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Assay Detail

CHEMBL4137803

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

Binding
Transactivation of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-RXRalpha and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in interaction with RXRalpha by beta-galactosidase reporter gene based mammalian two-hybrid assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

25 S-Adamantyl-23-yne-26,27-dinor-1α,25-dihydroxyvitamin D3: Synthesis, Tissue Selective Biological Activities, and X-ray Crystal Structural Analysis of Its Vitamin D Receptor Complex.
Otero R, Ishizawa M, Numoto N, Ikura T, Ito N, Tokiwa H, Mouriño A, Makishima M, Yamada S.
J Med Chem (2018) 61 : 6658 -6673
PubMed 29989817 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 10.00 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL846 CALCITRIOL 4.0 1 10.15
CHEMBL4159525 1 9.85
CHEMBL4173602 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL846 CALCITRIOL EC50 = 0.07 nM 10.15
CHEMBL4159525 EC50 = 0.14 nM 9.85
CHEMBL4173602 EC50 > 1.2 nM -