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Assay Detail

CHEMBL2175827

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

Binding
Inhibition of 7-dehydroxycholesterol reductase-mediated cholesterol biosynthesis in human HL60 cells assessed as inhibition of 2-[13C]acetate after 24 hrs GC/MS analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HL-60
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

7-dehydrocholesterol reductase (CHEMBL2169735)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A new class of selective and potent 7-dehydrocholesterol reductase inhibitors.
Horling A, Müller C, Barthel R, Bracher F, Imming P.
J Med Chem (2012) 55 : 7614 -7622
PubMed 22882119 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.75 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172347 1 8.64
CHEMBL2172349 1 6.92
CHEMBL2172263 1 6.30
CHEMBL2172350 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172347 IC50 = 2.3 nM 8.64
CHEMBL2172349 IC50 = 120.0 nM 6.92
CHEMBL2172263 IC50 = 500.0 nM 6.30
CHEMBL2172350 IC50 = 7300.0 nM 5.14