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Assay Detail

CHEMBL4275701

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

Binding
Displacement of fluormone VDR red from human full-length VDR after 4 hrs by fluorescence polarization assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
Kang ZS, Wang C, Han XL, Wang B, Yuan HL, Hou SY, Hao MX, Du JJ, Li YY, Zhou AW, Zhang C.
Eur J Med Chem (2018) 157 : 1174 -1191
PubMed 30193216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.44 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL846 CALCITRIOL 4.0 1 8.85
CHEMBL4288947 1 7.05
CHEMBL2434990 1 6.94
CHEMBL4290851 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL846 CALCITRIOL IC50 = 1.42 nM 8.85
CHEMBL4288947 IC50 = 89.1 nM 7.05
CHEMBL2434990 IC50 = 115.3 nM 6.94
CHEMBL4290851 IC50 = 125.4 nM 6.90