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Assay Detail

CHEMBL840253

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Binding
Effective concentration for mouse Melanocortin-5 receptor
26
Total Activities
26
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 5 (CHEMBL4489)
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 26 8.00 10.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430239 MELATONAN 1 10.17
CHEMBL441738 AFAMELANOTIDE 4.0 1 10.02
CHEMBL214332 INTERMEDINE 2.0 1 9.49
CHEMBL2369959 1 9.43
CHEMBL2369967 1 9.34
CHEMBL2369964 1 9.02
CHEMBL2369963 1 8.71
CHEMBL2369969 1 8.69
CHEMBL2096742 1 8.64
CHEMBL2369973 1 8.63
CHEMBL2369960 1 8.50
CHEMBL2369982 1 8.50
CHEMBL2369965 1 8.46
CHEMBL2369983 1 8.31
CHEMBL2369975 1 8.28
CHEMBL2369971 1 8.14
CHEMBL2369974 1 7.65
CHEMBL2369966 1 7.37
CHEMBL2369970 1 7.30
CHEMBL2369961 1 6.36
CHEMBL2369962 1 6.16
CHEMBL2369968 1 6.16
CHEMBL2369977 1 6.10
CHEMBL2369976 1 5.50
CHEMBL2369972 1 5.10
CHEMBL2096710 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430239 MELATONAN EC50 = 0.068 nM 10.17
CHEMBL441738 AFAMELANOTIDE EC50 = 0.095 nM 10.02
CHEMBL214332 INTERMEDINE EC50 = 0.32 nM 9.49
CHEMBL2369959 EC50 = 0.37 nM 9.43
CHEMBL2369967 EC50 = 0.46 nM 9.34
CHEMBL2369964 EC50 = 0.95 nM 9.02
CHEMBL2369963 EC50 = 1.93 nM 8.71
CHEMBL2369969 EC50 = 2.06 nM 8.69
CHEMBL2096742 EC50 = 2.31 nM 8.64
CHEMBL2369973 EC50 = 2.33 nM 8.63
CHEMBL2369960 EC50 = 3.15 nM 8.50
CHEMBL2369982 EC50 = 3.13 nM 8.50
CHEMBL2369965 EC50 = 3.43 nM 8.46
CHEMBL2369983 EC50 = 4.87 nM 8.31
CHEMBL2369975 EC50 = 5.27 nM 8.28
CHEMBL2369971 EC50 = 7.16 nM 8.14
CHEMBL2369974 EC50 = 22.3 nM 7.65
CHEMBL2369966 EC50 = 42.7 nM 7.37
CHEMBL2369970 EC50 = 50.1 nM 7.30
CHEMBL2369961 EC50 = 440.0 nM 6.36
CHEMBL2369962 EC50 = 700.0 nM 6.16
CHEMBL2369968 EC50 = 690.0 nM 6.16
CHEMBL2369977 EC50 = 800.0 nM 6.10
CHEMBL2369976 EC50 = 3200.0 nM 5.50
CHEMBL2369972 EC50 = 7900.0 nM 5.10
CHEMBL2096710 EC50 > 100000.0 nM -