Assay Detail
Functional
CHEMBL4041386
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse melanocortin receptor 3 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 | 6.15 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071633 | — | — | 1 | 6.70 |
| CHEMBL4102048 | — | — | 1 | 6.52 |
| CHEMBL4104582 | — | — | 1 | 6.46 |
| CHEMBL4072662 | — | — | 1 | 6.40 |
| CHEMBL3577981 | — | — | 1 | 6.30 |
| CHEMBL4075125 | — | — | 1 | 6.20 |
| CHEMBL4065443 | — | — | 1 | 6.10 |
| CHEMBL4101128 | — | — | 1 | 5.90 |
| CHEMBL4095539 | — | — | 1 | 5.72 |
| CHEMBL4066929 | — | — | 1 | 5.70 |
| CHEMBL4067947 | — | — | 1 | 5.70 |
| CHEMBL4093379 | — | — | 1 | - |
| CHEMBL4086679 | — | — | 1 | - |
| CHEMBL4083137 | — | — | 1 | - |
| CHEMBL4066514 | — | — | 1 | - |
| CHEMBL4087835 | — | — | 1 | - |
| CHEMBL4098651 | — | — | 1 | - |
| CHEMBL4072797 | — | — | 1 | - |
| CHEMBL4093505 | — | — | 1 | - |
| CHEMBL4078828 | — | — | 1 | - |
| CHEMBL4096856 | — | — | 1 | - |
| CHEMBL4089149 | — | — | 1 | - |
| CHEMBL4094419 | — | — | 1 | - |
| CHEMBL4077783 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071633 | — | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL4102048 | — | Kd | = | 302.0 | nM | 6.52 |
| CHEMBL4104582 | — | Kd | = | 346.74 | nM | 6.46 |
| CHEMBL4072662 | — | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL3577981 | — | Kd | = | 501.19 | nM | 6.30 |
| CHEMBL4075125 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL4065443 | — | Kd | = | 794.33 | nM | 6.10 |
| CHEMBL4101128 | — | Kd | = | 1258.93 | nM | 5.90 |
| CHEMBL4095539 | — | Kd | = | 1905.46 | nM | 5.72 |
| CHEMBL4066929 | — | Kd | = | 1995.26 | nM | 5.70 |
| CHEMBL4067947 | — | Kd | = | 1995.26 | nM | 5.70 |
| CHEMBL4093379 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4086679 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4083137 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4066514 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4087835 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4098651 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4072797 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4093505 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4078828 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4096856 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4089149 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4094419 | — | Kd | > | 3162.28 | nM | - |
| CHEMBL4077783 | — | Kd | > | 3162.28 | nM | - |