ChEMBL ligand: CHEMBL846 (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-215535, RO-21-5535, Rocaltrol, Silkis, Topitriol, Vectical)
Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] There should be some charts here, you may need to enable JavaScript!
Vitamin D receptor/Retinoid X receptor-α/Retinoic acid receptor RXR-alpha/Vitamin D3 receptor in Human [ChEMBL: CHEMBL3885632] [GtoPdb: 605, 610] [UniProtKB: P11473, P19793] There should be some charts here, you may need to enable JavaScript!
Vitamin D3 receptor in Pig [ChEMBL: CHEMBL5304] [UniProtKB: A3RGC1] There should be some charts here, you may need to enable JavaScript!
Vitamin D3 receptor A in Danio rerio [ChEMBL: CHEMBL3217399] [UniProtKB: Q9PTN2] There should be some charts here, you may need to enable JavaScript!
Vitamin D-binding protein in Human [ChEMBL: CHEMBL2259] [UniProtKB: P02774] There should be some charts here, you may need to enable JavaScript!
Vitamin D receptor in Chicken [ChEMBL: CHEMBL2353] [UniProtKB: O42392] Vitamin D receptor in Human [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473] Vitamin D receptor in Bovine [ChEMBL: CHEMBL3452] [UniProtKB: Q28037] Vitamin D receptor in Mouse [ChEMBL: CHEMBL5601] [UniProtKB: P48281] Vitamin D receptor in Rat [ChEMBL: CHEMBL3150] [GtoPdb: 605] [UniProtKB: P13053] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
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	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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]