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Assay Detail

CHEMBL4384334

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

Binding
Activation of VDR in mouse ASZ001 cells assessed as change in Cyp24A1 mRNA expression after 48 hrs by q-PCR analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vitamin D3 receptor (CHEMBL5601)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
Maschinot CA, Chau LQ, Wechsler-Reya RJ, Hadden MK.
Eur J Med Chem (2019) 162 : 495 -506
PubMed 30471551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.53 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL197589 LG-190178 1 8.11
CHEMBL846 CALCITRIOL 4.0 1 7.00
CHEMBL4459512 1 7.00
CHEMBL4522782 1 6.40
CHEMBL1040 CALCIFEDIOL ANHYDROUS 4.0 1 6.22
CHEMBL4580825 1 6.22
CHEMBL4524451 1 6.22
CHEMBL4459996 1 6.16
CHEMBL1042 CHOLECALCIFEROL 4.0 1 6.05
CHEMBL4449816 1 5.89
CHEMBL4438180 1 -
CHEMBL4439766 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL197589 LG-190178 EC50 = 7.7 nM 8.11
CHEMBL846 CALCITRIOL EC50 = 100.0 nM 7.00
CHEMBL4459512 EC50 = 100.0 nM 7.00
CHEMBL4522782 EC50 = 400.0 nM 6.40
CHEMBL1040 CALCIFEDIOL ANHYDROUS EC50 = 600.0 nM 6.22
CHEMBL4580825 EC50 = 600.0 nM 6.22
CHEMBL4524451 EC50 = 600.0 nM 6.22
CHEMBL4459996 EC50 = 700.0 nM 6.16
CHEMBL1042 CHOLECALCIFEROL EC50 = 900.0 nM 6.05
CHEMBL4449816 EC50 = 1300.0 nM 5.89
CHEMBL4438180 EC50 > 10000.0 nM -
CHEMBL4439766 EC50 > 10000.0 nM -