Assay Detail
Binding
CHEMBL5320172
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of sCy5-MT-I from human MC1R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 |
|---|---|---|---|
| Ki | 14 | 7.99 | 10.00 |
| pKi | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 10.00 |
| CHEMBL5421885 | — | — | 1 | 8.95 |
| CHEMBL5432664 | — | — | 1 | 8.90 |
| CHEMBL5414451 | — | — | 1 | 8.60 |
| CHEMBL5399539 | — | — | 1 | 8.47 |
| CHEMBL5432868 | — | — | 1 | 8.45 |
| CHEMBL5398659 | — | — | 1 | 8.42 |
| CHEMBL5426684 | — | — | 1 | 8.30 |
| CHEMBL5405038 | — | — | 1 | 7.25 |
| CHEMBL5413092 | — | — | 1 | 7.19 |
| CHEMBL5421108 | — | — | 1 | 7.10 |
| CHEMBL504986 | — | — | 1 | 6.90 |
| CHEMBL5438253 | — | — | 1 | 6.80 |
| CHEMBL5438629 | — | — | 1 | 6.57 |
| CHEMBL5416095 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL5421885 | — | Ki | = | 1.122 | nM | 8.95 |
| CHEMBL5432664 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL5414451 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL5399539 | — | Ki | = | 3.388 | nM | 8.47 |
| CHEMBL5432868 | — | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL5398659 | — | Ki | = | 3.802 | nM | 8.42 |
| CHEMBL5426684 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL5405038 | — | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL5413092 | — | Ki | = | 64.57 | nM | 7.19 |
| CHEMBL5421108 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL504986 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL5438253 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL5438629 | — | Ki | = | 269.15 | nM | 6.57 |
| CHEMBL5416095 | — | pKi | - | — | - |