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Assay Detail

CHEMBL1694296

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Functional
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
9
Total Activities
9
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 Autocuration

Target

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

Publication

Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR.
Singh A, Wilczynski A, Holder JR, Witek RM, Dirain ML, Xiang Z, Edison AS, Haskell-Luevano C.
J Med Chem (2011) 54 : 1379 -1390
PubMed 21306168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.06 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441738 AFAMELANOTIDE 4.0 1 10.52
CHEMBL1688107 1 8.64
CHEMBL1688110 1 7.14
CHEMBL1688104 1 6.52
CHEMBL1688108 1 6.47
CHEMBL1688105 1 6.41
CHEMBL1688111 1 6.03
CHEMBL1688106 1 6.00
CHEMBL1688109 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441738 AFAMELANOTIDE EC50 = 0.03 nM 10.52
CHEMBL1688107 EC50 = 2.3 nM 8.64
CHEMBL1688110 EC50 = 72.0 nM 7.14
CHEMBL1688104 EC50 = 305.0 nM 6.52
CHEMBL1688108 EC50 = 335.0 nM 6.47
CHEMBL1688105 EC50 = 390.0 nM 6.41
CHEMBL1688111 EC50 = 925.0 nM 6.03
CHEMBL1688106 EC50 = 990.0 nM 6.00
CHEMBL1688109 EC50 = 1595.0 nM 5.80