 8.79 |
| CHEMBL5208830 | — | — | 1 | 8.73 |
| CHEMBL5195937 | — | — | 1 | 8.67 |
| CHEMBL5175444 | — | — | 1 | 8.53 |
| CHEMBL5181752 | — | — | 1 | 8.40 |
| CHEMBL5182345 | — | — | 1 | 8.32 |
| CHEMBL5177494 | — | — | 1 | 8.29 |
| CHEMBL5199932 | — | — | 1 | 8.06 |
| CHEMBL430239 | MELATONAN | — | 1 | - |
| CHEMBL5185945 | — | — | 2 | - |
| CHEMBL5175981 | — | — | 1 | - |
| CHEMBL5179373 | — | — | 1 | - |
| CHEMBL5204285 | — | — | 1 | - |
| CHEMBL5181812 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5191309 | — | EC50 | = | 0.04467 | nM | 10.35 |
| CHEMBL5185775 | — | EC50 | = | 0.04677 | nM | 10.33 |
| CHEMBL2070241 | BREMELANOTIDE | EC50 | = | 0.07762 | nM | 10.11 |
| CHEMBL5172738 | — | EC50 | = | 0.08128 | nM | 10.09 |
| CHEMBL5175487 | — | EC50 | = | 0.0871 | nM | 10.06 |
| CHEMBL5207936 | — | EC50 | = | 0.08913 | nM | 10.05 |
| CHEMBL5203986 | — | EC50 | = | 0.08913 | nM | 10.05 |
| CHEMBL5178164 | — | EC50 | = | 0.123 | nM | 9.91 |
| CHEMBL5170533 | — | EC50 | = | 0.1413 | nM | 9.85 |
| CHEMBL3301624 | SETMELANOTIDE | EC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL5192329 | — | EC50 | = | 0.195 | nM | 9.71 |
| CHEMBL5179081 | — | EC50 | = | 0.2399 | nM | 9.62 |
| CHEMBL5185405 | — | EC50 | = | 0.2884 | nM | 9.54 |
| CHEMBL5195641 | — | EC50 | = | 0.3388 | nM | 9.47 |
| CHEMBL5187932 | — | EC50 | = | 0.4786 | nM | 9.32 |
| CHEMBL5190042 | — | EC50 | = | 0.5495 | nM | 9.26 |
| CHEMBL5196407 | — | EC50 | = | 1.622 | nM | 8.79 |
| CHEMBL5208830 | — | EC50 | = | 1.862 | nM | 8.73 |
| CHEMBL5195937 | — | EC50 | = | 2.138 | nM | 8.67 |
| CHEMBL5175444 | — | EC50 | = | 2.951 | nM | 8.53 |
| CHEMBL5181752 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL5182345 | — | EC50 | = | 4.786 | nM | 8.32 |
| CHEMBL5177494 | — | EC50 | = | 5.129 | nM | 8.29 |
| CHEMBL5199932 | — | EC50 | = | 8.71 | nM | 8.06 |
| CHEMBL430239 | MELATONAN | EC50 | < | 0.03162 | nM | - |
| CHEMBL5185945 | — | EC50 | < | 0.00912 | nM | - |
| CHEMBL5175981 | — | pEC50 | - | — | - | |
| CHEMBL5179373 | — | pEC50 | - | — | - | |
| CHEMBL5204285 | — | pEC50 | - | — | - | |
| CHEMBL5181812 | — | pEC50 | - | — | - | |
| CHEMBL5176443 | — | pEC50 | - | — | - | |
| CHEMBL5191309 | — | EC50 | = | 0.004 | nM | - |
| CHEMBL5185945 | — | EC50 | < | 0.009 | nM | - |
| CHEMBL5179081 | — | EC50 | < | 0.3 | nM | - |