Vitamin D analog, 10 BDBM93065 Vitamin D analog, 14
Vitamin D analog, 11 BDBM93062 Vitamin D analog, 15
Vitamin D analog, 12 BDBM93066 Vitamin D analog, 16
Vitamin D analog, 17 BDBM93067 Vitamin D analog, 13
BDBM512999 Vitamin B12
Vitamin B12 BDBM420313
CHEBI:28940 Vitamin D 3 Vitamin D Cholecalciferol 7-Dehydrocholesterol BDBM50030475 Colecalciferol Dihydrocholesterol
BDBM93061 Vitamin D analog, 6
BDBM93063 Vitamin D analog, 8
BDBM93064 Vitamin D analog, 9
BDBM93068 Vitamin D analog, 14
BDBM93069 Vitamin D analog, 15
BDBM93070 Vitamin D analog, 16
BDBM93071 Vitamin D analog, 17
BDBM93072 Vitamin D analog, 7
CYANOCOBALAMIN Cobalamin SMR001233181 RUVITE MLS002153809 vitamin B12 cid_25102581 BDBM83973
Folic Acid Folvite Pteroylglutamic Acid CHEBI:27470 Natur Flow Folicet Folicare Vitamin Bc Roche Folacin Lexpec BDBM50237629 Preconceive Vitamin M Bio Science Folsan
CHEBI:16709 Pyridoxine Hexa-Betalin M.V.I.-12 BDBM50103505 Vitamin B6
CHEMBL494338 BDBM50257431 1,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3
2-methyl-1,4-naphthoquinone, 5 Menadione (Vitamin K3) 2-methyl-1,4-dihydronaphthalene-1,4-dione CHEMBL590 Menadione BDBM24778 cid_4055 Menadione (5d) Vitamin K3 Menadione, 9
Folvite BDBM50367343 Folacin FOLIC ACID Vitamin B9 (2S)-2-[[4-[(2-amino-4-oxo-1H-pteridin-6-yl)methylamino]benzoyl]amino]pentanedioic acid Vitamin M
Alpha Tocopherol BDBM50458513 Aquasol E E307 Vitamin E CHEBI:18145 Tocopherol
Viosterol in Oil Vitamin D2 Osto-D2 Drisdol Ergoral D2 Uvesterol D BDBM50247883 Caltrate Ergocalciferol Oleovitamin D, Synthetic Oleovitamin D D-Forte Sterogyl Sterogyl 15H Vitamin D 2 Ergo-D2 Calciferol Vitamin D Eciferol D2 Deltalin Calciferol In Arach Oil Lanes Sterogyl-15 CHEBI:28934
Phytomenadione Konakion mm BDBM50553259 Konakion mm paed Orakay Vitamin k1 Mephyton Kanavit NSC-270681 Aquamephyton Neokay Vitamin K 1 CHEBI:18067 Phylloquinone Phylloquinone e-form Konakion Phytonadione
CHEMBL220846 (20S,22R)-22-methyl-1-alpha-25-dihydroxy-vitamin D3 BDBM50205234
CHEMBL222195 BDBM50205233 (20S,22R)-22-methyl-1-alpha-25-dihydroxy-vitamin D3
CHEMBL375811 BDBM50205235 (20S,22R)-22-methyl-1-alpha-25-dihydroxy-vitamin D3
BDBM50373877 THIAMINE (VIT B1) Betaxin ThOH CA inhibitor, 3 Vitamin B 1 Thiamine
Vitamin B 5 CHEBI:46905 Cantopal BDBM50240040 Calc Pantoth Pantothenic Acid Pantothenic acid
CHEMBL492749 BDBM50293274 1alpha,25(OH)2-24-oxo-16-ene-20-cyclopropyl-vitamin D3
TRETINOIN all-trans retinoic acid MLS000028588 [3H]RA Vitamin A acid ALL-TRANS-RETINOIC ACID [3H]Retinoic acid cid_444795 9-cis-retinoic acid (9cRA) BDBM31883 AT-RA Atralin CHEMBL38 SMR000058245 [3H]tretinoin [3H]Vitamin A acid
2-methyl-3-[(2E,7R,11R)-3,7,11,15-tetramethylhexadec-2-en-1-yl]-1,4-dihydronaphthalene-1,4-dione vitamin K1, 11 Phylloquinone BDBM24782 Phytonadione
Alphalin all-trans-retinyl alcohol all-trans-vitamin A alcohol CHEMBL986 Afaxin Chocola A all-trans-retinol (2E,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohex-1-en-1-yl)nona-2,4,6,8-tetraen-1-ol BDBM50092056 Retinol
13-RA isotretinoin 13-cis-Vitamin A acid 13-cis-retinoic acid CHEMBL547 (2Z,4E6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohex-1-en-1-yl)nona-2,4,6,8-tetraenoic acid (7E,9E,11E,13Z)-retinoic acid Neovitamin A acid BDBM50031459
CHEMBL196 (R)-2-((S)-1,2-dihydroxyethyl)-4,5-dihydroxyfuran-3(2H)-one ascorbic acid 5-(1,2-Dihydroxy-ethyl)-3,4-dihydroxy-5H-furan-2-one(AsA) vitamin C (R)-5-((S)-1,2-Dihydroxy-ethyl)-3,4-dihydroxy-5H-furan-2-one (R)-5-((S)-1,2-dihydroxyethyl)-3,4-dihydroxyfuran-2(5H)-one BDBM50090256
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- ChEMBL_305987 (CHEMBL832974) Inhibitory concentration against beef liver Vitamin K epoxide reductase (vitamin K 2,3-epoxide reductase)
- ChEBML_214476 Binding affinity for vitamin K epoxide reductase
- ChEMBL_987815 (CHEMBL2437763) Inhibition of human vitamin D3 receptor
- ChEBML_214470 Apparent kinetic constant for Vitamin K epoxide reductase
- ChEMBL_214322 (CHEMBL818350) Effective concentration required for inhibition of Vitamin D3 receptor
- ChEMBL_622880 (CHEMBL1116619) Binding affinity to human vitamin D binding protein
- ChEBML_214154 Displacement from vitamin D receptor in chick intestine: 50% displacement
- ChEMBL_214155 (CHEMBL818834) Displacement from vitamin D receptor in chick intestine: 50% displacement
- ChEMBL_2260044 (CHEMBL5215055) Agonist activity at Vitamin D receptor (unknown origin) by fluorescence polarization assay
- ChEBML_214183 In vitro relative binding affinity for chick intestinal vitamin D3 receptor compared to [3H]1
- ChEMBL_1657647 (CHEMBL4007117) Inhibition of VKORC1 in rat liver microsomes in presence of 0.003 to 0.2 mM vitamin K
- ChEMBL_428140 (CHEMBL915778) Displacement of [3H]1,25-(OH)2D3 from vitamin D receptor in bovine thymus
- ChEMBL_514897 (CHEMBL972705) Displacement of [3H]1,25-(OH)2D3 from bovine thymus vitamin D receptor
- ChEMBL_214183 (CHEMBL820132) In vitro relative binding affinity for chick intestinal vitamin D3 receptor compared to [3H]1
- ChEMBL_2322206 Agonist activity at human Vitamin D receptor assessed as increase in gene transcriptional activity by luciferase reporter gene based assay
- ChEMBL_674300 (CHEMBL1274500) Vitamin-D activity at VDR receptor in human HL60 cells assessed as induction of cell differentiation by NBT reduction assay
- ChEMBL_1505946 (CHEMBL3595548) Displacement of [3H]-1alpha25-(OH)2D3 from full length recombinant rat vitamin D receptor by scintillation counting analysis
- ChEMBL_412322 (CHEMBL910037) Antagonist activity against 1-alpha,25-dihydroxy vitamin D3-induced HL60 cell differentiation by NBT reduction method
- ChEMBL_1545531 (CHEMBL3749446) Binding affinity to vitamin D3 receptor (unknown origin) after 4 hrs using fluormone VDR red by polar screen VDR competitor assay
- ChEMBL_2322205 Agonist activity at Vitamin D receptor (unknown origin) assessed as increase in fluorescein labeled TRAP220/DRIP-2 coactivator peptide requirement by TR-FRET assay
- ChEMBL_1857759 (CHEMBL4358488) Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by HTRF assay
- ChEMBL_2014666 (CHEMBL4668244) Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by immunoblot analysis
- ChEMBL_1545532 (CHEMBL3749447) Agonist activity at vitamin D3 receptor in human HL-60 cells assessed as induction of cell differentiation after 96 hrs by NBT dye-based microscopic analysis
- ChEMBL_1670487 (CHEMBL4020375) Antagonist activity at human vitamin D receptor expressed in HEK293 cells assessed as inhibition of 1,25D3-induced transactivation after 16 hrs by dual luciferase reporter gene assay
- ChEMBL_830134 (CHEMBL2061944) Displacement of [3H]1alpha,25-dihydroxyvitamin D3 from human recombinant GST-tagged vitamin D3 receptor LBD expressed in Escherichia coli BL21 after 16 hrs
- ChEMBL_1670790 (CHEMBL4020678) Binding affinity to recombinant human GST-tagged VDR LBD (156 to 453 residues) expressed in Echerichia coli BL21 star (DE3) after 40 mins in presence of vitamin D3 by fluorescence polarization assay
- ChEBML_1686154 Agonist activity at vitamin D receptor (unknown origin) expressed in HEK293 cells co-expressing pCMX-RXRalpha and pCMX-beta-galactosidase assessed as induction of receptor transactivation incubated for 16 to 24 hrs by luciferase reporter gene assay
- ChEMBL_1670491 (CHEMBL4020379) Displacement of [3H]-1,25-(OH)2D3 from N-terminal GST-tagged human recombinant vitamin D receptor ligand binding domain expressed in Escherichia coli BL21 (DE3) pLys S after 16 hrs
- ChEMBL_2224380 (CHEMBL5137893) 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
- Inhibition Assay Reader: Synergy HT program: tyrosinase 280-490 kinetics: kinetics over 45 minutes, reading at t=10 minutes, Tests in transparent 96-well plates, Phosphate buffer (pH 6.8), Enzyme: mushroom tyrosinase (T-3824, Sigma), Substrate: L-tyrosine (T-3754, Sigma), Positive control: Kojic acid (KA) (60890, Fluka) (reference inhibitor). Reference Molecules for the Test: Kojic acid: 9 μM
- Cell-Based Assay The ability of representative disclosed to block influenza infection was assessed in a cell-based assay using A549 human epithelial cells (ATCC CCL-185). Briefly, a spatial infection model for testing drug efficacy and influenza replication was adapted from Lam et al. (Biotechnol Bioeng. (2005) 90(7):793-804). A549 cells were plated on Lab-Tek two well Permanox slides (Nalge Nunc International, Rochester, N.Y.) and allowed to become nearly confluent during an overnight incubation. Culture media used in these experiments was as described above, i.e. in DMEM supplemented with 5% fetal bovine serum, 100 U/ml penicillin, and 100 ug/ml streptomycin. Following overnight incubation, the cells were then washed three times with PBS, and 2 ml of a binary mixture of 2% agar and 2xMEM (with 100 U/ml penicillin, 100 ug/ml streptomycin, 2 mM L-glutamine, and 1xMEM vitamin solution (e.g. Gibco Cat. No. 111120 for 100x solution) was added to the cells.
- Cellular Assay Alternatively, the present compounds might also be assessed for their capacity to inhibit Btk-dependent FcG receptor-induced IL-8 secretion in human cells. The human myeloid leukemia THP1 cell line (ATCC TIB202) was grown in RPMI 1640 medium supplemented with 10% FCS and 15 nM 1, 25-dihydroxy Vitamin D3 during 4 days before use to induced myeloid differentiation. A sufficient number of tissue-culture grade 384-well plates was coated with human IgG of unknown specificity by incubating overnight at 4° C. with 40 ul/well of a 50 ug/ml IgG solution in PBS. On the day of the experiment, plates were washed 5 times with 80 ul water on a Molecular Devices Aquamax DW4 plate washer. Solutions of the test compounds in 90% DMSO were added to each well on a Hamilton Microlab Star liquid handling station to 40 ul/well tissue culture medium and the total DMSO concentration was adjusted to 0.1%. Differentiated THP1 cells were then added in 40 ul/well to reach a final density of 5'000 cells/well in 80 ul culture medium. After 24 hours, IL-8 secretion was measured in the supernatant by the IL-8 HTRF assay following the protocol of the vendor (CisBio international).