Assay Detail
Functional
CHEMBL834875
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Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
14
Total Activities
13
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 | Expert |
Publication
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.53 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL405282 | — | — | 1 | 9.48 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.10 |
| CHEMBL439691 | — | — | 1 | 8.80 |
| CHEMBL443071 | — | — | 1 | 8.70 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 8.17 |
| CHEMBL2371712 | — | — | 1 | 7.96 |
| CHEMBL2310901 | — | — | 1 | 7.89 |
| CHEMBL2096759 | — | — | 1 | 6.85 |
| CHEMBL413439 | — | — | 1 | 6.52 |
| CHEMBL437050 | — | — | 2 | 6.28 |
| CHEMBL414778 | — | — | 1 | 6.02 |
| CHEMBL411359 | — | — | 1 | 6.00 |
| CHEMBL408509 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL405282 | — | EC50 | = | 0.33 | nM | 9.48 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL439691 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL443071 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 6.7 | nM | 8.17 |
| CHEMBL2371712 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2310901 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2096759 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL413439 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL437050 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL437050 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL414778 | — | EC50 | = | 951.0 | nM | 6.02 |
| CHEMBL411359 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL408509 | — | EC50 | > | 10000.0 | nM | - |