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Assay Detail

CHEMBL4775514

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

Binding
Agonist activity at VDR in human HL-60 cells assessed as induction of cell differentiation of promyelocytes to monocytes after 4 days by NBT reduction assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HL-60
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 8.51 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4776651 1 9.28
CHEMBL846 CALCITRIOL 4.0 1 8.80
CHEMBL4794075 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4776651 EC50 = 0.53 nM 9.28
CHEMBL846 CALCITRIOL EC50 = 1.6 nM 8.80
CHEMBL4794075 EC50 = 36.0 nM 7.44