Assay Detail
Functional
CHEMBL925931
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP release
16
Total Activities
16
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 | 16 | 7.10 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429854 | — | — | 1 | 8.68 |
| CHEMBL254589 | — | — | 1 | 8.55 |
| CHEMBL257759 | — | — | 1 | 8.34 |
| CHEMBL255286 | — | — | 1 | 7.87 |
| CHEMBL404696 | — | — | 1 | 7.75 |
| CHEMBL403834 | — | — | 1 | 7.17 |
| CHEMBL403421 | — | — | 1 | 7.05 |
| CHEMBL254792 | — | — | 1 | 6.96 |
| CHEMBL403420 | — | — | 1 | 6.92 |
| CHEMBL257770 | — | — | 1 | 6.88 |
| CHEMBL254351 | — | — | 1 | 6.81 |
| CHEMBL404905 | — | — | 1 | 6.67 |
| CHEMBL402009 | — | — | 1 | 6.61 |
| CHEMBL256286 | — | — | 1 | 6.25 |
| CHEMBL257616 | — | — | 1 | 5.72 |
| CHEMBL257615 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429854 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL254589 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL257759 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL255286 | — | EC50 | = | 13.4 | nM | 7.87 |
| CHEMBL404696 | — | EC50 | = | 17.9 | nM | 7.75 |
| CHEMBL403834 | — | EC50 | = | 67.2 | nM | 7.17 |
| CHEMBL403421 | — | EC50 | = | 88.8 | nM | 7.05 |
| CHEMBL254792 | — | EC50 | = | 110.8 | nM | 6.96 |
| CHEMBL403420 | — | EC50 | = | 120.5 | nM | 6.92 |
| CHEMBL257770 | — | EC50 | = | 130.3 | nM | 6.88 |
| CHEMBL254351 | — | EC50 | = | 155.6 | nM | 6.81 |
| CHEMBL404905 | — | EC50 | = | 214.5 | nM | 6.67 |
| CHEMBL402009 | — | EC50 | = | 244.7 | nM | 6.61 |
| CHEMBL256286 | — | EC50 | = | 565.0 | nM | 6.25 |
| CHEMBL257616 | — | EC50 | = | 1922.0 | nM | 5.72 |
| CHEMBL257615 | — | EC50 | = | 3702.0 | nM | 5.43 |