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Assay Detail

CHEMBL4357467

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Functional
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
3
Total Activities
3
Compounds Tested
1
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

Target

Melanocyte-stimulating hormone receptor (CHEMBL4077)
Type SINGLE PROTEIN
Organism Mus musculus

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.
Koerperich ZM, Ericson MD, Freeman KT, Speth RC, Pogozheva ID, Mosberg HI, Haskell-Luevano C.
J Med Chem (2020) 63 : 2194 -2208
PubMed 31845801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.20 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441738 AFAMELANOTIDE 4.0 1 11.00
CHEMBL4541505 1 5.40
CHEMBL4466724 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441738 AFAMELANOTIDE EC50 = 0.01 nM 11.00
CHEMBL4541505 EC50 = 4000.0 nM 5.40
CHEMBL4466724 EC50 > 100000.0 nM -