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Assay Detail

CHEMBL840252

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Binding
Effective concentration for mouse Melanocortin-4 receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocortin receptor 4 (CHEMBL3719)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
Wilczynski A, Wilson KR, Scott JW, Edison AS, Haskell-Luevano C.
J Med Chem (2005) 48 : 3060 -3075
PubMed 15828845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 7.99 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430239 MELATONAN 1 10.28
CHEMBL2369959 1 9.89
CHEMBL441738 AFAMELANOTIDE 4.0 1 9.80
CHEMBL2369963 1 9.57
CHEMBL2369967 1 9.44
CHEMBL2369975 1 9.24
CHEMBL2369982 1 9.24
CHEMBL2369971 1 9.20
CHEMBL2369960 1 9.19
CHEMBL2369983 1 9.18
CHEMBL2369964 1 9.17
CHEMBL214332 INTERMEDINE 2.0 1 8.71
CHEMBL2369969 1 7.49
CHEMBL2369965 1 7.37
CHEMBL2369961 1 6.94
CHEMBL2369966 1 6.58
CHEMBL2369970 1 6.15
CHEMBL2369976 1 5.37
CHEMBL2369962 1 5.14
CHEMBL2369977 1 5.07
CHEMBL2369972 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430239 MELATONAN EC50 = 0.053 nM 10.28
CHEMBL2369959 EC50 = 0.13 nM 9.89
CHEMBL441738 AFAMELANOTIDE EC50 = 0.16 nM 9.80
CHEMBL2369963 EC50 = 0.27 nM 9.57
CHEMBL2369967 EC50 = 0.36 nM 9.44
CHEMBL2369975 EC50 = 0.57 nM 9.24
CHEMBL2369982 EC50 = 0.57 nM 9.24
CHEMBL2369971 EC50 = 0.63 nM 9.20
CHEMBL2369960 EC50 = 0.64 nM 9.19
CHEMBL2369983 EC50 = 0.66 nM 9.18
CHEMBL2369964 EC50 = 0.67 nM 9.17
CHEMBL214332 INTERMEDINE EC50 = 1.93 nM 8.71
CHEMBL2369969 EC50 = 32.5 nM 7.49
CHEMBL2369965 EC50 = 42.6 nM 7.37
CHEMBL2369961 EC50 = 115.0 nM 6.94
CHEMBL2369966 EC50 = 260.0 nM 6.58
CHEMBL2369970 EC50 = 710.0 nM 6.15
CHEMBL2369976 EC50 = 4300.0 nM 5.37
CHEMBL2369962 EC50 = 7200.0 nM 5.14
CHEMBL2369977 EC50 = 8600.0 nM 5.07
CHEMBL2369972 EC50 = 16700.0 nM 4.78