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Assay Detail

CHEMBL948042

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

Binding
Effect on VDR transcriptional activity in human osteosarcoma cells
5
Total Activities
5
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

(2S,2'R)-analogue of LG190178 is a major active isomer.
Hakamata W, Sato Y, Okuda H, Honzawa S, Saito N, Kishimoto S, Yamashita A, Sugiura T, Kittaka A, Kurihara M.
Bioorg Med Chem Lett (2008) 18 : 120 -123
PubMed 18054230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 9.26 10.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL846 CALCITRIOL 4.0 1 10.97
CHEMBL272304 1 10.40
CHEMBL403885 1 8.78
CHEMBL403670 1 8.33
CHEMBL272502 1 7.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL846 CALCITRIOL EC50 = 0.0106 nM 10.97
CHEMBL272304 EC50 = 0.0396 nM 10.40
CHEMBL403885 EC50 = 1.66 nM 8.78
CHEMBL403670 EC50 = 4.68 nM 8.33
CHEMBL272502 EC50 = 15.6 nM 7.81