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Assay Detail

CHEMBL972705

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

Binding
Displacement of [3H]1,25-(OH)2D3 from bovine thymus vitamin D receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vitamin D3 receptor (CHEMBL3452)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

A new class of vitamin D analogues that induce structural rearrangement of the ligand-binding pocket of the receptor.
Inaba Y, Yoshimoto N, Sakamaki Y, Nakabayashi M, Ikura T, Tamamura H, Ito N, Shimizu M, Yamamoto K.
J Med Chem (2009) 52 : 1438 -1449
PubMed 19193059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 8.44 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL846 CALCITRIOL 4.0 1 10.30
CHEMBL454123 1 8.92
CHEMBL454124 1 8.70
CHEMBL454141 1 8.47
CHEMBL454947 1 8.42
CHEMBL454122 1 7.96
CHEMBL507787 1 7.80
CHEMBL454925 1 7.70
CHEMBL454142 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL846 CALCITRIOL EC50 = 0.05 nM 10.30
CHEMBL454123 EC50 = 1.2 nM 8.92
CHEMBL454124 EC50 = 2.0 nM 8.70
CHEMBL454141 EC50 = 3.4 nM 8.47
CHEMBL454947 EC50 = 3.8 nM 8.42
CHEMBL454122 EC50 = 11.0 nM 7.96
CHEMBL507787 EC50 = 16.0 nM 7.80
CHEMBL454925 EC50 = 20.0 nM 7.70
CHEMBL454142 EC50 = 20.0 nM 7.70