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Displacement of 25-hydroxy-[26,27-methyl-3H]-vitamin D3 from CYP24 in 1,25(OH)2D3-treated human DU-145 cells using 25-(OH)D3 as substrate pretreated with 1,25(OH)2D3 for 24 hrs followed by compound addition measured after 30 mins by HPLC analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of CYP24 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Induction of CYP24A1 (unknown orgin) transcriptional activity trasfected in human MCF7 cells at 0.1 to 1000 nM incuabted for 48 hrs by luciferase reporter gene assay relative to (1R,3S)-5-(2-((1R,3aS,7aR)-1-((R)-6-hydroxy-6-methylheptan-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Induction of CYP24A1 (unknown orgin) transcriptional activity trasfected in human MCF7 cells incuabted for 48 hrs by luciferase reporter gene assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
CYP24A1Inhibition Assay from Article 10.1021/bi101488p: "Screening of selective inhibitors of 1a,25-dihydroxyvitamin D3 24-hydroxylase using recombinant human enzyme expressed in Escherichia coli."
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of CYP24A1 (unknown origin) expressed in Chinese hamster V79 cells using [3H-1beta]-1alpha,25(OH)2D3 as substrate preincubated for 30 mins followed by substrate addition and measured after 2 hrs by scintillation counting method
Potency index, ratio of ketoconazole IC50 to test compound IC50 for inhibition of human CYP24A1 expressed in Chinese hamster V79 cells
Assay data:1 Tested
Inhibition of human CYP24A1 expressed in Chinese hamster V79 cells using [3H-1beta]-1alpha,25(OH)2D3 as substrate preincubated for 10 mins followed by substrate addition and measured after 2 hrs by scintillation counting method
Binding affinity to CYP24A1 in human A549 cells lysates grown on SILAC media at 10 uM incubated for 1 hr by LC-MS/MS analysis relative to untreated control
Binding affinity to CYP24A1 in human A549 cells lysates grown on SILAC media at 10 uM incubated for 1 hr by LC-MS/MS analysis
Assay data:2 Active, 2 Tested
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of MBP-tagged human CYP24A1 expressed Escherichia coli BL21-Gold(DE3) incubated for 25 mins in presence of Adx, AdR 1,25(OH)2D3 and NADPH by HPLC method
Assay data:12 Active, 12 Activity ≤ 1 µM, 12 Tested
Inhibition of N-terminal MBP-tagged human CYP24A1 expressed in Escherichia coli assessed as reduction in hydrolase activity incubated for 25 mins using Adx, AdR and 1,25(OH)2D3
Assay data:3 Active, 1 Activity ≤ 1 µM, 3 Tested
Inhibition of human CYP24A1
Assay data:2 Active, 1 Activity ≤ 1 µM, 3 Tested
Human CYP24A1 (CYP24, CYP26 and CYP27 families)
Assay data:3 Active, 3 Tested
Genome-wide siRNA screen of genes regulating the Lipopolysaccharide-induced TNF-alpha response in human macrophages_Primary screen TNF readout
Assay data:2853 Active, 18113 Tested
SummaryRelated BioAssays by Same Project
Inhibition of N-terminally MBP-fused human CYP24A1 by cell-free assay
Assay data:14 Active, 13 Activity ≤ 1 µM, 14 Tested
Inhibition of CYP24A1 in human primary CLL cells assessed as increase in VDR-regulated CDKN1A mRNA expression at 0.05 to 0.10 uM in presence of 100 nM 1,25(OH)2D3 incubated for 24 hrs by quantitative RT-PCR method
Inhibition of CYP24A1 in human primary CLL cells assessed as increase in VDR-regulated GADD45alpha mRNA expression at 0.05 to 0.10 uM in presence of 100 nM 1,25(OH)2D3 incubated for 24 hrs by quantitative RT-PCR method
Inhibition of CYP24A1 in human primary CLL cells assessed as increase in VDR-regulated CDKN1A mRNA expression in presence of 100 nM calcitriol incubated for 24 hrs by quantitative RT-PCR method
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