Assay Detail
Functional
CHEMBL835628
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Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
13
Total Activities
12
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 | 13 | 7.06 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.00 |
| CHEMBL443071 | — | — | 1 | 8.72 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 8.09 |
| CHEMBL411359 | — | — | 1 | 7.09 |
| CHEMBL405282 | — | — | 1 | 7.09 |
| CHEMBL439691 | — | — | 1 | 7.00 |
| CHEMBL438920 | — | — | 1 | 6.70 |
| CHEMBL2310901 | — | — | 1 | 6.60 |
| CHEMBL437050 | — | — | 2 | 6.41 |
| CHEMBL2096759 | — | — | 1 | 6.39 |
| CHEMBL414778 | — | — | 1 | 6.31 |
| CHEMBL408509 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL443071 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL411359 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL405282 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL439691 | — | EC50 | = | 99.0 | nM | 7.00 |
| CHEMBL438920 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2310901 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL437050 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2096759 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL414778 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL437050 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL408509 | — | EC50 | = | 870.0 | nM | 6.06 |