Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)
Found 167 hits in this display
Ki: 0.0100nMAssay Description:Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcription...More data for this Ligand-Target Pair
BDBM50304585((20S)-1alpha,25-Dihydroxy-2-methylene-18,19-dinorv...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
Ki: 0.0600nMAssay Description:Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcription...More data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50304583(1alpha,25-Dihydroxy-2-methylene-18,19,21-trinorvit...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
Ki: 0.100nMAssay Description:Displacement of [3H]-1alpha25-(OH)2D3 from full length recombinant rat vitamin D receptor by scintillation counting analysisMore data for this Ligand-Target Pair
Ki: 0.200nMAssay Description:Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcription...More data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
Ki: 0.200nMAssay Description:Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcription...More data for this Ligand-Target Pair
BDBM50304584(1alpha,25-Dihydroxy-2-methylene-19,21-dinorvitamin...)
BDBM93061(Vitamin D analog, 6)
BDBM93064(Vitamin D analog, 9)
BDBM93072(Vitamin D analog, 7)
BDBM93063(Vitamin D analog, 8)
Ki: 0.400nMAssay Description:Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcription...More data for this Ligand-Target Pair
BDBM50186661(1alpha,25-dihydroxy-2-(3'-hydroxypropylidene)-19-n...)
Ki: 20nMAssay Description:Displacement of [3H]-1alpha25-(OH)2D3 from full length recombinant rat vitamin D receptor by scintillation counting analysisMore data for this Ligand-Target Pair
Ki: 20nMAssay Description:Displacement of [3H]-1alpha25-(OH)2D3 from full length recombinant rat vitamin D receptor by scintillation counting analysisMore data for this Ligand-Target Pair
Ki: >1.00E+4nMAssay Description:Displacement of [3H]-1alpha25-(OH)2D3 from full length recombinant rat vitamin D receptor by scintillation counting analysisMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
IC50: 0.0600nMAssay Description:Displacement of [3H]-1alpha,25-dihydroxyvitamin D3 from recombinant human VDR LBD expressed in Escherichia coli BL21 (DE3) pLysS after 16 hrsMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
IC50: 1.10nMAssay Description:Binding affinity to vitamin D3 receptor (unknown origin) after 4 hrs using fluormone VDR red by polar screen VDR competitor assayMore data for this Ligand-Target Pair
IC50: 1.10nMAssay Description:Inhibition of Fluormone VDR Red binding to human VDR LBD expressed in insect cells assessed as binding ability by fluorescence polarization assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50030475(7-Dehydrocholesterol | CHEBI:28940 | Cholecalcifer...)
BDBM50147583((S)-4-Methylene-3-{2-[(R)-7a-(R)-methyl-1-((R)-5-m...)
BDBM50521013(CHEBI:17933 | Calcifediol)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50030475(7-Dehydrocholesterol | CHEBI:28940 | Cholecalcifer...)
BDBM50030475(7-Dehydrocholesterol | CHEBI:28940 | Cholecalcifer...)
BDBM50030475(7-Dehydrocholesterol | CHEBI:28940 | Cholecalcifer...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50030475(7-Dehydrocholesterol | CHEBI:28940 | Cholecalcifer...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50030475(7-Dehydrocholesterol | CHEBI:28940 | Cholecalcifer...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 0.100nMAssay Description:Displacement of [3H]1,25-(OH)2D3 from rat recombinant His-tagged VDR ligand-binding domain expressed in Escherichia coli BL21More data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 1.60nMAssay Description:Agonist activity at VDR in human MCF7 cells assessed as increase in transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
EC50: 1.20nMAssay Description:Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 5.5nMAssay Description:Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assayMore data for this Ligand-Target Pair
Kd: 3.30E+3nMAssay Description:Agonist activity at zebrafish VDR LBD assessed as binding affinity to TAMRA-labeled SRC-1 peptide by fluorescence anisotropy assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 1.60nMAssay Description:Transactivation of recombinant human VDR/RXRalpha expressed in HEK293 cells after 24 hrs by Dual-luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 0.0110nMAssay Description:Agonist activity at human VDR expressed in HOS cells co-expressing human RXR by Dual-Glo luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50030475(7-Dehydrocholesterol | CHEBI:28940 | Cholecalcifer...)
BDBM50521013(CHEBI:17933 | Calcifediol)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
Kd: 1.20E+3nMAssay Description:Binding affinity to zebrafish VDR LBD assessed as Kd for fluorescein-labeled SRC1 NR2 peptide binding by micro-scale thermophoresis methodMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 3nMAssay Description:Induction of CYP24A1 (unknown orgin) transcriptional activity trasfected in human MCF7 cells incuabted for 48 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 0.0260nMAssay Description:Transactivation of VDR-mediated osteocalcin promoter in human HOS/SF cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 1nMAssay Description:Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50030475(7-Dehydrocholesterol | CHEBI:28940 | Cholecalcifer...)
BDBM50143770((1R,3S)-5-[2-[(3aS,7aR)-1-((R)-5-Hydroxy-1,5-dimet...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50030475(7-Dehydrocholesterol | CHEBI:28940 | Cholecalcifer...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 0.120nMAssay Description:Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 0.600nMAssay Description:Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 10nMAssay Description:Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCRMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 10nMAssay Description:Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCRMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 203nMAssay Description:Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured afte...More data for this Ligand-Target Pair
EC50: 31nMAssay Description:Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured afte...More data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 241nMAssay Description:Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after...More data for this Ligand-Target Pair
EC50: 172nMAssay Description:Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after...More data for this Ligand-Target Pair
EC50: 562nMAssay Description:Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after...More data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 250nMAssay Description:Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after...More data for this Ligand-Target Pair
EC50: 175nMAssay Description:Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after...More data for this Ligand-Target Pair
EC50: 117nMAssay Description:Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after...More data for this Ligand-Target Pair
EC50: 653nMAssay Description:Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured afte...More data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50293092(22R-Butyl-1alpha,24-dihydroxy-24,25,26-trinorvitam...)
BDBM50293093((1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R,3S)-3-(2...)
BDBM50293094((1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2S,3S)-3-(2...)
BDBM50293095(20S,22R-Butyl-1alpha,24-dihydroxy-24,25,26-trinorv...)
BDBM50293096((1alpha,22R,24R)-22-Butyl-1,24-dihydroxyvitamin D3...)
BDBM50293097((1alpha,22R,24S)-22-Butyl-1,24-dihydroxyvitamin D3...)
BDBM50293098((1R,3S,5Z)-5-[(2E)-2-{(1R,3aS,7aR)-1-[(1R,2S,4R)-2...)
BDBM50293099((1alpha,22S,24S)-22-Butyl-1,24-dihydroxyvitamin D3...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 0.300nMAssay Description:Activity at VDR in rat osteosarcoma cells assessed as induction of 24-hydroxylase reporter gene transcription by luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50304584(1alpha,25-Dihydroxy-2-methylene-19,21-dinorvitamin...)
EC50: 0.200nMAssay Description:Activity at VDR in rat osteosarcoma cells assessed as induction of 24-hydroxylase reporter gene transcription by luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50304585((20S)-1alpha,25-Dihydroxy-2-methylene-18,19-dinorv...)
EC50: 0.0200nMAssay Description:Activity at VDR in rat osteosarcoma cells assessed as induction of 24-hydroxylase reporter gene transcription by luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50304583(1alpha,25-Dihydroxy-2-methylene-18,19,21-trinorvit...)
EC50: 0.0600nMAssay Description:Activity at VDR in rat osteosarcoma cells assessed as induction of 24-hydroxylase reporter gene transcription by luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 5.74nMAssay Description:Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
EC50: 9.04nMAssay Description:Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
EC50: 8.19nMAssay Description:Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 3.28nMAssay Description:Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50205233((20S,22R)-22-methyl-1-alpha-25-dihydroxy-vitamin D...)
BDBM50205234((20S,22R)-22-methyl-1-alpha-25-dihydroxy-vitamin D...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
BDBM50200182((1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-...)
EC50: 0.5nMAssay Description:Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50205234((20S,22R)-22-methyl-1-alpha-25-dihydroxy-vitamin D...)
EC50: 0.00300nMAssay Description:Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50205233((20S,22R)-22-methyl-1-alpha-25-dihydroxy-vitamin D...)
EC50: 0.00200nMAssay Description:Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50205235((20S,22R)-22-methyl-1-alpha-25-dihydroxy-vitamin D...)
EC50: 0.200nMAssay Description:Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assayMore data for this Ligand-Target Pair
BDBM50205235((20S,22R)-22-methyl-1-alpha-25-dihydroxy-vitamin D...)
EC50: 7.10nMAssay Description:Agonist activity at VDR in human HL60 cells assessed as induction of cell differentiation after 96 hrs by NBT reduction assayMore data for this Ligand-Target Pair
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