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Assay Detail

CHEMBL828399

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

Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 1 receptor expressed in HEK293 cells; (N = 4)
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
Cai M, Mayorov AV, Cabello C, Stankova M, Trivedi D, Hruby VJ.
J Med Chem (2005) 48 : 1839 -1848
PubMed 15771429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.61 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414778 1 9.80
CHEMBL413439 1 9.52
CHEMBL214332 INTERMEDINE 2.0 1 9.40
CHEMBL443071 1 9.30
CHEMBL438920 1 9.15
CHEMBL2096759 1 9.00
CHEMBL437050 2 8.92
CHEMBL2371712 1 8.70
CHEMBL2310901 1 7.70
CHEMBL411359 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414778 IC50 = 0.16 nM 9.80
CHEMBL413439 IC50 = 0.3 nM 9.52
CHEMBL214332 INTERMEDINE IC50 = 0.4 nM 9.40
CHEMBL443071 IC50 = 0.5 nM 9.30
CHEMBL438920 IC50 = 0.7 nM 9.15
CHEMBL2096759 IC50 = 1.0 nM 9.00
CHEMBL437050 IC50 = 1.2 nM 8.92
CHEMBL2371712 IC50 = 2.0 nM 8.70
CHEMBL2310901 IC50 = 20.0 nM 7.70
CHEMBL411359 IC50 = 60.0 nM 7.22
CHEMBL437050 IC50 = 1000.0 nM 6.00