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Assay Detail

CHEMBL4824182

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

Binding
Inhibition of SREBP (unknown origin) expressed in CHO-K1 cells by luciferase reporter assay
7
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sterol regulatory element-binding protein 1 (CHEMBL4630818)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Vitamin D Receptor-Silent Vitamin D Derivative That Impairs Sterol Regulatory Element-Binding Protein In Vivo.
Kawagoe F, Mendoza A, Hayata Y, Asano L, Kotake K, Mototani S, Kawamura S, Kurosaki S, Akagi Y, Takemoto Y, Nagasawa K, Nakagawa H, Uesugi M, Kittaka A.
J Med Chem (2021) 64 : 5689 -5709
PubMed 33899473 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.88 6.16
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1824673 1 6.16
CHEMBL4851466 2 6.14
CHEMBL4876668 1 5.94
CHEMBL1040 CALCIFEDIOL ANHYDROUS 4.0 1 5.93
CHEMBL4851396 1 5.80
CHEMBL1824658 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1824673 IC50 = 700.0 nM 6.16
CHEMBL4851466 IC50 = 722.7 nM 6.14
CHEMBL4876668 IC50 = 1160.0 nM 5.94
CHEMBL1040 CALCIFEDIOL ANHYDROUS IC50 = 1176.0 nM 5.93
CHEMBL4851396 IC50 = 1600.0 nM 5.80
CHEMBL1824658 IC50 = 5000.0 nM 5.30
CHEMBL4851466 Inhibition - % -