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Assay Detail

CHEMBL970546

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 NPC1L1 in pig enterocyte brush border membrane
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Spiroimidazolidinone NPC1L1 inhibitors. 1: Discovery by 3D-similarity-based virtual screening.
McMasters DR, Garcia-Calvo M, Maiorov V, McCann ME, Meurer RD, Bull HG, Lisnock J, Howell KL, Devita RJ.
Bioorg Med Chem Lett (2009) 19 : 2965 -2968
PubMed 19410454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.20 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL504066 1 7.89
CHEMBL321017 1 6.50
CHEMBL466849 1 -
CHEMBL468523 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL504066 IC50 = 13.0 nM 7.89
CHEMBL321017 IC50 = 320.0 nM 6.50
CHEMBL466849 IC50 > 500000.0 nM -
CHEMBL468523 IC50 > 500000.0 nM -