Assay Detail
Functional
CHEMBL4357478
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin-5 Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 6.52 | 7.30 |
| pA2 | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4102048 | — | — | 1 | 7.30 |
| CHEMBL4566163 | — | — | 1 | 6.50 |
| CHEMBL3577981 | — | — | 1 | 6.40 |
| CHEMBL4565367 | — | — | 1 | 6.30 |
| CHEMBL4538274 | — | — | 1 | 6.10 |
| CHEMBL4587214 | — | — | 1 | - |
| CHEMBL4466724 | — | — | 1 | - |
| CHEMBL4474215 | — | — | 1 | - |
| CHEMBL4531291 | — | — | 1 | - |
| CHEMBL4541505 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4102048 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL4566163 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL3577981 | — | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL4565367 | — | Kd | = | 501.19 | nM | 6.30 |
| CHEMBL4538274 | — | Kd | = | 794.33 | nM | 6.10 |
| CHEMBL4587214 | — | pA2 | - | — | - | |
| CHEMBL4466724 | — | pA2 | - | — | - | |
| CHEMBL4474215 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4531291 | — | pA2 | - | — | - | |
| CHEMBL4541505 | — | pA2 | - | — | - |