Assay Detail
Functional
CHEMBL925942
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MC5R expressed in CHO cells assesses as cAMP release
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 6.38 | 6.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429854 | — | — | 1 | 6.99 |
| CHEMBL257759 | — | — | 1 | 6.78 |
| CHEMBL254589 | — | — | 1 | 6.43 |
| CHEMBL255286 | — | — | 1 | 6.34 |
| CHEMBL403420 | — | — | 1 | 5.91 |
| CHEMBL254757 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429854 | — | EC50 | = | 101.6 | nM | 6.99 |
| CHEMBL257759 | — | EC50 | = | 166.7 | nM | 6.78 |
| CHEMBL254589 | — | EC50 | = | 372.0 | nM | 6.43 |
| CHEMBL255286 | — | EC50 | = | 455.0 | nM | 6.34 |
| CHEMBL403420 | — | EC50 | = | 1233.0 | nM | 5.91 |
| CHEMBL254757 | — | EC50 | = | 1600.0 | nM | 5.80 |