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Assay Detail

CHEMBL4137799

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

Binding
Displacement of [26,27-Methyl-3H]-1,25(OH)2D3 from recombinant human GST-tagged VDR LBD (140 to 427 residues) expressed in Escherichia coli BL21 preincubated for 30 mins followed by radioligand addition measured after 20 hrs
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
IC50 2 9.06 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4159525 1 9.62
CHEMBL4173602 1 8.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4159525 IC50 = 0.24 nM 9.62
CHEMBL4173602 IC50 = 3.13 nM 8.50