Assay Detail
Functional
CHEMBL3297367
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Agonist activity at mouse melanocortin-3 receptor 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 | Mus musculus |
| 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 | 7.73 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.48 |
| CHEMBL3287323 | — | — | 1 | 7.93 |
| CHEMBL3287327 | — | — | 1 | 7.72 |
| CHEMBL3287329 | — | — | 1 | 7.68 |
| CHEMBL3287325 | — | — | 1 | 7.66 |
| CHEMBL3287322 | — | — | 1 | 7.46 |
| CHEMBL3287324 | — | — | 1 | 7.33 |
| CHEMBL3287326 | — | — | 1 | 7.26 |
| CHEMBL3287328 | — | — | 1 | 7.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.33 | nM | 9.48 |
| CHEMBL3287323 | — | EC50 | = | 11.7 | nM | 7.93 |
| CHEMBL3287327 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3287329 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3287325 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3287322 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3287324 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3287326 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3287328 | — | EC50 | = | 94.0 | nM | 7.03 |