Assay Detail
Functional
CHEMBL4041394
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at the Melanocortin-5 Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 24 | 7.17 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4102048 | — | — | 1 | 8.70 |
| CHEMBL4071633 | — | — | 1 | 8.58 |
| CHEMBL4104582 | — | — | 1 | 8.30 |
| CHEMBL3577981 | — | — | 1 | 8.20 |
| CHEMBL4075125 | — | — | 1 | 8.20 |
| CHEMBL4065443 | — | — | 1 | 8.16 |
| CHEMBL4072662 | — | — | 1 | 7.76 |
| CHEMBL4101128 | — | — | 1 | 7.70 |
| CHEMBL4066929 | — | — | 1 | 7.34 |
| CHEMBL4077783 | — | — | 1 | 7.32 |
| CHEMBL4083137 | — | — | 1 | 7.30 |
| CHEMBL4098651 | — | — | 1 | 7.00 |
| CHEMBL4086679 | — | — | 1 | 6.90 |
| CHEMBL4067947 | — | — | 1 | 6.81 |
| CHEMBL4093379 | — | — | 1 | 6.79 |
| CHEMBL4089149 | — | — | 1 | 6.63 |
| CHEMBL4087835 | — | — | 1 | 6.18 |
| CHEMBL4093505 | — | — | 1 | 6.11 |
| CHEMBL4066514 | — | — | 1 | 6.10 |
| CHEMBL4072797 | — | — | 1 | 6.07 |
| CHEMBL4094419 | — | — | 1 | 5.90 |
| CHEMBL4095539 | — | — | 1 | 5.71 |
| CHEMBL4096856 | — | — | 1 | - |
| CHEMBL4078828 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4102048 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL4071633 | — | Kd | = | 2.63 | nM | 8.58 |
| CHEMBL4104582 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL3577981 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL4075125 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL4065443 | — | Kd | = | 6.918 | nM | 8.16 |
| CHEMBL4072662 | — | Kd | = | 17.38 | nM | 7.76 |
| CHEMBL4101128 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL4066929 | — | Kd | = | 45.71 | nM | 7.34 |
| CHEMBL4077783 | — | Kd | = | 47.86 | nM | 7.32 |
| CHEMBL4083137 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL4098651 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL4086679 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL4067947 | — | Kd | = | 154.88 | nM | 6.81 |
| CHEMBL4093379 | — | Kd | = | 162.18 | nM | 6.79 |
| CHEMBL4089149 | — | Kd | = | 234.42 | nM | 6.63 |
| CHEMBL4087835 | — | Kd | = | 660.69 | nM | 6.18 |
| CHEMBL4093505 | — | Kd | = | 776.25 | nM | 6.11 |
| CHEMBL4066514 | — | Kd | = | 794.33 | nM | 6.10 |
| CHEMBL4072797 | — | Kd | = | 851.14 | nM | 6.07 |
| CHEMBL4094419 | — | Kd | = | 1258.93 | nM | 5.90 |
| CHEMBL4095539 | — | Kd | = | 1949.84 | nM | 5.71 |
| CHEMBL4096856 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4078828 | — | Kd | > | 3162.28 | nM | - |