Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL921912

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

Functional
Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
5
Total Activities
5
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 Autocuration

Target

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

Publication

2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.
Yoshimoto N, Inaba Y, Yamada S, Makishima M, Shimizu M, Yamamoto K.
Bioorg Med Chem (2008) 16 : 457 -473
PubMed 17904370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.99 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL846 CALCITRIOL 4.0 1 9.30
CHEMBL429347 1 8.22
CHEMBL409470 1 8.00
CHEMBL263638 1 7.60
CHEMBL261197 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL846 CALCITRIOL EC50 = 0.5 nM 9.30
CHEMBL429347 EC50 = 6.0 nM 8.22
CHEMBL409470 EC50 = 10.0 nM 8.00
CHEMBL263638 EC50 = 25.0 nM 7.60
CHEMBL261197 EC50 = 150.0 nM 6.82