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Assay Detail

CHEMBL919366

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

Binding
Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent and selective agonists of human melanocortin receptor 5: cyclic analogues of alpha-melanocyte-stimulating hormone.
Bednarek MA, MacNeil T, Tang R, Fong TM, Cabello MA, Maroto M, Teran A.
J Med Chem (2007) 50 : 2520 -2526
PubMed 17455928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.92 7.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2371964 1 7.13
CHEMBL2371966 1 6.80
CHEMBL2371962 1 6.24
CHEMBL389674 1 6.23
CHEMBL2371967 1 6.14
CHEMBL2371971 1 6.00
CHEMBL2371963 1 6.00
CHEMBL438118 1 5.92
CHEMBL2371973 1 5.80
CHEMBL375947 1 5.80
CHEMBL227239 1 5.44
CHEMBL376339 1 5.35
CHEMBL2371969 1 5.33
CHEMBL2371965 1 5.33
CHEMBL438294 1 5.32
CHEMBL2371970 1 -
CHEMBL2371968 1 -
CHEMBL426904 1 -
CHEMBL223427 1 -
CHEMBL223394 1 -
CHEMBL434372 1 -
CHEMBL426756 1 -
CHEMBL373726 1 -
CHEMBL373727 1 -
CHEMBL228194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2371964 IC50 = 74.0 nM 7.13
CHEMBL2371966 IC50 = 160.0 nM 6.80
CHEMBL2371962 IC50 = 570.0 nM 6.24
CHEMBL389674 IC50 = 590.0 nM 6.23
CHEMBL2371967 IC50 = 720.0 nM 6.14
CHEMBL2371971 IC50 = 990.0 nM 6.00
CHEMBL2371963 IC50 = 1000.0 nM 6.00
CHEMBL438118 IC50 = 1200.0 nM 5.92
CHEMBL2371973 IC50 = 1600.0 nM 5.80
CHEMBL375947 IC50 = 1600.0 nM 5.80
CHEMBL227239 IC50 = 3600.0 nM 5.44
CHEMBL376339 IC50 = 4500.0 nM 5.35
CHEMBL2371969 IC50 = 4700.0 nM 5.33
CHEMBL2371965 IC50 = 4700.0 nM 5.33
CHEMBL438294 IC50 = 4800.0 nM 5.32
CHEMBL2371970 IC50 > 10000.0 nM -
CHEMBL2371968 IC50 > 5000.0 nM -
CHEMBL426904 IC50 > 10000.0 nM -
CHEMBL223427 IC50 > 10000.0 nM -
CHEMBL223394 IC50 > 10000.0 nM -
CHEMBL434372 IC50 > 10000.0 nM -
CHEMBL426756 IC50 > 5000.0 nM -
CHEMBL373726 IC50 > 10000.0 nM -
CHEMBL373727 IC50 > 10000.0 nM -
CHEMBL228194 IC50 > 10000.0 nM -