Target family: 1I. Vitamin D receptor-like receptors (type: nhr)
Target: Vitamin D receptor

Ligand: ZK159222 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Design and synthesis of potent vitamin D receptor antagonists with A-ring modifications: remarkable effects of 2alpha-methyl introduction on antagonistic activity.
Published in: Bioorg Med Chem

Ligand: ZK159222 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Carboxylic ester antagonists of 1alpha,25-dihydroxyvitamin D(3) show cell-specific actions.
Published in: Chem Biol

Ligand: TEI-9647 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Further synthetic and biological studies on vitamin D hormone antagonists based on C24-alkylation and C2alpha-functionalization of 25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones.
Published in: J Med Chem

Ligand: tacalcitol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKd
Reference (Journal): Profile of ligand specificity of the vitamin D binding protein for 1 alpha,25-dihydroxyvitamin D3 and its analogs.
Published in: J Bone Miner Res

Ligand: seocalcitol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKd
Reference (Journal): Studies on two new vitamin D analogs, EB 1089 and KH 1060: effects on bone resorption and osteoclast recruitment in vitro.
Published in: Bone

Ligand: seocalcitol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKd
Reference (Journal): EB1089: a new vitamin D analogue that inhibits the growth of breast cancer cells in vivo and in vitro.
Published in: Biochem Pharmacol

Ligand: paricalcitol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: yes
Median affinity:  -

Ligand: maxacalcitol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.21 pEC50
Reference (Journal): Effects of two new vitamin D3 derivatives, 22-oxa-1 alpha-25-dihydroxyvitamin D3 (OCT) and 2 beta-(3-hydroxypropoxy)-1 alpha, 25-dihydroxyvitamin D3 (ED-71), on bone metabolism in organ culture.
Published in: Bone

Ligand: lithocholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.1 pKi
Reference (Journal): Vitamin D receptor as an intestinal bile acid sensor.
Published in: Science

Ligand: LG190178 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.82 pKi
Reference (Journal): Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3.
Published in: Chem Biol

Ligand: lexacalcitol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 10.1 pKd
Reference (Journal): Studies on two new vitamin D analogs, EB 1089 and KH 1060: effects on bone resorption and osteoclast recruitment in vitro.
Published in: Bone

Ligand: inecalcitol (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.279999732971191 pKd
Reference (Journal): Two novel 14-Epi-analogues of 1,25-dihydroxyvitamin D3 inhibit the growth of human breast cancer cells in vitro and in vivo.
Published in: Cancer Res

Ligand: gemini (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.5 pKd
Reference (Journal): Novel Gemini analogs of 1alpha,25-dihydroxyvitamin D(3) with enhanced transcriptional activity.
Published in: Biochem Pharmacol

Ligand: falecalcitriol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKd
Reference (Journal): Synthesis and biological evaluations of A-ring isomers of 26,26,26,27,27,27-hexafluoro-1,25-dihydroxyvitamin D3.
Published in: Bioorg Med Chem

Ligand: elocalcitol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.21 pIC50
Reference (Journal): Cellular and molecular events associated with the bone-protecting activity of the noncalcemic vitamin D analog Ro-26-9228 in osteopenic rats.
Published in: Endocrinology

Ligand: eldecalcitol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: Japan only
Median affinity: 8 pKd
Reference (Journal): Synthetic studies of vitamin D analogues. XIV. Synthesis and calcium regulating activity of vitamin D3 analogues bearing a hydroxyalkoxy group at the 2 beta-position.
Published in: Chem Pharm Bull

Ligand: doxercalciferol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2000)
Primary target: no
Median affinity:  -

Ligand: calcitriol-26,23-lactone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.5 pKd
Reference (Journal): Biological activity of 24,24-difluoro-1 alpha, 25-dihydroxyvitamin D3 and 1 alpha, 25-dihydroxyvitamin D3-26,23-lactone in inducing differentiation of human myeloid leukemia cells.
Published in: Arch Biochem Biophys

Ligand: calcipotriol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: UK (1991), FDA (1993)
Primary target: yes
Median affinity: 9.300000190734863 pKd
Reference (Journal): Profile of ligand specificity of the vitamin D binding protein for 1 alpha,25-dihydroxyvitamin D3 and its analogs.
Published in: J Bone Miner Res

Ligand: 3-keto-lithocholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.54 pKi
Reference (Journal): Vitamin D receptor as an intestinal bile acid sensor.
Published in: Science

Ligand: 2MD (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 10 pEC50
Reference (Journal): New 1alpha,25-dihydroxy-19-norvitamin D3 compounds of high biological activity: synthesis and biological evaluation of 2-hydroxymethyl, 2-methyl, and 2-methylene analogues.
Published in: J Med Chem

Ligand: 1,25-dihydroxyvitamin D3 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1978)
Primary target: yes
Median affinity:  pKd
Reference (Journal): Deletion of deoxyribonucleic acid binding domain of the vitamin D receptor abrogates genomic and nongenomic functions of vitamin D.
Published in: Mol Endocrinol

Ligand: 1,25-dihydroxyvitamin D3 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1978)
Primary target: yes
Median affinity:  pKd
Reference (Journal): Profile of ligand specificity of the vitamin D binding protein for 1 alpha,25-dihydroxyvitamin D3 and its analogs.
Published in: J Bone Miner Res