Assay Detail
Binding
CHEMBL5320174
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of sCy5-MT-I from human MC4R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
16
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 | 15 | 9.54 | 10.47 |
| pKi | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | — | 1 | 10.47 |
| CHEMBL5414451 | — | — | 2 | 10.22 |
| CHEMBL5421885 | — | — | 1 | 9.99 |
| CHEMBL5398659 | — | — | 1 | 9.85 |
| CHEMBL5426684 | — | — | 1 | 9.83 |
| CHEMBL5432868 | — | — | 1 | 9.79 |
| CHEMBL5413092 | — | — | 1 | 9.63 |
| CHEMBL5438629 | — | — | 1 | 9.48 |
| CHEMBL5399539 | — | — | 1 | 9.34 |
| CHEMBL5438253 | — | — | 1 | 9.10 |
| CHEMBL5421108 | — | — | 1 | 9.06 |
| CHEMBL5432664 | — | — | 1 | 8.90 |
| CHEMBL504986 | — | — | 1 | 8.80 |
| CHEMBL5405038 | — | — | 1 | 8.52 |
| CHEMBL5416095 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430239 | MELATONAN | Ki | = | 0.03388 | nM | 10.47 |
| CHEMBL5414451 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL5414451 | — | Ki | = | 0.06457 | nM | 10.19 |
| CHEMBL5421885 | — | Ki | = | 0.1023 | nM | 9.99 |
| CHEMBL5398659 | — | Ki | = | 0.1413 | nM | 9.85 |
| CHEMBL5426684 | — | Ki | = | 0.1479 | nM | 9.83 |
| CHEMBL5432868 | — | Ki | = | 0.1622 | nM | 9.79 |
| CHEMBL5413092 | — | Ki | = | 0.2344 | nM | 9.63 |
| CHEMBL5438629 | — | Ki | = | 0.3311 | nM | 9.48 |
| CHEMBL5399539 | — | Ki | = | 0.4571 | nM | 9.34 |
| CHEMBL5438253 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL5421108 | — | Ki | = | 0.871 | nM | 9.06 |
| CHEMBL5432664 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL504986 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL5405038 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL5416095 | — | pKi | - | — | - |