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Assay Detail

CHEMBL1067951

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

Binding
Displacement of radiolabeled 1-alpha,25-(OH)2D3 from rat recombinant full length VDR
4
Total Activities
4
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

Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
Barycki R, Sicinski RR, Plum LA, Grzywacz P, Clagett-Dame M, Deluca HF.
Bioorg Med Chem (2009) 17 : 7658 -7669
PubMed 19819702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 10.10 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL596532 1 10.70
CHEMBL846 CALCITRIOL 4.0 1 10.00
CHEMBL594078 1 10.00
CHEMBL607373 1 9.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL596532 Ki = 0.02 nM 10.70
CHEMBL846 CALCITRIOL Ki = 0.1 nM 10.00
CHEMBL594078 Ki = 0.1 nM 10.00
CHEMBL607373 Ki = 0.2 nM 9.70