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Assay Detail

CHEMBL717325

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Functional
Effective concentration against mouse Melanocortin 1 receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
Wilczynski A, Wang XS, Joseph CG, Xiang Z, Bauzo RM, Scott JW, Sorensen NB, Shaw AM, Millard WJ, Richards NG, Haskell-Luevano C.
J Med Chem (2004) 47 : 2194 -2207
PubMed 15084118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.09 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216295 1 10.70
CHEMBL269274 1 9.80
CHEMBL2369484 1 9.68
CHEMBL441738 AFAMELANOTIDE 4.0 1 9.42
CHEMBL214332 INTERMEDINE 2.0 1 9.26
CHEMBL2369485 1 7.22
CHEMBL2370695 1 5.76
CHEMBL406550 1 5.31
CHEMBL409190 1 5.29
CHEMBL410091 1 5.21
CHEMBL2371699 1 4.88
CHEMBL413465 1 4.87
CHEMBL440633 1 4.71
CHEMBL266288 1 -
CHEMBL428134 1 -
CHEMBL2369483 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216295 EC50 = 0.02 nM 10.70
CHEMBL269274 EC50 = 0.16 nM 9.80
CHEMBL2369484 EC50 = 0.21 nM 9.68
CHEMBL441738 AFAMELANOTIDE EC50 = 0.38 nM 9.42
CHEMBL214332 INTERMEDINE EC50 = 0.55 nM 9.26
CHEMBL2369485 EC50 = 59.5 nM 7.22
CHEMBL2370695 EC50 = 1730.0 nM 5.76
CHEMBL406550 EC50 = 4850.0 nM 5.31
CHEMBL409190 EC50 = 5120.0 nM 5.29
CHEMBL410091 EC50 = 6120.0 nM 5.21
CHEMBL2371699 EC50 = 13300.0 nM 4.88
CHEMBL413465 EC50 = 13500.0 nM 4.87
CHEMBL440633 EC50 = 19700.0 nM 4.71
CHEMBL266288 EC50 > 100000.0 nM -
CHEMBL428134 EC50 > 100000.0 nM -
CHEMBL2369483 EC50 > 100000.0 nM -