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Assay Detail

CHEMBL716497

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Binding
The concentration that inhibits 50% specific binding was determined against the Melanocortin 1 receptor
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Melanocyte-stimulating hormone receptor (CHEMBL3795)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
Haskell-Luevano C, Boteju LW, Miwa H, Dickinson C, Gantz I, Yamada T, Hadley ME, Hruby VJ.
J Med Chem (1995) 38 : 4720 -4729
PubMed 7473600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.84 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430239 MELATONAN 2 9.40
CHEMBL2364555 1 9.30
CHEMBL2370906 1 8.70
CHEMBL3350330 1 8.52
CHEMBL2364550 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430239 MELATONAN IC50 = 0.4 nM 9.40
CHEMBL430239 MELATONAN IC50 = 0.5 nM 9.30
CHEMBL2364555 IC50 = 0.5 nM 9.30
CHEMBL2370906 IC50 = 2.0 nM 8.70
CHEMBL3350330 IC50 = 3.0 nM 8.52
CHEMBL2364550 IC50 = 15.0 nM 7.82