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ChEMBL ligand: CHEMBL846 (1,25-dihydroxy vitamin d3, 1,25-dihydroxyvitamin d3, 1,25-hydroxylated vitamin d, 1alpha,25-dihydroxycholecalciferol, 1alpha,25-dihydroxyvitamin d3, Calcijex, Calcitriol, Dihydroxycholecalciferol, Dihydroxyvitamin D 3, RO 21-5535, RO-21-5535, RO-215535, Rocaltrol, Silkis, Topitriol, Vectical) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
ChEMBL | Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 1643-1651 [PMID:23462715] |
Vitamin D receptor/Retinoid X receptor-α/Retinoic acid receptor RXR-alpha/Vitamin D3 receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885632] [GtoPdb: 605, 610] [UniProtKB: P11473, P19793] | ||||||||
GtoPdb | - | - | 9.2 | pKd | - | - | - |
J Bone Miner Res (1994) 9: 1277-88 [PMID:7976510]; Mol Endocrinol (2002) 16: 1524-37 [PMID:12089348] |
ChEMBL | Transactivation of recombinant human VDR/RXRalpha expressed in HEK293 cells after 24 hrs by Dual-luciferase reporter gene assay | B | 8.8 | pEC50 | 1.58 | nM | EC50 | Eur J Med Chem (2018) 157: 1174-1191 [PMID:30193216] |
Vitamin D3 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5304] [UniProtKB: A3RGC1] | ||||||||
ChEMBL | Displacement of [3H]1-alpha,25-(OH)2D3 from VDR in pig intestinal mucosa | B | 10.15 | pKd | 0.07 | nM | Kd | J Med Chem (2009) 52: 6158-6162 [PMID:19739672] |
Vitamin D3 receptor A in Danio rerio (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3217399] [UniProtKB: Q9PTN2] | ||||||||
ChEMBL | Binding affinity to zebrafish VDR LBD assessed as Kd for fluorescein-labeled SRC1 NR2 peptide binding by micro-scale thermophoresis method | B | 5.92 | pKd | 1200 | nM | Kd | J Med Chem (2020) 63: 9457-9463 [PMID:32787090] |
ChEMBL | Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay | B | 8.26 | pEC50 | 5.5 | nM | EC50 | Medchemcomm (2011) 2: 424-429 [PMID:22180837] |
Vitamin D-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2259] [UniProtKB: P02774] | ||||||||
ChEMBL | Binding affinity to human vitamin D binding protein | B | 7.62 | pKd | 24 | nM | Kd | J Med Chem (2009) 52: 6158-6162 [PMID:19739672] |
Vitamin D receptor in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2353] [UniProtKB: O42392] | ||||||||
ChEMBL | Displacement from vitamin D receptor in chick intestine: 50% displacement | B | 10.6 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 1845-1848 |
Vitamin D receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473] | ||||||||
GtoPdb | - | - | 9.2 | pKd | - | - | - |
J Bone Miner Res (1994) 9: 1277-88 [PMID:7976510]; Mol Endocrinol (2002) 16: 1524-37 [PMID:12089348] |
ChEMBL | Binding affinity to VDR receptor | B | 10.19 | pKd | 0.07 | nM | Kd | J Med Chem (2001) 44: 281-297 [PMID:11462969] |
ChEMBL | Binding affinity to VDR in scrambled siRNA-transfected human MCF7 cells assessed as cell growth inhibition by measuring reduction in BrdU incorporation after 16 hrs by ELISA | B | 5.19 | pIC50 | 6430 | nM | IC50 | Eur J Med Chem (2018) 157: 1174-1191 [PMID:30193216] |
ChEMBL | Binding affinity to VDR ligand binding domain by fluorescence polarization competition assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem (2010) 18: 4119-4137 [PMID:20452225] |
ChEMBL | Binding affinity to VDR (unknown origin) | B | 8.03 | pIC50 | 9.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5949-5952 [PMID:24035340] |
ChEMBL | Displacement of fluormone VDR red from human full-length VDR after 4 hrs by fluorescence polarization assay | B | 8.85 | pIC50 | 1.42 | nM | IC50 | Eur J Med Chem (2018) 157: 1174-1191 [PMID:30193216] |
ChEMBL | Displacement of fluormone from human full length VDR after 2 hrs by fluorescence polarization assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2018) 61: 4928-4937 [PMID:29733645] |
ChEMBL | Binding affinity to VDR assessed as inhibition of fluorescent ligand by fluorescence polarization competition assay | B | 8.91 | pIC50 | 1.24 | nM | IC50 | J Med Chem (2012) 55: 8642-8656 [PMID:22989379] |
ChEMBL | Competitive binding affinity to His-tagged human VDR LBD (156 to 453 residues) expressed in Escherichia coli BL23 (DE3) cells in presence of 1,25D3 by fluorescent polarization assay | B | 8.91 | pIC50 | 1.24 | nM | IC50 | J Med Chem (2022) 65: 13112-13124 [PMID:36166643] |
ChEMBL | Binding affinity to vitamin D3 receptor (unknown origin) after 4 hrs using fluormone VDR red by polar screen VDR competitor assay | B | 8.95 | pIC50 | 1.13 | nM | IC50 | Eur J Med Chem (2016) 107: 48-62 [PMID:26562542] |
ChEMBL | Displacement of fluormone VDR red from human full length VDR after 4 hrs by fluorescence polarization assay | B | 8.95 | pIC50 | 1.13 | nM | IC50 | J Med Chem (2018) 61: 3059-3075 [PMID:29518319] |
ChEMBL | Displacement of 1-alpha, 25-(OH)[3H]D3 from human VDR expressed in COS1 cells | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2007) 50: 5824-5832 [PMID:17924616] |
ChEMBL | Displacement of [3H]1,25-dihydroxyvitamin D3 from human VDR by HAP assay | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2006) 49: 7513-7517 [PMID:17149880] |
ChEMBL | Displacement of [3H]-1,25(OH)2D3 from recombinant human VDR ligand binding domain | B | 9.46 | pIC50 | 0.35 | nM | IC50 | J Med Chem (2015) 58: 9510-9521 [PMID:26613420] |
ChEMBL | 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 | B | 9.8 | pIC50 | 0.16 | nM | IC50 | J Med Chem (2017) 60: 8394-8406 [PMID:28954197] |
ChEMBL | Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay | B | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (2015) 58: 9510-9521 [PMID:26613420] |
ChEMBL | Agonist activity at GAL4 DNA-binding domain fused VDR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay | B | 10.02 | pIC50 | 0.1 | nM | IC50 | Eur J Med Chem (2018) 157: 791-804 [PMID:30144697] |
ChEMBL | Displacement of [3H]-1-alpha,25-dihydroxyvitamin D3 from N-terminal GST-tagged human recombinant VDR LBD expressed in Escherichia coli Rosetta2 (DE3) after 16 hrs | B | 10.1 | pIC50 | 0.08 | nM | IC50 | J Med Chem (2014) 57: 4351-4367 [PMID:24742174] |
ChEMBL | Displacement of [3H]-1alpha,25-dihydroxyvitamin D3 from recombinant human VDR LBD expressed in Escherichia coli BL21 (DE3) pLysS after 16 hrs | B | 10.22 | pIC50 | 0.06 | nM | IC50 | Bioorg Med Chem (2015) 23: 7274-7281 [PMID:26515040] |
ChEMBL | Transrepression of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-NCoR and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in NCoR recruitment by beta-galactosidase reporter gene based mammalian two-hybrid assay | B | 10.3 | pIC50 | 0.05 | nM | IC50 | J Med Chem (2018) 61: 6658-6673 [PMID:29989817] |
ChEMBL | Displacement of [3H]-1,25D3 from C-terminal GST-tagged human recombinant VDR LBD expressed in Escherichia coli BL21 (DE3) after 16 hrs by radioligand binding assay | B | 10.4 | pIC50 | 0.04 | nM | IC50 | J Med Chem (2018) 61: 6339-6349 [PMID:29936834] |
ChEMBL | Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay | B | 6.29 | pEC50 | 515.2 | nM | EC50 | J Med Chem (2015) 58: 7881-7887 [PMID:26367019] |
ChEMBL | Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay | B | 6.49 | pEC50 | 321.5 | nM | EC50 | J Med Chem (2015) 58: 7881-7887 [PMID:26367019] |
ChEMBL | Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay | B | 6.6 | pEC50 | 249.7 | nM | EC50 | J Med Chem (2016) 59: 5102-5108 [PMID:27070779] |
ChEMBL | Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay | B | 6.65 | pEC50 | 223.4 | nM | EC50 | J Med Chem (2016) 59: 5102-5108 [PMID:27070779] |
ChEMBL | Agonist activity at VDR ligand binding domain (unknown origin) by reporter gene assay | B | 7.82 | pEC50 | 15 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 5949-5952 [PMID:24035340] |
ChEMBL | Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2009) 52: 2204-2213 [PMID:19309155] |
ChEMBL | Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2009) 52: 2204-2213 [PMID:19309155] |
ChEMBL | 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 | B | 8.05 | pEC50 | 9 | nM | EC50 | Eur J Med Chem (2016) 107: 48-62 [PMID:26562542] |
ChEMBL | Agonist activity at VDR in human HL60 cells assessed as induction of cell differentiation after 96 hrs by NBT assay | B | 8.05 | pEC50 | 9 | nM | EC50 | J Med Chem (2018) 61: 3059-3075 [PMID:29518319] |
ChEMBL | Inhibition of human VDR-cofactor interaction by EnBio receptor cofactor assay system | B | 8.11 | pEC50 | 7.7 | nM | EC50 | Bioorg Med Chem (2015) 23: 1055-1061 [PMID:25637122] |
ChEMBL | Agonist activity at human VDR | B | 8.11 | pEC50 | 7.7 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4292-4296 [PMID:23806555] |
ChEMBL | Agonist activity at human VDR expressed in African green monkey COS7 cells expressing mouse osteopontin VDRE assessed as induction of receptor transactivation incubated for 16 hrs by luciferase reporter gene assay | B | 8.15 | pEC50 | 7 | nM | EC50 | J Med Chem (2021) 64: 516-526 [PMID:33369416] |
ChEMBL | Agonist activity at human VDR expressed in HEK293 cells expressing mouse osteopontin VDRE assessed as induction of receptor transactivation incubated for 16 hrs by luciferase reporter gene assay | B | 8.31 | pEC50 | 4.9 | nM | EC50 | J Med Chem (2021) 64: 516-526 [PMID:33369416] |
ChEMBL | Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay | B | 8.4 | pEC50 | 3.94 | nM | EC50 | J Med Chem (2016) 59: 5102-5108 [PMID:27070779] |
ChEMBL | Effect on VDR transcriptional activity in human Caco-2 cells in presence of 5% fetal calf serum | B | 8.45 | pEC50 | 3.52 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 120-123 [PMID:18054230] |
ChEMBL | Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay | F | 8.48 | pEC50 | 3.28 | nM | EC50 | J Med Chem (2012) 55: 8642-8656 [PMID:22989379] |
ChEMBL | Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay | B | 8.52 | pEC50 | 3 | nM | EC50 | Bioorg Med Chem (2013) 21: 1643-1651 [PMID:23462715] |
ChEMBL | Transactivation of full length human VDR expressed in human HeLa cells assessed as increase in CYP24 transcription after 18 hrs by luciferase reporter gene assay | B | 8.6 | pEC50 | 2.5 | nM | EC50 | J Med Chem (2012) 55: 8440-8449 [PMID:22957834] |
ChEMBL | Agonist activity at VDR in human MCF7 cells assessed as increase in transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay | B | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2018) 61: 4928-4937 [PMID:29733645] |
ChEMBL | Agonist activity at VDR in human HL-60 cells assessed as induction of cell differentiation of promyelocytes to monocytes after 4 days by NBT reduction assay | B | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2021) 64: 516-526 [PMID:33369416] |
ChEMBL | Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay | F | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem (2008) 16: 457-473 [PMID:17904370] |
ChEMBL | Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay | B | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2012) 55: 8440-8449 [PMID:22957834] |
ChEMBL | Transactivation of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-SRC-1 and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in SRC-1 recruitment by beta-galactosidase reporter gene based mammalian two-hybrid assay | B | 9.05 | pEC50 | >0.9 | nM | EC50 | J Med Chem (2018) 61: 6658-6673 [PMID:29989817] |
ChEMBL | Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay | B | 9.22 | pEC50 | 0.6 | nM | EC50 | J Med Chem (2015) 58: 9510-9521 [PMID:26613420] |
ChEMBL | Effect on VDR transcriptional activity in human osteosarcoma cells in presence of 5% fetal calf serum | B | 9.26 | pEC50 | 0.56 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 120-123 [PMID:18054230] |
ChEMBL | Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay | B | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2007) 50: 932-939 [PMID:17298045] |
ChEMBL | Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay | F | 9.3 | pEC50 | 0.5 | nM | EC50 | Bioorg Med Chem (2008) 16: 457-473 [PMID:17904370] |
ChEMBL | Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay | B | 9.52 | pEC50 | 0.3 | nM | EC50 | J Med Chem (2016) 59: 4601-4610 [PMID:27145071] |
ChEMBL | Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay | B | 9.92 | pEC50 | 0.12 | nM | EC50 | J Med Chem (2015) 58: 9510-9521 [PMID:26613420] |
ChEMBL | Agonist activity at human VDR | B | 10 | pEC50 | 0.1 | nM | EC50 | J Med Chem (2016) 59: 9201-9214 [PMID:27652492] |
ChEMBL | Transactivation of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-RXRalpha and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in interaction with RXRalpha by beta-galactosidase reporter gene based mammalian two-hybrid assay | B | 10.15 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2018) 61: 6658-6673 [PMID:29989817] |
ChEMBL | Transactivation of VDR-mediated osteocalcin promoter in human HOS/SF cells after 24 hrs by luciferase reporter gene assay | B | 10.59 | pEC50 | 0.03 | nM | EC50 | ACS Med Chem Lett (2013) 4: 671-674 [PMID:24900728] |
ChEMBL | Agonist activity at human VDR expressed in HOS cells co-expressing human RXR by Dual-Glo luciferase reporter gene assay | B | 10.96 | pEC50 | 0.01 | nM | EC50 | Bioorg Med Chem (2018) 26: 6146-6152 [PMID:30446437] |
ChEMBL | Effect on VDR transcriptional activity in human osteosarcoma cells | B | 10.97 | pEC50 | 0.01 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 120-123 [PMID:18054230] |
ChEMBL | Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay | B | 11 | pEC50 | 0.01 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 6104-6107 [PMID:21889334] |
Vitamin D receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3452] [UniProtKB: Q28037] | ||||||||
ChEMBL | Displacement of [3H]-1-alpha,25-(OH)2D3 from bovine thymus VDR incubated for 18 hrs by competitive binding assay | B | 10.32 | pIC50 | 0.05 | nM | IC50 | J Med Chem (2021) 64: 516-526 [PMID:33369416] |
ChEMBL | Displacement of [3H]1,25-(OH)2D3 from vitamin D receptor in bovine thymus | B | 10.15 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2007) 50: 932-939 [PMID:17298045] |
ChEMBL | Displacement of [3H]1,25-(OH)2D3 from bovine thymus vitamin D receptor | B | 10.3 | pEC50 | 0.05 | nM | EC50 | J Med Chem (2009) 52: 1438-1449 [PMID:19193059] |
Vitamin D receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5601] [UniProtKB: P48281] | ||||||||
ChEMBL | Activation of VDR in mouse ASZ001 cells assessed as change in Cyp24A1 mRNA expression after 48 hrs by q-PCR analysis | B | 7 | pEC50 | 100 | nM | EC50 | Eur J Med Chem (2019) 162: 495-506 [PMID:30471551] |
Vitamin D receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3150] [GtoPdb: 605] [UniProtKB: P13053] | ||||||||
ChEMBL | Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcriptional activation after 16 hrs by luciferase reporter gene assay | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2010) 53: 8642-8649 [PMID:21105677] |
ChEMBL | Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant full length VDR | B | 10 | pKi | 0.1 | nM | Ki | Bioorg Med Chem (2009) 17: 1747-1763 [PMID:19167893] |
ChEMBL | Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant full length VDR | B | 10 | pKi | 0.1 | nM | Ki | J Med Chem (2009) 52: 3496-3504 [PMID:19402630] |
ChEMBL | Displacement of radiolabeled 1-alpha,25-(OH)2D3 from rat recombinant full length VDR | B | 10 | pKi | 0.1 | nM | Ki | Bioorg Med Chem (2009) 17: 7658-7669 [PMID:19819702] |
ChEMBL | Displacement of [3H]1alpha,25-(OH)2D3 from rat recombinant full length VDR | B | 10 | pKi | 0.1 | nM | Ki | J Med Chem (2010) 53: 8642-8649 [PMID:21105677] |
ChEMBL | Displacement of radiolabeled 1alpha, 25-(OH)2D3 from recombinant rat VDR | B | 10 | pKi | 0.1 | nM | Ki | J Med Chem (2011) 54: 6832-6842 [PMID:21902235] |
ChEMBL | Displacement of [3H]-1alpha,25(OH)2D3 from recombinant rat VDR by scintillation counting | B | 10 | pKi | 0.1 | nM | Ki | Bioorg Med Chem (2011) 19: 7205-7220 [PMID:22018918] |
ChEMBL | Displacement of [3H]-1alpha25-(OH)2D3 from full length recombinant rat vitamin D receptor by scintillation counting analysis | B | 10 | pKi | 0.1 | nM | Ki | J Med Chem (2015) 58: 6237-6247 [PMID:26206427] |
ChEMBL | Displacement of [3H]-1alpha,25(OH)2D3 from recombinant rat VDR after overnight incubation by scintillation counting | B | 10 | pKi | 0.1 | nM | Ki | J Med Chem (2012) 55: 4352-4366 [PMID:22490010] |
ChEMBL | Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant full length VDR | B | 10.3 | pKi | 0.05 | nM | Ki | Bioorg Med Chem (2008) 16: 8563-8573 [PMID:18722130] |
ChEMBL | Displacement of [3H]1alpha,25-(OH)2D3 from full-length recombinant rat VDR by scintillation counter | B | 10.4 | pKi | 0.04 | nM | Ki | J Med Chem (2015) 58: 9731-9741 [PMID:26630444] |
ChEMBL | Activity at VDR in rat osteosarcoma cells assessed as induction of 24-hydroxylase reporter gene transcription by luciferase reporter gene assay | B | 9.52 | pEC50 | 0.3 | nM | EC50 | Bioorg Med Chem (2009) 17: 7658-7669 [PMID:19819702] |
ChEMBL | Activity at VDR in rat osteosarcoma cells assessed as 24-hydroxylase transcription by reporter gene assay | B | 9.7 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2007) 50: 6154-6164 [PMID:17960924] |
ChEMBL | Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcriptional activation after 16 hrs by luciferase reporter gene assay | B | 9.7 | pEC50 | 0.2 | nM | EC50 | Bioorg Med Chem (2008) 16: 8563-8573 [PMID:18722130] |
ChEMBL | Activity at VDR in rat ROS 17/2.8 cells assessed as transcriptional activation of 24-hydroxylase gene promoter after 16 hrs by luciferase reporter gene assay | B | 9.7 | pEC50 | 0.2 | nM | EC50 | Bioorg Med Chem (2009) 17: 1747-1763 [PMID:19167893] |
ChEMBL | Agonist activity at rat VDR in ROS 17/2.8 cells transfected with Cyp24a1 reporter plasmid assessed as increase in Cyp24a1 transcription after 16 hrs by luciferase reporter gene assay | F | 9.7 | pEC50 | 0.2 | nM | EC50 | Bioorg Med Chem (2011) 19: 7205-7220 [PMID:22018918] |
ChEMBL | Displacement of [3H]1,25-(OH)2D3 from rat recombinant His-tagged VDR ligand-binding domain expressed in Escherichia coli BL21 | B | 10 | pEC50 | 0.1 | nM | EC50 | Bioorg Med Chem (2008) 16: 457-473 [PMID:17904370] |
ChEMBL | Displacement of 1-alpha,25-dihydroxyvitamin from rat recombinant VDR | B | 10.3 | pEC50 | 0.05 | nM | EC50 | J Med Chem (2007) 50: 6154-6164 [PMID:17960924] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]