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Assay Detail

CHEMBL4731050

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at mouse MC5R assessed as antagonist potency by alphascreen cAMP assay
4
Total Activities
4
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

Target

Melanocortin receptor 5 (CHEMBL4489)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Peptoid NPhe in AGRP-Based c[Pro-Arg-Phe-Phe-Xxx-Ala-Phe-DPro] Scaffolds Maintain Mouse MC4R Antagonist Potency.
Ericson MD,Freeman KT,Haskell-Luevano C
ACS Med Chem Lett (2020) 11 : 1942 -1948
PubMed 33062177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 6.85 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4102048 1 7.50
CHEMBL4747952 1 7.40
CHEMBL3577981 1 6.40
CHEMBL4740561 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4102048 Kd = 31.62 nM 7.50
CHEMBL4747952 Kd = 39.81 nM 7.40
CHEMBL3577981 Kd = 398.11 nM 6.40
CHEMBL4740561 Kd = 794.33 nM 6.10