Assay Detail
Functional
CHEMBL910342
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MC4R
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 8.33 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL379054 | — | — | 1 | 9.70 |
| CHEMBL212614 | — | — | 1 | 9.52 |
| CHEMBL215833 | — | — | 1 | 9.47 |
| CHEMBL384176 | — | — | 1 | 9.30 |
| CHEMBL215895 | — | — | 1 | 8.80 |
| CHEMBL378837 | — | — | 1 | 8.80 |
| CHEMBL214410 | — | — | 1 | 8.80 |
| CHEMBL211975 | — | — | 1 | 8.77 |
| CHEMBL384774 | — | — | 1 | 8.70 |
| CHEMBL213566 | — | — | 1 | 8.66 |
| CHEMBL211699 | — | — | 1 | 8.24 |
| CHEMBL385000 | — | — | 1 | 8.06 |
| CHEMBL215576 | — | — | 1 | 8.05 |
| CHEMBL213284 | — | — | 1 | 7.92 |
| CHEMBL212855 | — | — | 1 | 7.75 |
| CHEMBL202699 | — | — | 1 | 7.36 |
| CHEMBL214770 | — | — | 1 | 7.35 |
| CHEMBL212332 | — | — | 1 | 6.85 |
| CHEMBL387246 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL379054 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL212614 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL215833 | — | EC50 | = | 0.34 | nM | 9.47 |
| CHEMBL384176 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL215895 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL378837 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL214410 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL211975 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL384774 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL213566 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL211699 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL385000 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL215576 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL213284 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL212855 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL202699 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL214770 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL212332 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL387246 | — | EC50 | = | 809.0 | nM | 6.09 |