Assay Detail
Functional
CHEMBL910338
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MC1R
16
Total Activities
16
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 |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 16 | 7.23 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212614 | — | — | 1 | 10.15 |
| CHEMBL215833 | — | — | 1 | 9.43 |
| CHEMBL384774 | — | — | 1 | 8.77 |
| CHEMBL379054 | — | — | 1 | 8.77 |
| CHEMBL384176 | — | — | 1 | 8.64 |
| CHEMBL214410 | — | — | 1 | 8.43 |
| CHEMBL211699 | — | — | 1 | 7.85 |
| CHEMBL385000 | — | — | 1 | 7.52 |
| CHEMBL215895 | — | — | 1 | 6.98 |
| CHEMBL378837 | — | — | 1 | 6.50 |
| CHEMBL213566 | — | — | 1 | 6.45 |
| CHEMBL211975 | — | — | 1 | 6.28 |
| CHEMBL215576 | — | — | 1 | 5.86 |
| CHEMBL387246 | — | — | 1 | 4.70 |
| CHEMBL202699 | — | — | 1 | 4.70 |
| CHEMBL212332 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212614 | — | EC50 | = | 0.07 | nM | 10.15 |
| CHEMBL215833 | — | EC50 | = | 0.37 | nM | 9.43 |
| CHEMBL384774 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL379054 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL384176 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL214410 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL211699 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL385000 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL215895 | — | EC50 | = | 104.0 | nM | 6.98 |
| CHEMBL378837 | — | EC50 | = | 317.0 | nM | 6.50 |
| CHEMBL213566 | — | EC50 | = | 353.0 | nM | 6.45 |
| CHEMBL211975 | — | EC50 | = | 526.0 | nM | 6.28 |
| CHEMBL215576 | — | EC50 | = | 1391.0 | nM | 5.86 |
| CHEMBL387246 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL202699 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL212332 | — | EC50 | = | 21667.0 | nM | 4.66 |