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Assay Detail

CHEMBL828129

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Functional
In vitro agonist potency for Mouse Melanocortin 5 receptor
16
Total Activities
16
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

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

Publication

N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
Todorovic A, Holder JR, Bauzo RM, Scott JW, Kavanagh R, Abdel-Malek Z, Haskell-Luevano C.
J Med Chem (2005) 48 : 3328 -3336
PubMed 15857138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 8.75 10.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441738 AFAMELANOTIDE 4.0 1 10.11
CHEMBL2371851 1 9.80
CHEMBL191303 1 9.24
CHEMBL214332 INTERMEDINE 2.0 1 9.15
CHEMBL195439 1 9.06
CHEMBL364726 1 8.61
CHEMBL370254 1 8.56
CHEMBL191304 1 8.55
CHEMBL264190 1 8.52
CHEMBL193151 1 8.52
CHEMBL265236 1 8.52
CHEMBL370261 1 8.47
CHEMBL190366 1 8.35
CHEMBL426282 1 8.32
CHEMBL195468 1 8.20
CHEMBL194217 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441738 AFAMELANOTIDE EC50 = 0.078 nM 10.11
CHEMBL2371851 EC50 = 0.16 nM 9.80
CHEMBL191303 EC50 = 0.57 nM 9.24
CHEMBL214332 INTERMEDINE EC50 = 0.7 nM 9.15
CHEMBL195439 EC50 = 0.88 nM 9.06
CHEMBL364726 EC50 = 2.43 nM 8.61
CHEMBL370254 EC50 = 2.78 nM 8.56
CHEMBL191304 EC50 = 2.82 nM 8.55
CHEMBL264190 EC50 = 3.02 nM 8.52
CHEMBL193151 EC50 = 3.02 nM 8.52
CHEMBL265236 EC50 = 2.99 nM 8.52
CHEMBL370261 EC50 = 3.39 nM 8.47
CHEMBL190366 EC50 = 4.43 nM 8.35
CHEMBL426282 EC50 = 4.83 nM 8.32
CHEMBL195468 EC50 = 6.3 nM 8.20
CHEMBL194217 EC50 = 10.0 nM 8.00