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Assay Detail

CHEMBL1046285

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

Binding
Displacement of [35S](2S,3S,4S,5R,6S)-6-(4-((2S,3R)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-1-(4-(3-(methylsulfonamido)prop-1-ynyl)phenyl)-4-oxoazetidin-2-yl)phenoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid from human intestinal brush border membrane NPC1L1 by single tube filtration assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

NPC1-like intracellular cholesterol transporter 1 (CHEMBL2027)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Multiple strategies for the preparation of a sulfur-35 labeled NPC1L1 radioligand.
Simeone JP, Braun MP, Leone JF, Lin P, DeVita RJ, Garcia-Calvo M, Bull HG, Lisnock J, Dean DC.
Bioorg Med Chem Lett (2009) 19 : 5033 -5036
PubMed 19631535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.61 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL578400 1 8.40
CHEMBL578401 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL578400 IC50 = 4.0 nM 8.40
CHEMBL578401 IC50 = 150.0 nM 6.82