Assay Detail
Functional
CHEMBL5320165
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MC1R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Flp-In-293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Targeting Melanocortin Receptors Using S<sub><i>N</i></sub>Ar-Type Macrocyclization: A Doubly Orthogonal Route to Cyclic Peptide Conjugates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 7.93 | 10.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 10.20 |
| CHEMBL5421885 | — | — | 1 | 8.80 |
| CHEMBL5399539 | — | — | 1 | 8.65 |
| CHEMBL5398659 | — | — | 1 | 8.57 |
| CHEMBL5432868 | — | — | 1 | 8.32 |
| CHEMBL5432664 | — | — | 1 | 8.01 |
| CHEMBL5426684 | — | — | 1 | 8.00 |
| CHEMBL5414451 | — | — | 1 | 7.78 |
| CHEMBL5416095 | — | — | 2 | 7.68 |
| CHEMBL5421108 | — | — | 1 | 7.47 |
| CHEMBL5413092 | — | — | 1 | 7.46 |
| CHEMBL5438629 | — | — | 1 | 7.30 |
| CHEMBL5405038 | — | — | 1 | 7.20 |
| CHEMBL504986 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | EC50 | = | 0.0631 | nM | 10.20 |
| CHEMBL5421885 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL5399539 | — | EC50 | = | 2.239 | nM | 8.65 |
| CHEMBL5398659 | — | EC50 | = | 2.692 | nM | 8.57 |
| CHEMBL5432868 | — | EC50 | = | 4.786 | nM | 8.32 |
| CHEMBL5432664 | — | EC50 | = | 9.772 | nM | 8.01 |
| CHEMBL5426684 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5414451 | — | EC50 | = | 16.6 | nM | 7.78 |
| CHEMBL5416095 | — | EC50 | = | 20.89 | nM | 7.68 |
| CHEMBL5416095 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5421108 | — | EC50 | = | 33.88 | nM | 7.47 |
| CHEMBL5413092 | — | EC50 | = | 34.67 | nM | 7.46 |
| CHEMBL5438629 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL5405038 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL504986 | — | EC50 | = | 1258.93 | nM | 5.90 |