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Assay Detail

CHEMBL4775519

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

Binding
Agonist activity at human VDR expressed in African green monkey COS7 cells expressing mouse osteopontin VDRE assessed as induction of receptor transactivation incubated for 16 hrs by luciferase reporter gene assay
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.
Sasaki H,Masuno H,Kawasaki H,Yoshihara A,Numoto N,Ito N,Ishida H,Yamamoto K,Hirata N,Kanda Y,Kawachi E,Kagechika H,Tanatani A
J Med Chem (2021) 64 : 516 -526
PubMed 33369416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.92 9.62
Activity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4794075 2 9.62
CHEMBL4776651 2 9.00
CHEMBL846 CALCITRIOL 4.0 2 8.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4794075 EC50 = 0.24 nM 9.62
CHEMBL4776651 EC50 = 1.0 nM 9.00
CHEMBL846 CALCITRIOL EC50 = 7.0 nM 8.15
CHEMBL4776651 Activity - -
CHEMBL4794075 Activity - -
CHEMBL846 CALCITRIOL Activity - -