Assay Detail
Binding
CHEMBL5320173
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of sCy5-MT-I from human MC3R 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 |
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 | 6.85 | 9.03 |
| pKi | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 9.03 |
| CHEMBL5432664 | — | — | 1 | 8.10 |
| CHEMBL5421885 | — | — | 1 | 7.10 |
| CHEMBL5426684 | — | — | 1 | 7.01 |
| CHEMBL5399539 | — | — | 1 | 6.88 |
| CHEMBL5432868 | — | — | 1 | 6.83 |
| CHEMBL5414451 | — | — | 1 | 6.76 |
| CHEMBL5398659 | — | — | 1 | 6.58 |
| CHEMBL504986 | — | — | 1 | 6.50 |
| CHEMBL5421108 | — | — | 1 | 6.36 |
| CHEMBL5405038 | — | — | 1 | 6.29 |
| CHEMBL5438253 | — | — | 1 | 6.18 |
| CHEMBL5413092 | — | — | 1 | 6.13 |
| CHEMBL5438629 | — | — | 1 | 6.09 |
| CHEMBL5416095 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | Ki | = | 0.9333 | nM | 9.03 |
| CHEMBL5432664 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL5421885 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL5426684 | — | Ki | = | 97.72 | nM | 7.01 |
| CHEMBL5399539 | — | Ki | = | 131.83 | nM | 6.88 |
| CHEMBL5432868 | — | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL5414451 | — | Ki | = | 173.78 | nM | 6.76 |
| CHEMBL5398659 | — | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL504986 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL5421108 | — | Ki | = | 436.52 | nM | 6.36 |
| CHEMBL5405038 | — | Ki | = | 512.86 | nM | 6.29 |
| CHEMBL5438253 | — | Ki | = | 660.69 | nM | 6.18 |
| CHEMBL5413092 | — | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL5438629 | — | Ki | = | 812.83 | nM | 6.09 |
| CHEMBL5416095 | — | pKi | - | — | - |