Assay Detail
Functional
CHEMBL3297364
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 6.23 | 7.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3287326 | — | — | 1 | 7.09 |
| CHEMBL3287322 | — | — | 1 | 6.72 |
| CHEMBL3287327 | — | — | 1 | 6.58 |
| CHEMBL3287328 | — | — | 1 | 6.33 |
| CHEMBL264190 | — | — | 1 | 5.92 |
| CHEMBL3287324 | — | — | 1 | 4.71 |
| CHEMBL3287323 | — | — | 1 | - |
| CHEMBL3287325 | — | — | 1 | - |
| CHEMBL3287329 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3287326 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3287322 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3287327 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3287328 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL264190 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3287324 | — | EC50 | = | 19650.0 | nM | 4.71 |
| CHEMBL3287323 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3287325 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3287329 | — | EC50 | > | 100000.0 | nM | - |