Assay Detail
Binding
CHEMBL925930
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells
20
Total Activities
20
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
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 | 20 | 7.51 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254757 | — | — | 1 | 8.48 |
| CHEMBL429854 | — | — | 1 | 8.40 |
| CHEMBL255286 | — | — | 1 | 8.39 |
| CHEMBL254589 | — | — | 1 | 8.21 |
| CHEMBL402769 | — | — | 1 | 8.11 |
| CHEMBL256526 | — | — | 1 | 8.01 |
| CHEMBL257759 | — | — | 1 | 7.95 |
| CHEMBL254792 | — | — | 1 | 7.88 |
| CHEMBL254351 | — | — | 1 | 7.75 |
| CHEMBL403421 | — | — | 1 | 7.64 |
| CHEMBL403834 | — | — | 1 | 7.55 |
| CHEMBL402009 | — | — | 1 | 7.43 |
| CHEMBL404696 | — | — | 1 | 7.16 |
| CHEMBL403420 | — | — | 1 | 7.12 |
| CHEMBL403556 | — | — | 1 | 7.08 |
| CHEMBL257615 | — | — | 1 | 7.00 |
| CHEMBL257770 | — | — | 1 | 6.89 |
| CHEMBL404905 | — | — | 1 | 6.67 |
| CHEMBL257616 | — | — | 1 | 6.28 |
| CHEMBL256286 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254757 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL429854 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL255286 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL254589 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL402769 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL256526 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL257759 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL254792 | — | IC50 | = | 13.23 | nM | 7.88 |
| CHEMBL254351 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL403421 | — | IC50 | = | 22.7 | nM | 7.64 |
| CHEMBL403834 | — | IC50 | = | 28.1 | nM | 7.55 |
| CHEMBL402009 | — | IC50 | = | 37.2 | nM | 7.43 |
| CHEMBL404696 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL403420 | — | IC50 | = | 76.2 | nM | 7.12 |
| CHEMBL403556 | — | IC50 | = | 82.2 | nM | 7.08 |
| CHEMBL257615 | — | IC50 | = | 101.1 | nM | 7.00 |
| CHEMBL257770 | — | IC50 | = | 127.6 | nM | 6.89 |
| CHEMBL404905 | — | IC50 | = | 216.2 | nM | 6.67 |
| CHEMBL257616 | — | IC50 | = | 528.0 | nM | 6.28 |
| CHEMBL256286 | — | IC50 | = | 640.0 | nM | 6.19 |