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Assay Detail

CHEMBL3749446

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Binding
Binding affinity to vitamin D3 receptor (unknown origin) after 4 hrs using fluormone VDR red by polar screen VDR competitor assay
14
Total Activities
14
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

Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.
Ge Z, Hao M, Xu M, Su Z, Kang Z, Xue L, Zhang C.
Eur J Med Chem (2016) 107 : 48 -62
PubMed 26562542 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.33 8.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL846 CALCITRIOL 4.0 1 8.95
CHEMBL3747730 1 7.15
CHEMBL3746465 1 6.71
CHEMBL3747184 1 6.71
CHEMBL3747703 1 6.41
CHEMBL3747394 1 6.25
CHEMBL3747341 1 6.06
CHEMBL3747314 1 6.00
CHEMBL3746013 1 5.92
CHEMBL3747293 1 5.45
CHEMBL3747642 1 5.28
CHEMBL3747395 1 5.03
CHEMBL3747218 1 -
CHEMBL3746404 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL846 CALCITRIOL IC50 = 1.13 nM 8.95
CHEMBL3747730 IC50 = 71.06 nM 7.15
CHEMBL3746465 IC50 = 196.6 nM 6.71
CHEMBL3747184 IC50 = 194.3 nM 6.71
CHEMBL3747703 IC50 = 389.3 nM 6.41
CHEMBL3747394 IC50 = 563.6 nM 6.25
CHEMBL3747341 IC50 = 863.0 nM 6.06
CHEMBL3747314 IC50 = 1007.0 nM 6.00
CHEMBL3746013 IC50 = 1189.0 nM 5.92
CHEMBL3747293 IC50 = 3521.0 nM 5.45
CHEMBL3747642 IC50 = 5235.0 nM 5.28
CHEMBL3747395 IC50 = 9245.0 nM 5.03
CHEMBL3747218 IC50 > 10000.0 nM -
CHEMBL3746404 IC50 > 10000.0 nM -