Assay Detail
Binding
CHEMBL5356876
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Binding affinity to mouse MC4R expressed in HEK293 cells assessed as inhibition constant by schild plot analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Pan-Melanocortin Receptor Antagonist [Ac-DPhe(pI)-Arg-Nal(2')-Orn-NH<sub>2</sub>] at the MC1R, MC3R, MC4R, and MC5R that Mediates an Increased Feeding Response in Mice and a 40-Fold Selective MC1R Antagonist [Ac-DPhe(pI)-DArg-Nal(2')-Arg-NH<sub>2</sub>].
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.75 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3422426 | — | — | 1 | 9.20 |
| CHEMBL4865888 | — | — | 1 | 8.89 |
| CHEMBL5408661 | — | — | 1 | 8.89 |
| CHEMBL5403689 | — | — | 1 | 8.80 |
| CHEMBL5421386 | — | — | 1 | 8.80 |
| CHEMBL5413535 | — | — | 1 | 8.49 |
| CHEMBL5405613 | — | — | 1 | 8.20 |
| CHEMBL5419394 | — | — | 1 | 8.20 |
| CHEMBL5414015 | — | — | 1 | 8.10 |
| CHEMBL5413452 | — | — | 1 | 8.10 |
| CHEMBL5417913 | — | — | 1 | 7.80 |
| CHEMBL5406385 | — | — | 1 | 7.70 |
| CHEMBL4866219 | — | — | 1 | 7.70 |
| CHEMBL5397924 | — | — | 1 | 7.70 |
| CHEMBL5438129 | — | — | 1 | 7.00 |
| CHEMBL5397668 | — | — | 1 | 7.00 |
| CHEMBL5421355 | — | — | 1 | 6.60 |
| CHEMBL5409282 | — | — | 1 | 6.50 |
| CHEMBL5397260 | — | — | 1 | 5.80 |
| CHEMBL5435335 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3422426 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL4865888 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL5408661 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL5403689 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL5421386 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL5413535 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL5405613 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL5419394 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL5414015 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5413452 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5417913 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL5406385 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4866219 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5397924 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5438129 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5397668 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5421355 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL5409282 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL5397260 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL5435335 | — | Ki | = | 3200.0 | nM | 5.50 |