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Assay Detail

CHEMBL716474

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism frog
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
EC50 7 9.52 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3350330 1 10.22
CHEMBL430239 MELATONAN 2 10.00
CHEMBL214332 INTERMEDINE 2.0 1 10.00
CHEMBL2370906 1 9.52
CHEMBL2364555 1 9.36
CHEMBL2364550 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3350330 EC50 = 0.06 nM 10.22
CHEMBL430239 MELATONAN EC50 = 0.1 nM 10.00
CHEMBL430239 MELATONAN EC50 = 0.1 nM 10.00
CHEMBL214332 INTERMEDINE EC50 = 0.1 nM 10.00
CHEMBL2370906 EC50 = 0.3 nM 9.52
CHEMBL2364555 EC50 = 0.44 nM 9.36
CHEMBL2364550 EC50 = 28.6 nM 7.54