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Assay Detail

CHEMBL3632106

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

Binding
Displacement of [3H]-1alpha,25-dihydroxyvitamin D3 from recombinant human VDR LBD expressed in Escherichia coli BL21 (DE3) pLysS after 16 hrs
5
Total Activities
5
Compounds Tested
2
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

Fine tuning of agonistic/antagonistic activity for vitamin D receptor by 22-alkyl chain length of ligands: 22S-Hexyl compound unexpectedly restored agonistic activity.
Anami Y, Sakamaki Y, Itoh T, Inaba Y, Nakabayashi M, Ikura T, Ito N, Yamamoto K.
Bioorg Med Chem (2015) 23 : 7274 -7281
PubMed 26515040 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 3 - -
IC50 2 9.95 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL846 CALCITRIOL 4.0 1 10.22
CHEMBL3629552 1 9.68
CHEMBL1214509 1 -
CHEMBL1214508 1 -
CHEMBL1212956 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL846 CALCITRIOL IC50 = 0.06 nM 10.22
CHEMBL3629552 IC50 = 0.21 nM 9.68
CHEMBL1214509 Inhibition - % -
CHEMBL1214508 Inhibition - % -
CHEMBL1212956 Inhibition - % -