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Assay Detail

CHEMBL858933

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

Functional
Inhibition of transactivation of human VDR in COS7 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vitamin D3 receptor (CHEMBL1977)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Vitamin D receptor: ligand recognition and allosteric network.
Yamamoto K, Abe D, Yoshimoto N, Choi M, Yamagishi K, Tokiwa H, Shimizu M, Makishima M, Yamada S.
J Med Chem (2006) 49 : 1313 -1324
PubMed 16480267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.46 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL263638 1 6.52
CHEMBL3350951 1 6.40
CHEMBL442191 1 -
CHEMBL3350836 1 -
CHEMBL846 CALCITRIOL 4.0 1 -
CHEMBL432600 LEXACALCITOL 2.0 1 -
CHEMBL605525 DP001 2.0 1 -
CHEMBL383902 1 -
CHEMBL2104955 BECOCALCIDIOL 2.0 1 -
CHEMBL1478 LITHOCHOLIC ACID 1 -
CHEMBL410893 1 -
CHEMBL3350950 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL263638 IC50 = 300.0 nM 6.52
CHEMBL3350951 IC50 = 400.0 nM 6.40
CHEMBL442191 IC50 - -
CHEMBL3350836 IC50 - -
CHEMBL846 CALCITRIOL IC50 - -
CHEMBL432600 LEXACALCITOL IC50 - -
CHEMBL605525 DP001 IC50 - -
CHEMBL383902 IC50 - -
CHEMBL2104955 BECOCALCIDIOL IC50 - -
CHEMBL1478 LITHOCHOLIC ACID IC50 - -
CHEMBL410893 IC50 - -
CHEMBL3350950 IC50 - -