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Assay Detail

CHEMBL4482751

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

Binding
Inhibition of ACAT2 in human HepG2 cells using NBD22-labeled sterol as substrate incubated for 6 hrs by fluorescence based assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sterol O-acyltransferase 2 (CHEMBL4465)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Class of tricyclic analogue, preparation method and use thereof
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.90 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4553029 1 7.64
CHEMBL4565264 1 7.16
CHEMBL4585060 1 7.11
CHEMBL4519710 1 7.09
CHEMBL4536996 1 7.07
CHEMBL4555013 1 7.07
CHEMBL4539524 1 6.99
CHEMBL4554131 1 6.82
CHEMBL4518651 1 6.75
CHEMBL4569948 1 6.61
CHEMBL4555697 1 6.36
CHEMBL4554239 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4553029 IC50 = 23.0 nM 7.64
CHEMBL4565264 IC50 = 69.0 nM 7.16
CHEMBL4585060 IC50 = 78.0 nM 7.11
CHEMBL4519710 IC50 = 81.0 nM 7.09
CHEMBL4536996 IC50 = 86.0 nM 7.07
CHEMBL4555013 IC50 = 86.0 nM 7.07
CHEMBL4539524 IC50 = 103.0 nM 6.99
CHEMBL4554131 IC50 = 152.0 nM 6.82
CHEMBL4518651 IC50 = 179.0 nM 6.75
CHEMBL4569948 IC50 = 245.0 nM 6.61
CHEMBL4555697 IC50 = 433.0 nM 6.36
CHEMBL4554239 IC50 = 831.0 nM 6.08