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Assay Detail

CHEMBL717322

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Functional
Agonistic activity evaluated at melanocortin 1 receptor (MC1R) of mouse HEK293 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.
Holder JR, Bauzo RM, Xiang Z, Scott J, Haskell-Luevano C.
Bioorg Med Chem Lett (2003) 13 : 4505 -4509
PubMed 14643357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.11 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214332 INTERMEDINE 2.0 1 9.22
CHEMBL264190 1 7.70
CHEMBL343094 1 6.77
CHEMBL138212 1 6.30
CHEMBL138771 1 6.11
CHEMBL140847 1 5.77
CHEMBL141497 1 5.18
CHEMBL138100 1 5.12
CHEMBL140324 1 4.57
CHEMBL138356 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214332 INTERMEDINE EC50 = 0.6 nM 9.22
CHEMBL264190 EC50 = 20.0 nM 7.70
CHEMBL343094 EC50 = 170.0 nM 6.77
CHEMBL138212 EC50 = 500.0 nM 6.30
CHEMBL138771 EC50 = 780.0 nM 6.11
CHEMBL140847 EC50 = 1700.0 nM 5.77
CHEMBL141497 EC50 = 6600.0 nM 5.18
CHEMBL138100 EC50 = 7600.0 nM 5.12
CHEMBL140324 EC50 = 27000.0 nM 4.57
CHEMBL138356 EC50 = 48000.0 nM 4.32