Assay Detail
Functional
CHEMBL866559
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist potency at MC4 receptor
20
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis of Tic-D-Phe Psi[CH2-CH2] isostere and its use in the development of melanocortin receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 7.46 | 8.10 |
| Emax | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL380120 | — | — | 2 | 8.10 |
| CHEMBL437132 | — | — | 2 | 8.00 |
| CHEMBL381357 | — | — | 2 | 8.00 |
| CHEMBL203252 | — | — | 2 | 7.70 |
| CHEMBL206033 | — | — | 2 | 7.66 |
| CHEMBL444883 | — | — | 2 | 7.42 |
| CHEMBL202699 | — | — | 2 | 7.36 |
| CHEMBL380437 | — | — | 2 | 6.85 |
| CHEMBL383256 | — | — | 2 | 6.80 |
| CHEMBL206018 | — | — | 2 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL380120 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL381357 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL437132 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL203252 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL206033 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL444883 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL202699 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL380437 | — | EC50 | = | 142.0 | nM | 6.85 |
| CHEMBL383256 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL206018 | — | EC50 | = | 193.0 | nM | 6.71 |
| CHEMBL202699 | — | Emax | = | 84.0 | % | - |
| CHEMBL380437 | — | Emax | = | 76.0 | % | - |
| CHEMBL206033 | — | Emax | = | 89.0 | % | - |
| CHEMBL380120 | — | Emax | = | 84.0 | % | - |
| CHEMBL383256 | — | Emax | = | 77.0 | % | - |
| CHEMBL206018 | — | Emax | = | 100.0 | % | - |
| CHEMBL203252 | — | Emax | = | 102.0 | % | - |
| CHEMBL437132 | — | Emax | = | 91.0 | % | - |
| CHEMBL444883 | — | Emax | = | 90.0 | % | - |
| CHEMBL381357 | — | Emax | = | 81.0 | % | - |