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Assay Detail

CHEMBL717326

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

Functional
Maximal agonist response of mouse melanocortin 1 receptor (MC1R)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.
Han G, Haskell-Luevano C, Kendall L, Bonner G, Hadley ME, Cone RD, Hruby VJ.
J Med Chem (2004) 47 : 1514 -1526
PubMed 14998337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 8.52 10.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441738 AFAMELANOTIDE 4.0 1 10.34
CHEMBL414965 1 10.33
CHEMBL405087 1 9.64
CHEMBL406842 1 9.43
CHEMBL410404 1 8.82
CHEMBL407845 1 8.52
CHEMBL406891 1 8.29
CHEMBL411400 1 8.16
CHEMBL405791 1 7.66
CHEMBL411378 1 7.46
CHEMBL415200 1 7.33
CHEMBL2372365 1 6.31
CHEMBL427814 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441738 AFAMELANOTIDE EC50 = 0.046 nM 10.34
CHEMBL414965 EC50 = 0.047 nM 10.33
CHEMBL405087 EC50 = 0.23 nM 9.64
CHEMBL406842 EC50 = 0.37 nM 9.43
CHEMBL410404 EC50 = 1.5 nM 8.82
CHEMBL407845 EC50 = 3.0 nM 8.52
CHEMBL406891 EC50 = 5.1 nM 8.29
CHEMBL411400 EC50 = 6.9 nM 8.16
CHEMBL405791 EC50 = 22.0 nM 7.66
CHEMBL411378 EC50 = 35.0 nM 7.46
CHEMBL415200 EC50 = 47.0 nM 7.33
CHEMBL2372365 EC50 = 490.0 nM 6.31
CHEMBL427814 EC50 = - nM -