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Assay Detail

CHEMBL3748723

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

Binding
Displacement of [3H]1alpha,25-(OH)2D3 from full-length recombinant rat VDR by scintillation counter
6
Total Activities
6
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

A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1α,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.
Flores A, Massarelli I, Thoden JB, Plum LA, DeLuca HF.
J Med Chem (2015) 58 : 9731 -9741
PubMed 26630444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 10.51 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3745798 1 10.70
CHEMBL3746107 1 10.52
CHEMBL3746058 1 10.52
CHEMBL1214620 1 10.52
CHEMBL3746759 1 10.40
CHEMBL846 CALCITRIOL 4.0 1 10.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3745798 Ki = 0.02 nM 10.70
CHEMBL3746107 Ki = 0.03 nM 10.52
CHEMBL3746058 Ki = 0.03 nM 10.52
CHEMBL1214620 Ki = 0.03 nM 10.52
CHEMBL3746759 Ki = 0.04 nM 10.40
CHEMBL846 CALCITRIOL Ki = 0.04 nM 10.40