Assay Detail
Binding
CHEMBL925938
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Binding affinity to human MC5R
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| IC50 | 7 | 6.63 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429854 | — | — | 1 | 7.18 |
| CHEMBL254589 | — | — | 1 | 6.89 |
| CHEMBL257759 | — | — | 1 | 6.69 |
| CHEMBL254757 | — | — | 1 | 6.61 |
| CHEMBL255286 | — | — | 1 | 6.55 |
| CHEMBL402769 | — | — | 1 | 6.35 |
| CHEMBL403420 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429854 | — | IC50 | = | 65.3 | nM | 7.18 |
| CHEMBL254589 | — | IC50 | = | 129.4 | nM | 6.89 |
| CHEMBL257759 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL254757 | — | IC50 | = | 245.4 | nM | 6.61 |
| CHEMBL255286 | — | IC50 | = | 280.3 | nM | 6.55 |
| CHEMBL402769 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL403420 | — | IC50 | = | 675.0 | nM | 6.17 |