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Assay Detail

CHEMBL4233176

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

Binding
Inhibition of ACAT1 in mouse J774 cells assessed as reduction in esterified cholesterol accumulation after 18 hrs in presence of 25-hydroxycholesterol
ChEMBL ↗
63
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type J774
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sterol O-acyltransferase 1 (CHEMBL4464) ↗
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design, synthesis and pharmacology of aortic-selective acyl-CoA: Cholesterol O-acyltransferase (ACAT/SOAT) inhibitors.
Shibuya K, Kawamine K, Miura T, Ozaki C, Edano T, Mizuno K, Yoshinaka Y, Tsunenari Y.
Bioorg Med Chem (2018) 26 : 4001 -4013
PubMed 29945757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 63 6.04 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4247249 — — 1 8.15
CHEMBL4241747 — — 1 7.52
CHEMBL4243015 — — 1 7.40
CHEMBL4240947 — — 1 7.37
CHEMBL4245998 — — 1 7.32
CHEMBL4248936 — — 1 7.23
CHEMBL4249263 — — 1 7.00
CHEMBL4239138 — — 1 7.00
CHEMBL4249787 — — 1 7.00
CHEMBL4239248 — — 1 6.75
CHEMBL4245984 — — 1 6.75
CHEMBL4238015 — — 1 6.55
CHEMBL4248950 — — 1 6.52
CHEMBL4248172 — — 1 6.51
CHEMBL22373 CL-976 — 1 6.51
CHEMBL4238030 — — 1 6.46
CHEMBL4249719 — — 1 6.40
CHEMBL4244680 — — 1 6.39
CHEMBL4245518 — — 1 6.39
CHEMBL4244693 — — 1 6.34
CHEMBL4243773 — — 1 6.33
CHEMBL4249269 — — 1 6.30
CHEMBL4238769 — — 1 6.30
CHEMBL4245696 — — 1 6.30
CHEMBL4245162 — — 1 6.24
CHEMBL4249612 — — 1 6.24
CHEMBL101309 AVASIMIBE 2.0 1 6.23
CHEMBL4242889 — — 1 6.22
CHEMBL4242494 — — 1 6.10
CHEMBL274185 LECIMIBIDE 2.0 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4247249 — IC50 = 7.0 nM 8.15
CHEMBL4241747 — IC50 = 30.0 nM 7.52
CHEMBL4243015 — IC50 = 40.0 nM 7.40
CHEMBL4240947 — IC50 = 43.0 nM 7.37
CHEMBL4245998 — IC50 = 48.0 nM 7.32
CHEMBL4248936 — IC50 = 59.0 nM 7.23
CHEMBL4249263 — IC50 = 100.0 nM 7.00
CHEMBL4239138 — IC50 = 100.0 nM 7.00
CHEMBL4249787 — IC50 = 100.0 nM 7.00
CHEMBL4239248 — IC50 = 180.0 nM 6.75
CHEMBL4245984 — IC50 = 180.0 nM 6.75
CHEMBL4238015 — IC50 = 280.0 nM 6.55
CHEMBL4248950 — IC50 = 300.0 nM 6.52
CHEMBL4248172 — IC50 = 310.0 nM 6.51
CHEMBL22373 CL-976 IC50 = 310.0 nM 6.51
CHEMBL4238030 — IC50 = 350.0 nM 6.46
CHEMBL4249719 — IC50 = 400.0 nM 6.40
CHEMBL4244680 — IC50 = 410.0 nM 6.39
CHEMBL4245518 — IC50 = 410.0 nM 6.39
CHEMBL4244693 — IC50 = 460.0 nM 6.34
CHEMBL4243773 — IC50 = 470.0 nM 6.33
CHEMBL4249269 — IC50 = 500.0 nM 6.30
CHEMBL4238769 — IC50 = 500.0 nM 6.30
CHEMBL4245696 — IC50 = 500.0 nM 6.30
CHEMBL4249612 — IC50 = 580.0 nM 6.24
CHEMBL4245162 — IC50 = 570.0 nM 6.24
CHEMBL101309 AVASIMIBE IC50 = 590.0 nM 6.23
CHEMBL4242889 — IC50 = 600.0 nM 6.22
CHEMBL4242494 — IC50 = 800.0 nM 6.10
CHEMBL274185 LECIMIBIDE IC50 = 820.0 nM 6.09
CHEMBL4250140 — IC50 = 900.0 nM 6.05
CHEMBL4245509 — IC50 = 1100.0 nM 5.96
CHEMBL4242952 — IC50 = 1100.0 nM 5.96
CHEMBL4247160 — IC50 = 1200.0 nM 5.92
CHEMBL4245060 — IC50 = 1300.0 nM 5.89
CHEMBL4246755 — IC50 = 1300.0 nM 5.89
CHEMBL4241732 — IC50 = 1700.0 nM 5.77
CHEMBL4245885 — IC50 = 1800.0 nM 5.75
CHEMBL4238820 — IC50 = 1800.0 nM 5.75
CHEMBL4239246 — IC50 = 1900.0 nM 5.72
CHEMBL4249315 — IC50 = 2200.0 nM 5.66
CHEMBL4240484 — IC50 = 2300.0 nM 5.64
CHEMBL4250104 — IC50 = 2400.0 nM 5.62
CHEMBL4244682 — IC50 = 2800.0 nM 5.55
CHEMBL4249196 — IC50 = 2800.0 nM 5.55
CHEMBL4249785 — IC50 = 2800.0 nM 5.55
CHEMBL4237641 — IC50 = 3000.0 nM 5.52
CHEMBL4249325 — IC50 = 3100.0 nM 5.51
CHEMBL4239678 — IC50 = 3600.0 nM 5.44
CHEMBL4250566 — IC50 = 4100.0 nM 5.39