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Assay Detail

CHEMBL1027336

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

Binding
Inhibition of ACAT in human HepG2 cells
20
Total Activities
20
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 Intermediate

Target

Sterol O-acyltransferase 1 (CHEMBL2782)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 1,4-diarylpiperidine-4-methylureas as anti-hyperlipidemic agents: dual effectors on acyl-CoA:cholesterol O-acyltransferase and low-density lipoprotein receptor expression.
Asano S, Ban H, Kino K, Ioriya K, Muraoka M.
Bioorg Med Chem Lett (2009) 19 : 1062 -1065
PubMed 19167888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.13 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL454397 1 7.51
CHEMBL449832 1 7.50
CHEMBL453491 1 7.50
CHEMBL459999 1 7.46
CHEMBL500498 1 7.43
CHEMBL449977 1 7.40
CHEMBL501429 1 7.37
CHEMBL510453 1 7.33
CHEMBL442567 1 7.32
CHEMBL503766 1 7.32
CHEMBL447674 1 7.31
CHEMBL509834 1 7.17
CHEMBL443151 1 7.11
CHEMBL448407 1 7.09
CHEMBL499122 1 7.09
CHEMBL364823 1 6.85
CHEMBL101309 AVASIMIBE 2.0 1 6.32
CHEMBL459998 1 6.26
CHEMBL459791 1 6.18
CHEMBL517393 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL454397 IC50 = 31.0 nM 7.51
CHEMBL449832 IC50 = 32.0 nM 7.50
CHEMBL453491 IC50 = 32.0 nM 7.50
CHEMBL459999 IC50 = 35.0 nM 7.46
CHEMBL500498 IC50 = 37.0 nM 7.43
CHEMBL449977 IC50 = 40.0 nM 7.40
CHEMBL501429 IC50 = 43.0 nM 7.37
CHEMBL510453 IC50 = 47.0 nM 7.33
CHEMBL442567 IC50 = 48.0 nM 7.32
CHEMBL503766 IC50 = 48.0 nM 7.32
CHEMBL447674 IC50 = 49.0 nM 7.31
CHEMBL509834 IC50 = 68.0 nM 7.17
CHEMBL443151 IC50 = 77.0 nM 7.11
CHEMBL448407 IC50 = 82.0 nM 7.09
CHEMBL499122 IC50 = 81.0 nM 7.09
CHEMBL364823 IC50 = 142.0 nM 6.85
CHEMBL101309 AVASIMIBE IC50 = 479.0 nM 6.32
CHEMBL459998 IC50 = 547.0 nM 6.26
CHEMBL459791 IC50 = 664.0 nM 6.18
CHEMBL517393 IC50 > 1000.0 nM -