General Information of the Protein
Protein ID
PT02576
Protein Name
Vitamin D3 receptor
Secondarily
Protein Name
1,25-dihydroxyvitamin D3 receptor
Nuclear receptor subfamily 1 group I member 1
Gene Name
VDR
Secondarily
Gene Name
Nr1i1
Sequence
MEATAASTSLPDPGDFDRNVPRICGVCGDRATGFHFNAMTCEGCKGFFRRSMKRKALFTCPFNGDCRITKDNRRHCQACRLKRCVDIGMMKEFILTDEEVQRKREMIMKRKEEEALKDSLRPKLSEEQQHIIAILLDAHHKTYDPTYADFRDFRPPVRMDGSTGSYSPRPTLSFSGNSSSSSSDLYTTSLDMMEPSGFSNLDLNGEDSDDPSVTLDLSPLSMLPHLADLVSYSIQKVIGFAKMIPGFRDLTSDDQIVLLKSSAIEVIMLRSNQSFTMDDMSWDCGSQDYKYDVTDVSKAGHTLELIEPLIKFQVGLKKLNLHEEEHVLLMAICIVSPDRPGVQDAKLVEAIQDRLSNTLQTYIRCRHPPPGSHQLYAKMIQKLADLRSLNEEHSKQYRSLSFQPENSMKLTPLVLEVFGNEIS
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Organism
Rattus norvegicus, Rat
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 1
>
Nuclear hormone receptor subfamily 1 group I
>
Nuclear hormone receptor subfamily 1 group I member 1
Function
Nuclear receptor for calcitriol, the active form of vitamin D3 which mediates the action of this vitamin on cells (PubMed:17227670). Enters the nucleus upon vitamin D3 binding where it forms heterodimers with the retinoid X receptor/RXR (By similarity). The VDR-RXR heterodimers bind to specific response elements on DNA and activate the transcription of vitamin D3-responsive target genes (By similarity). Plays a central role in calcium homeostasis (PubMed:17227670). Also functions as a receptor for the secondary bile acid lithocholic acid (LCA) and its metabolites (By similarity).
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Uniprot ID
P13053
Subcellular Location
Nucleus
Cytoplasm
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000994 , ROS 17/2.8
Compound ID Compound Name Compound Formula
CP0003145
(1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol
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C27H44O3
 2
1
EC50 = 0.2 nM
   TI
   LI
   LO
   TS
2
Ki = 0.2 nM
   TI
   LI
   LO
   TS
CP0211914
(1R,3R)-5-[(E)-(5'R,7'S)-11'-Hydroxy-5',7',11'-trimethyldodec-2'-enylidene]-2-methylene-cyclohexane-1,3-diol
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C22H38O3
 1
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
CP0222076
(1R,3R)-5-((R)-11-hydroxy-7,11-dimethyldodec-2-enylidene)-2-methylenecyclohexane-1,3-diol
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C21H36O3
 1
1
EC50 = 50 nM
   TI
   LI
   LO
   TS
CP0211913
(1R,3R)-5-[(E)-(5'S,7'S)-11'-hydroxy-5',7',11'-trimethyldodec-2'-enylidene]-2-methylene-cyclohexane-1,3-diol
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C22H38O3
 1
1
EC50 = 90 nM
   TI
   LI
   LO
   TS
CP0194570
(20S)-1alpha,25-Dihydroxy-2-methylene-8(12),14(17)-diseco-13(17)-dehydro-9,11,15,16,18,19-hexanorvitamin D3
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C22H36O3
 1
1
EC50 = 100 nM
   TI
   LI
   LO
   TS
CP0230663
(7Z)-(20S)-1alpha,25-Dihydroxy-2-methylene-8(12),14(17)-diseco-13(17)-dehydro-9,11,15,16,18,19-hexanorvitamin D3
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C22H36O3
 1
1
EC50 = 100 nM
   TI
   LI
   LO
   TS
CP0044715
(1R,3R)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2S,6R)-6-hydroxyheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-methylidenecyclohexane-1,3-diol
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C26H42O3
 1
1
Ki = 0.01 nM
   TI
   LI
   LO
   TS
CP0747032
(20S,25S)-2-methylene-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H42O3
 1
1
Ki = 0.06 nM
   TI
   LI
   LO
   TS
CP0752274
(20S,25S)-2alpha-methyl-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H44O3
 1
1
Ki = 0.08 nM
   TI
   LI
   LO
   TS
CP0103738
(1R,3R)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R,6R)-6-hydroxyheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-methylidenecyclohexane-1,3-diol
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C26H42O3
 1
1
Ki = 0.2 nM
   TI
   LI
   LO
   TS
CP0651809
(20R,25S)-2-methylene-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H42O3
 1
1
Ki = 0.4 nM
   TI
   LI
   LO
   TS
CP0657068
(20R,25R)-2alpha-methyl-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H44O3
 1
1
Ki = 0.4 nM
   TI
   LI
   LO
   TS
CP0651810
(20R,25S)-2alpha-methyl-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H44O3
 1
1
Ki = 0.6 nM
   TI
   LI
   LO
   TS
CP0651808
(20S,25R)-2beta-methyl-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H44O3
 1
1
Ki = 1 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0003145
(1S,3R,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol
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C27H44O3
 4
1 EC50 = 0.05 nM
2 Ki = 0.04 nM
3 Ki = 0.05 nM
4 Ki = 0.1 nM
CP0747032
(20S,25S)-2-methylene-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H42O3
 1
1 Ki = 0.06 nM
CP0044715
(1R,3R)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2S,6R)-6-hydroxyheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-methylidenecyclohexane-1,3-diol
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C26H42O3
 1
1 Ki = 0.09 nM
CP0103738
(1R,3R)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R,6R)-6-hydroxyheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-methylidenecyclohexane-1,3-diol
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C26H42O3
 1
1 Ki = 0.1 nM
CP0651809
(20R,25S)-2-methylene-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H42O3
 1
1 Ki = 0.1 nM
CP0752274
(20S,25S)-2alpha-methyl-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H44O3
 1
1 Ki = 0.1 nM
CP0651810
(20R,25S)-2alpha-methyl-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H44O3
 1
1 Ki = 0.2 nM
CP0657068
(20R,25R)-2alpha-methyl-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H44O3
 1
1 Ki = 0.3 nM
CP0651808
(20S,25R)-2beta-methyl-19,26-dinor-1alpha,25-dihydroxyvitamin D3
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C26H44O3
 1
1 Ki = 0.4 nM
CP0347418
(23S)-25-dehydro-2-methylene-19-nor-1alpha-hydroxyvitaminD3-26,23-lactone
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C27H38O4
 1
1 Ki = 1 nM
CP0347419
(23R)-25-dehydro-2-methylene-19-nor-1alpha-hydroxyvitaminD3-26,23-lactone
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C27H38O4
 1
1 Ki = 2 nM
CP0260172
(1R,3R)-5-[(E,7S)-11-hydroxy-5,5,7,11-tetramethyldodec-2-enylidene]-2-methylidenecyclohexane-1,3-diol
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C23H40O3
 1
1 Ki = 2 nM
CP0211913
(1R,3R)-5-[(E)-(5'S,7'S)-11'-hydroxy-5',7',11'-trimethyldodec-2'-enylidene]-2-methylene-cyclohexane-1,3-diol
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C22H38O3
 1
1 Ki = 10 nM
CP0106177
(1R,3R)-5-[(Z,7S)-11-hydroxy-5,5,7,11-tetramethyldodec-2-enylidene]-2-methylidenecyclohexane-1,3-diol
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C23H40O3
 1
1 Ki = 10 nM
CP0211914
(1R,3R)-5-[(E)-(5'R,7'S)-11'-Hydroxy-5',7',11'-trimethyldodec-2'-enylidene]-2-methylene-cyclohexane-1,3-diol
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C22H38O3
 1
1 Ki = 30 nM
CP0222076
(1R,3R)-5-((R)-11-hydroxy-7,11-dimethyldodec-2-enylidene)-2-methylenecyclohexane-1,3-diol
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C21H36O3
 1
1 Ki = 50 nM
CP0194570
(20S)-1alpha,25-Dihydroxy-2-methylene-8(12),14(17)-diseco-13(17)-dehydro-9,11,15,16,18,19-hexanorvitamin D3
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C22H36O3
 1
1 Ki = 60 nM
CP0230663
(7Z)-(20S)-1alpha,25-Dihydroxy-2-methylene-8(12),14(17)-diseco-13(17)-dehydro-9,11,15,16,18,19-hexanorvitamin D3
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C22H36O3
 1
1 Ki > 1000 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT06288 Vitamin D3 receptor Mus musculus, Mouse
50% Identity
Protein ID Protein Name Protein Organism
PT02378 Vitamin D3 receptor Homo sapiens, Human