Assay Detail
Functional
CHEMBL834876
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
15
Total Activities
14
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 | 15 | 7.50 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.70 |
| CHEMBL443071 | — | — | 1 | 8.85 |
| CHEMBL214332 | INTERMEDINE | 2.0 | 1 | 8.68 |
| CHEMBL2371712 | — | — | 1 | 8.48 |
| CHEMBL2310901 | — | — | 1 | 7.58 |
| CHEMBL2096759 | — | — | 1 | 7.54 |
| CHEMBL439691 | — | — | 1 | 7.47 |
| CHEMBL438920 | — | — | 1 | 7.44 |
| CHEMBL437050 | — | — | 2 | 7.19 |
| CHEMBL411359 | — | — | 1 | 7.16 |
| CHEMBL405282 | — | — | 1 | 7.00 |
| CHEMBL413439 | — | — | 1 | 6.20 |
| CHEMBL414778 | — | — | 1 | 5.57 |
| CHEMBL408509 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL443071 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL214332 | INTERMEDINE | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2371712 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2310901 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2096759 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL439691 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL438920 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL437050 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL411359 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL405282 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL413439 | — | EC50 | = | 630.0 | nM | 6.20 |
| CHEMBL437050 | — | EC50 | = | 710.0 | nM | 6.15 |
| CHEMBL414778 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL408509 | — | EC50 | > | 10000.0 | nM | - |