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Assay Detail

CHEMBL853052

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

Functional
Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Melanocortin receptor 4 (CHEMBL259)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
Hogan K, Peluso S, Gould S, Parsons I, Ryan D, Wu L, Visiers I.
J Med Chem (2006) 49 : 911 -922
PubMed 16451057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.26 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267492 1 8.06
CHEMBL40711 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267492 IC50 = 8.8 nM 8.06
CHEMBL40711 IC50 = 355.0 nM 6.45