Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL832206

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

Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocortin receptor 4 (CHEMBL259)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.
Bakshi RK, Hong Q, Olson JT, Ye Z, Sebhat IK, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Martin WJ, Strack A, McGowan E, Tamvakopoulos C, Miller RR, Stearns RA, Tang W, Maclntyre DE, van der Ploeg LH, Patchett AA, Nargund RP.
Bioorg Med Chem Lett (2005) 15 : 3430 -3433
PubMed 15951175 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 9.05 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL433764 1 9.43
CHEMBL362523 1 9.25
CHEMBL360818 1 9.11
CHEMBL2113041 1 8.96
CHEMBL360819 1 8.96
CHEMBL339053 1 8.92
CHEMBL187990 1 8.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL433764 IC50 = 0.37 nM 9.43
CHEMBL362523 IC50 = 0.56 nM 9.25
CHEMBL360818 IC50 = 0.77 nM 9.11
CHEMBL2113041 IC50 = 1.1 nM 8.96
CHEMBL360819 IC50 = 1.1 nM 8.96
CHEMBL339053 IC50 = 1.2 nM 8.92
CHEMBL187990 IC50 = 1.9 nM 8.72