Assay Detail
Binding
CHEMBL5320097
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human MC4R in CHO cells measured for 24 hrs
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.12 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5429895 | — | — | 1 | 8.42 |
| CHEMBL5416581 | — | — | 1 | 8.11 |
| CHEMBL5414435 | — | — | 1 | 8.08 |
| CHEMBL5432266 | — | — | 1 | 7.89 |
| CHEMBL5437451 | — | — | 1 | 7.41 |
| CHEMBL5403087 | — | — | 1 | 6.68 |
| CHEMBL5432198 | — | — | 1 | 6.62 |
| CHEMBL5418302 | — | — | 1 | 6.19 |
| CHEMBL5425592 | — | — | 1 | 4.70 |
| CHEMBL5411590 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5429895 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5416581 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5414435 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5432266 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5437451 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5403087 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5432198 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5418302 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5425592 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL5411590 | — | IC50 | - | — | - |