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Assay Detail

CHEMBL984593

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

Binding
Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant full length VDR
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vitamin D3 receptor (CHEMBL3150)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
Chiellini G, Grzywacz P, Plum LA, Barycki R, Clagett-Dame M, DeLuca HF.
Bioorg Med Chem (2008) 16 : 8563 -8573
PubMed 18722130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 9.33 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL846 CALCITRIOL 4.0 1 10.30
CHEMBL263638 1 9.00
CHEMBL261197 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL846 CALCITRIOL Ki = 0.05 nM 10.30
CHEMBL263638 Ki = 1.0 nM 9.00
CHEMBL261197 Ki = 2.0 nM 8.70