Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3824698

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

Binding
Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Caco-2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vitamin D3 receptor (CHEMBL1977)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer.
Lin Z, Marepally SR, Ma D, Kim TK, Oak AS, Myers LK, Tuckey RC, Slominski AT, Miller DD, Li W.
J Med Chem (2016) 59 : 5102 -5108
PubMed 27070779 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.62 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333950 MAXACALCITOL 3.0 1 6.84
CHEMBL3822832 1 6.76
CHEMBL846 CALCITRIOL 4.0 1 6.65
CHEMBL3822994 1 6.62
CHEMBL3823776 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333950 MAXACALCITOL EC50 = 144.5 nM 6.84
CHEMBL3822832 EC50 = 171.7 nM 6.76
CHEMBL846 CALCITRIOL EC50 = 223.4 nM 6.65
CHEMBL3822994 EC50 = 241.4 nM 6.62
CHEMBL3823776 EC50 = 562.0 nM 6.25