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Assay Detail

CHEMBL973607

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Functional
Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands.
Marinkovic D, Tucci FC, Tran JA, Fleck BA, Wen J, Chen C.
Bioorg Med Chem Lett (2008) 18 : 4817 -4822
PubMed 18682322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.46 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511826 1 6.60
CHEMBL454916 1 6.60
CHEMBL513404 1 6.58
CHEMBL454900 1 6.40
CHEMBL471340 1 6.38
CHEMBL460942 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511826 IC50 = 250.0 nM 6.60
CHEMBL454916 IC50 = 250.0 nM 6.60
CHEMBL513404 IC50 = 260.0 nM 6.58
CHEMBL454900 IC50 = 400.0 nM 6.40
CHEMBL471340 IC50 = 420.0 nM 6.38
CHEMBL460942 IC50 = 650.0 nM 6.19