Assay Detail
Functional
CHEMBL925941
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Agonist activity at human MC3R expressed in CHO cells assessed as cAMP release
4
Total Activities
4
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 | 4 | 6.61 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429854 | — | — | 1 | 7.01 |
| CHEMBL257759 | — | — | 1 | 6.80 |
| CHEMBL254589 | — | — | 1 | 6.60 |
| CHEMBL255286 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429854 | — | EC50 | = | 97.4 | nM | 7.01 |
| CHEMBL257759 | — | EC50 | = | 156.7 | nM | 6.80 |
| CHEMBL254589 | — | EC50 | = | 249.9 | nM | 6.60 |
| CHEMBL255286 | — | EC50 | = | 917.5 | nM | 6.04 |