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Assay Detail

CHEMBL1019666

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

Binding
Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
Laverny G, Penna G, Uskokovic M, Marczak S, Maehr H, Jankowski P, Ceailles C, Vouros P, Smith B, Robinson M, Reddy GS, Adorini L.
J Med Chem (2009) 52 : 2204 -2213
PubMed 19309155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.78 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494338 1 9.17
CHEMBL492749 1 9.16
CHEMBL846 CALCITRIOL 4.0 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494338 EC50 = 0.68 nM 9.17
CHEMBL492749 EC50 = 0.69 nM 9.16
CHEMBL846 CALCITRIOL EC50 = 10.0 nM 8.00