General Information of the Protein
Protein ID
PT02378
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
MEAMAASTSLPDPGDFDRNVPRICGVCGDRATGFHFNAMTCEGCKGFFRRSMKRKALFTCPFNGDCRITKDNRRHCQACRLKRCVDIGMMKEFILTDEEVQRKREMILKRKEEEALKDSLRPKLSEEQQRIIAILLDAHHKTYDPTYSDFCQFRPPVRVNDGGGSHPSRPNSRHTPSFSGDSSSSCSDHCITSSDMMDSSSFSNLDLSEEDSDDPSVTLELSQLSMLPHLADLVSYSIQKVIGFAKMIPGFRDLTSEDQIVLLKSSAIEVIMLRSNESFTMDDMSWTCGNQDYKYRVSDVTKAGHSLELIEPLIKFQVGLKKLNLHEEEHVLLMAICIVSPDRPGVQDAALIEAIQDRLSNTLQTYIRCRHPPPGSHLLYAKMIQKLADLRSLNEEHSKQYRCLSFQPECSMKLTPLVLEVFGNEIS
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Organism
Homo sapiens, Human
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:28698609, PubMed:16913708, PubMed:15728261, PubMed:10678179). Enters the nucleus upon vitamin D3 binding where it forms heterodimers with the retinoid X receptor/RXR (PubMed:28698609). The VDR-RXR heterodimers bind to specific response elements on DNA and activate the transcription of vitamin D3-responsive target genes (PubMed:28698609). Plays a central role in calcium homeostasis (By similarity). Also functions as a receptor for the secondary bile acid lithocholic acid (LCA) and its metabolites (PubMed:12016314, PubMed:32354638).
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Uniprot ID
Primary ID:
P11473

Secondarily ID:
B2R5Q1
G3V1V9
Q5PSV3
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HGNC ID
HGNC:12679
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: CL000109 , COS-1
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
 1
1
IC50 = 0.8 nM
   TI
   LI
   LO
   TS
CP0552250
(1R,3S,Z)-5-((E)-2-((1R,3aS,7aR)-1-((S)-1-(4,4-dimethylpent-2-ynyloxy)propan-2-yl)-7a-methyl-octahydroinden-4-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol
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C29H44O3
 1
1
IC50 = 47 nM
   TI
   LI
   LO
   TS
CP0523217
(1R,3S,Z)-5-((E)-2-((1R,3aS,7aR)-1-((S)-1-(benzyloxy)propan-2-yl)-7a-methyl-octahydroinden-4-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol
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C29H40O3
 1
1
IC50 = 63 nM
   TI
   LI
   LO
   TS
CP0426994
(1R,3S,Z)-5-((E)-2-((1R,3aS,7aR)-1-((S)-1-(3,3-dimethyl-2-methylenebutoxy)propan-2-yl)-7a-methyl-octahydroinden-4-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol
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C29H46O3
 1
1
IC50 = 85 nM
   TI
   LI
   LO
   TS
CP0523218
(1R,3S,Z)-5-((E)-2-((1R,3aS,7aR)-7a-methyl-1-((S)-1-(2-(1-methylcyclohexyl)allyloxy)propan-2-yl)-octahydroinden-4-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol
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C32H50O3
 1
1
IC50 = 198 nM
   TI
   LI
   LO
   TS
CP0528403
(1R,3S,Z)-5-((E)-2-((1R,3aS,7aR)-1-((S)-1-(2-(6,6-dimethylcyclohex-1-enyl)allyloxy)propan-2-yl)-7a-methyl-octahydroinden-4-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol
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C33H50O3
 1
1
IC50 = 300 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
 13
1 EC50 = 0.1 nM
2 EC50 = 7.7 nM
3 EC50 = 15 nM
4 ED50 = 0.5 nM
5 IC50 = 0.35 nM
6 IC50 = 0.7 nM
7 IC50 = 1.13 nM
8 IC50 = 1.24 nM
9 IC50 = 1.3 nM
10 IC50 = 1.42 nM
11 IC50 = 9.3 nM
12 IC50 = 13 nM
13 Kd = 0.065 nM
CP0134848
LG-190178
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C28H42O5
 1
1 EC50 = 40 nM
CP0216245
LG190155
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C31H44O4
 1
1 EC50 = 40 nM
CP0235442
(2S,3S,4S,5R,6R)-6-[[(3R,5R,8R,9S,10S,13R,14S,17R)-17-[(2R)-4-carboxybutan-2-yl]-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl]oxy]-3,4,5-trihydroxyoxane-2-carboxylic acid
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C30H48O9
 1
1 EC50 = 12300 nM
CP0203797
(2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-[(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]oxyoxane-2-carboxylic acid
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C30H48O9
 1
1 EC50 = 21300 nM
CP0283742
(1S,3Z,5S)-3-[(2E)-2-[(3aS,7aS)-1-[(2R)-6-ethyl-5,5-difluoro-6-hydroxyoctan-2-yl]-7a-methyl-3a,5,6,7-tetrahydro-3H-inden-4-ylidene]ethylidene]-5-(difluoromethyl)-4-methylidenecyclohexan-1-ol
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C30H44F4O2
 2
1 ED50 = 4 nM
2 IC50 = 50 nM
CP0198154
(1S,3Z,5S)-3-[(2E)-2-[(1S,3aS,7aS)-1-[(1R)-1-(4-ethyl-4-hydroxyhexoxy)ethyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-5-(difluoromethyl)-4-methylidenecyclohexan-1-ol
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C30H48F2O3
 2
1 ED50 = 100 nM
2 IC50 = 19.5 nM
CP0283743
(1S,3S,Z)-3-(difluoromethyl)-5-((E)-2-((1R,3aS,7aR)-1-((R)-6-hydroxy-6-methylheptan-2-yl)-7a-methyl-octahydroinden-4-ylidene)ethylidene)-4-methylenecyclohexanol
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C28H44F2O2
 2
1 ED50 = 500 nM
2 IC50 = 30 nM
CP0149325
(1R,3S,5Z)-5-[(E)-3-[3-(6-hydroxy-6-methylheptyl)phenyl]dec-2-enylidene]-4-methylidenecyclohexane-1,3-diol
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C31H48O3
 1
1 IC50 = 3.5 nM
CP0072528
(1R,3S,5Z)-5-[(E)-3-[3-(6-hydroxy-6-methylheptyl)phenyl]pent-2-enylidene]-4-methylidenecyclohexane-1,3-diol
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C26H38O3
 1
1 IC50 = 4.5 nM
CP0148647
(1R,3R)-5-[(2E)-2-[(1S,3aS,7aS)-1-[(5S)-5-(1-adamantyl)-5-hydroxypenta-1,3-diynyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-methylidenecyclohexane-1,3-diol
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C34H44O3
 1
1 IC50 = 5 nM
CP0149324
(1R,3S,5Z)-5-[(E)-3-[3-(6-hydroxy-6-methylheptyl)phenyl]hex-2-enylidene]-4-methylidenecyclohexane-1,3-diol
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C27H40O3
 1
1 IC50 = 5.6 nM
CP0242002
(1R,3S,5Z)-5-[(E)-3-[3-(6-hydroxy-6-methylheptyl)phenyl]non-2-enylidene]-4-methylidenecyclohexane-1,3-diol
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C30H46O3
 1
1 IC50 = 8.3 nM
CP0242003
(1R,3S,5Z)-5-[(E)-3-[3-(6-hydroxy-6-methylheptyl)phenyl]hept-2-enylidene]-4-methylidenecyclohexane-1,3-diol
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C28H42O3
 1
1 IC50 = 10 nM
CP0148646
(1R,3R)-5-[(2E)-2-[(1S,3aS,7aS)-1-[(5R)-5-(1-adamantyl)-5-hydroxypenta-1,3-diynyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-methylidenecyclohexane-1,3-diol
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C34H44O3
 1
1 IC50 = 12.5 nM
CP0256628
(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7R,7aR)-7-(7-hydroxy-7-methyloctyl)-1-[(2R)-5-hydroxypentan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
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C33H56O4
 1
1 IC50 = 15.7 nM
CP0247674
(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7R,7aR)-7-(7-hydroxy-7-methyloctyl)-1-[(2S)-1-hydroxypropan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
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C31H52O4
 1
1 IC50 = 20.9 nM
CP0187961
(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7R,7aR)-1-[(2R)-4-hydroxybutan-2-yl]-7-(7-hydroxy-7-methyloctyl)-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
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C32H54O4
 1
1 IC50 = 27.3 nM
CP0065795
(1R,3R)-5-[(2E)-2-[(1S,3aS,7aS)-1-[(5R)-6-(1-adamantyl)-5-hydroxyhexa-1,3-diynyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-methylidenecyclohexane-1,3-diol
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C35H46O3
 1
1 IC50 = 35 nM
CP0230842
(1R,3R)-5-[(2E)-2-[(1S,3aS,7aS)-1-[(5S)-6-(1-adamantyl)-5-hydroxyhexa-1,3-diynyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-methylidenecyclohexane-1,3-diol
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C35H46O3
 1
1 IC50 = 35 nM
CP0149000
N-[3-(diethylamino)propyl]-1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carboxamide
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C32H53N3O3
 1
1 IC50 = 71.06 nM
CP0072299
7-Dehydrocholesterol
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C27H44O
 1
1 IC50 = 87 nM
CP0008907
N-[2-(diethylamino)ethyl]-1-ethyl-5-[3-[3-methyl-4-(methylsulfanylmethoxy)phenyl]pentan-3-yl]pyrrole-2-carboxamide
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C27H43N3O2S
 1
1 IC50 = 89.1 nM
CP0008908
1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]-N-[(2S)-1-hydroxypropan-2-yl]pyrrole-2-carboxamide
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C28H44N2O4
 1
1 IC50 = 115.3 nM
CP0006113
4-[3-[4-(benzenesulfonylmethoxy)-3-methylphenyl]pentan-3-yl]-N-[2-(diethylamino)ethyl]-1-ethylpyrrole-2-carboxamide
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C32H45N3O4S
 1
1 IC50 = 125.4 nM
CP0099447
N-(2-aminoethyl)-1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carboxamide
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C27H43N3O3
 1
1 IC50 = 194.3 nM
CP0469317
N-[3-(dimethylamino)propyl]-1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carboxamide
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C30H49N3O3
 1
1 IC50 = 196.6 nM
CP0207144
1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]-N-(1-hydroxypropan-2-yl)pyrrole-2-carboxamide
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C28H44N2O4
 1
1 IC50 = 228 nM
CP0326260
N-[2-(diethylamino)ethyl]-1-ethyl-5-[3-[4-(3-ethyl-3-hydroxypentoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carboxamide
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C32H53N3O3
 1
1 IC50 = 271.2 nM
CP0127889
N-[3-(diethylamino)propyl]-1-ethyl-5-[3-[4-(3-ethyl-3-hydroxypentoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carboxamide
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C33H55N3O3
 1
1 IC50 = 295.8 nM
CP0313015
(2S,3R)-2-[[1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carbonyl]amino]-3-methylpentanoic acid
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C31H48N2O5
 1
1 IC50 = 389.3 nM
CP0180831
1-ethyl-5-[3-[4-(3-ethyl-3-hydroxypentoxy)-3-methylphenyl]pentan-3-yl]-N-(3-morpholin-4-ylpropyl)pyrrole-2-carboxamide
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C33H53N3O4
 1
1 IC50 = 406.1 nM
CP0225335
(2S,3R)-2-[[5-[3-[4-(3,3-dimethyl-2-oxobutoxy)-3-methylphenyl]pentan-3-yl]-1-ethylpyrrole-2-carbonyl]amino]-3-methylpentanoic acid
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C31H46N2O5
 1
1 IC50 = 563.6 nM
CP0326261
N-(cyanomethyl)-1-ethyl-5-[3-[4-(3-ethyl-3-hydroxypentoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carboxamide
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C28H41N3O3
 1
1 IC50 = 825 nM
CP0100481
N-[3-(diethylamino)propyl]-5-[3-[4-(3,3-dimethyl-2-oxobutoxy)-3-methylphenyl]pentan-3-yl]-1-ethylpyrrole-2-carboxamide
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C32H51N3O3
 1
1 IC50 = 863 nM
CP0227920
2-[[1-ethyl-5-[3-[4-(3-ethyl-3-hydroxypentoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carbonyl]-methylamino]acetic acid
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C29H44N2O5
 1
1 IC50 = 873.1 nM
CP0321314
N-(2-aminoethyl)-5-[3-[4-(3,3-dimethyl-2-oxobutoxy)-3-methylphenyl]pentan-3-yl]-1-ethylpyrrole-2-carboxamide
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C27H41N3O3
 1
1 IC50 = 1007 nM
CP0313014
1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]-N-(3-morpholin-4-ylpropyl)pyrrole-2-carboxamide
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C32H51N3O4
 1
1 IC50 = 1189 nM
CP0250425
methyl 2-[(E)-2-(4-methoxyphenyl)ethenyl]-1,3,3-trimethylindol-1-ium-5-carboxylate
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C22H24NO3+
 1
1 IC50 = 3300 nM
CP0366053
5-[3-[4-(3,3-dimethyl-2-oxobutoxy)-3-methylphenyl]pentan-3-yl]-1-ethyl-N-(3-morpholin-4-ylpropyl)pyrrole-2-carboxamide
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C32H49N3O4
 1
1 IC50 = 3521 nM
CP0237889
5-methoxy-2-[(E)-2-(4-methoxyphenyl)ethenyl]-1,3,3-trimethylindol-1-ium
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C21H24NO2+
 1
1 IC50 = 3900 nM
CP0331561
N-(4-ethoxyphenyl)-1-ethyl-5-[3-[4-(3-ethyl-3-hydroxypentoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carboxamide
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C34H48N2O4
 1
1 IC50 = 4543 nM
CP0552229
N-(2,2-dimethoxyethyl)-1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carboxamide
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C29H46N2O5
 1
1 IC50 = 5235 nM
CP0341779
methyl 2-[(E)-2-(4-ethoxyphenyl)ethenyl]-1,3,3-trimethylindol-1-ium-5-carboxylate
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C23H26NO3+
 1
1 IC50 = 5900 nM
CP0341777
4-(4-fluorophenyl)sulfonyl-5-(2-methylpropylsulfonyl)-2-thiophen-2-yl-1,3-oxazole
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C17H16FNO5S3
 1
1 IC50 = 6900 nM
CP0502940
4-(4-fluorophenyl)sulfonyl-5-propylsulfonyl-2-thiophen-2-yl-1,3-oxazole
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C16H14FNO5S3
 1
1 IC50 = 7100 nM
CP0270650
N-[(2-chlorophenyl)-(2-methyl-1H-indol-3-yl)methyl]-3,4-dimethoxyaniline
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C24H23ClN2O2
 1
1 IC50 = 7200 nM
CP0283396
N-benzyl-1-(2-chlorophenyl)-1-(2-methyl-1H-indol-3-yl)methanamine
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C23H21ClN2
 1
1 IC50 = 7200 nM
CP0383342
4-(benzenesulfonyl)-5-ethylsulfonyl-2-thiophen-2-yl-1,3-oxazole
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C15H13NO5S3
 1
1 IC50 = 8100 nM
CP0154442
methyl 4-[(E)-2-(5-methoxy-1,3,3-trimethylindol-1-ium-2-yl)ethenyl]benzoate
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C22H24NO3+
 1
1 IC50 = 8600 nM
CP0197019
N-(4-ethoxyphenyl)-1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carboxamide
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C33H46N2O4
 1
1 IC50 = 9245 nM
CP0201030
1-(2-chlorophenyl)-1-(2,6-dimethyl-1H-indol-3-yl)-N-[(4-methylphenyl)methyl]methanamine
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C25H25ClN2
 1
1 IC50 = 9500 nM
CP0061777
(1,3-dioxoisoindol-2-yl) 4-ethylbenzenesulfonate
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C16H13NO5S
 1
1 IC50 = 10500 nM
CP0174891
3,4-dimethoxy-N-[(4-methoxyphenyl)-(2-methyl-1H-indol-3-yl)methyl]aniline
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C25H26N2O3
 1
1 IC50 = 11300 nM
CP0070398
4-chloro-N-[(2-methyl-1H-indol-3-yl)-(1,3-thiazol-2-yl)methyl]aniline
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C19H16ClN3S
 1
1 IC50 = 11900 nM
CP0134640
N-[(4-methoxyphenyl)-(2-methyl-1H-indol-3-yl)methyl]-4-(trifluoromethyl)aniline
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C24H21F3N2O
 1
1 IC50 = 12400 nM
CP0349887
N-[(2-chlorophenyl)-(2-methyl-1H-indol-3-yl)methyl]-3,4-dimethylaniline
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C24H23ClN2
 1
1 IC50 = 12800 nM
CP0341778
2-[(E)-2-(4-hydroxyphenyl)ethenyl]-1,3,3-trimethyl-5-indol-1-iumcarboxylic acid methyl ester;iodide
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C21H22NO3+
 1
1 IC50 = 13800 nM
CP0387891
4-chloro-N-[(2-methoxypyridin-3-yl)-(2-methyl-1H-indol-3-yl)methyl]aniline
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C22H20ClN3O
 1
1 IC50 = 14200 nM
CP0249991
N-[(2-methyl-1H-indol-3-yl)-(4-propan-2-ylphenyl)methyl]pyridin-2-amine
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C24H25N3
 1
1 IC50 = 15300 nM
CP0134642
4-chloro-N-[(2-chlorophenyl)-(2,6-dimethyl-1H-indol-3-yl)methyl]aniline
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C23H20Cl2N2
 1
1 IC50 = 15600 nM
CP0134641
N-[(2-chlorophenyl)-(2-methyl-1H-indol-3-yl)methyl]-2-methyl-1,3-benzothiazol-5-amine
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C24H20ClN3S
 1
1 IC50 = 15800 nM
CP0070399
4-chloro-N-[1H-imidazol-2-yl-(2-methyl-1H-indol-3-yl)methyl]aniline
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C19H17ClN4
 1
1 IC50 = 16700 nM
CP0263042
N-[(2-chlorophenyl)-(2,6-dimethyl-1H-indol-3-yl)methyl]-4-(trifluoromethoxy)aniline
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C24H20ClF3N2O
 1
1 IC50 = 17200 nM
CP0349886
3,4-dimethoxy-N-[(2-methyl-1H-indol-3-yl)-(1,3-thiazol-2-yl)methyl]aniline
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C21H21N3O2S
 1
1 IC50 = 17300 nM
CP0249990
N-[(2-chlorophenyl)-(2-methyl-1H-indol-3-yl)methyl]-4-methylaniline
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C23H21ClN2
 1
1 IC50 = 17700 nM
CP0060349
(S)-8-amino-2-isobutyl-4-isopentyl-7-(2-methylprop-1-enyl)-4,5-dihydro-1H-benzo[e][1,4]diazepin-3(2H)-one
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C22H35N3O
 1
1 IC50 = 20000 nM
CP0341775
N-[(2-chlorophenyl)-(1H-indol-3-yl)methyl]aniline
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C21H17ClN2
 1
1 IC50 = 20300 nM
CP0070402
3,4-dimethoxy-N-[(2-methyl-1H-indol-3-yl)-[4-(trifluoromethyl)phenyl]methyl]aniline
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C25H23F3N2O2
 1
1 IC50 = 21800 nM
CP0290920
4-(benzenesulfonyl)-5-propan-2-ylsulfonyl-2-thiophen-2-yl-1,3-oxazole
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C16H15NO5S3
 1
1 IC50 = 22300 nM
CP0421524
3,4-dimethoxy-N-[(2-methyl-1H-indol-3-yl)-[4-(trifluoromethoxy)phenyl]methyl]aniline
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C25H23F3N2O3
 1
1 IC50 = 22800 nM
CP0154437
N-[(2-chlorophenyl)-(2-methyl-1H-indol-3-yl)methyl]-2-methoxyaniline
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C23H21ClN2O
 1
1 IC50 = 24300 nM
CP0061845
4-chloro-N-[(2-chlorophenyl)-(2-methyl-1H-indol-3-yl)methyl]aniline
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C22H18Cl2N2
 8
1 IC50 = 25400 nM
2 IC50 = 28500 nM
3 IC50 = 33100 nM
4 IC50 = 36800 nM
5 IC50 = 37500 nM
6 IC50 = 45400 nM
7 IC50 = 54500 nM
8 IC50 = 82200 nM
CP0061773
N-[(2-chlorophenyl)-(2-methyl-1H-indol-3-yl)methyl]-4-methoxyaniline
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C23H21ClN2O
 1
1 IC50 = 26500 nM
CP0089919
N-[(2-methyl-1H-indol-3-yl)-(4-nitrophenyl)methyl]aniline
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C22H19N3O2
 1
1 IC50 = 28500 nM
CP0256918
N-[(2-chlorophenyl)-(2,6-dimethyl-1H-indol-3-yl)methyl]pyridin-3-amine
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C22H20ClN3
 1
1 IC50 = 29300 nM
CP0061775
N-[(2-methyl-1H-indol-3-yl)-naphthalen-2-ylmethyl]aniline
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C26H22N2
 1
1 IC50 = 29600 nM
CP0154438
N-[(2-chlorophenyl)-(2-methyl-1H-indol-3-yl)methyl]aniline
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C22H19ClN2
 1
1 IC50 = 29800 nM
CP0073903
8-amino-2,7-diisobutyl-4-isopentyl-4,5-dihydro-1H-benzo[e][1,4]diazepin-3(2H)-one
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C22H37N3O
 1
1 IC50 = 30000 nM
CP0154440
N-[(2-methyl-1H-indol-3-yl)-phenylmethyl]aniline
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C22H20N2
 1
1 IC50 = 30200 nM
CP0338247
N-[(4-methoxyphenyl)-(2-methyl-1H-indol-3-yl)methyl]aniline
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C23H22N2O
 1
1 IC50 = 31200 nM
CP0341776
N-[(4-chlorophenyl)-(2-methyl-1H-indol-3-yl)methyl]aniline
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C22H19ClN2
 1
1 IC50 = 31700 nM
CP0499764
N-[(2,6-dimethyl-1H-indol-3-yl)-pyridin-3-ylmethyl]-2-methoxypyridin-3-amine
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C22H22N4O
 1
1 IC50 = 32300 nM
CP0070401
1-(2-chlorophenyl)-1-(2,6-dimethyl-1H-indol-3-yl)-N-[[4-(trifluoromethyl)phenyl]methyl]methanamine
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C25H22ClF3N2
 1
1 IC50 = 35200 nM
CP0061776
N-[(2-methyl-1H-indol-3-yl)-(4-methylphenyl)methyl]aniline
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C23H22N2
 1
1 IC50 = 43600 nM
CP0431770
4-chloro-N-[(2-methyl-1H-indol-3-yl)-pyridin-4-ylmethyl]aniline
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C21H18ClN3
 1
1 IC50 = 51500 nM
CP0267831
3-[4-[anilino-(2-methyl-1H-indol-3-yl)methyl]phenyl]propan-1-ol
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C25H26N2O
 1
1 IC50 = 58600 nM
CP0204440
N-benzyl-1-(2-chlorophenyl)-1-(2,6-dimethyl-1H-indol-3-yl)methanamine
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C24H23ClN2
 1
1 IC50 = 59900 nM
CP0364456
4-chloro-N-[(2-chlorophenyl)-(6-methoxy-2-methyl-1H-indol-3-yl)methyl]aniline
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C23H20Cl2N2O
 1
1 IC50 = 63100 nM
CP0099450
N,N-bis(2-cyanoethyl)-1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]pyrrole-2-carboxamide
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C31H44N4O3
 1
1 IC50 > 10000 nM
CP0149001
1-ethyl-5-[3-[4-(2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl]pentan-3-yl]-N-prop-2-ynylpyrrole-2-carboxamide
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C28H40N2O3
 1
1 IC50 > 10000 nM
CP0070400
4-chloro-N-[(2-methyl-1H-indol-3-yl)-pyridin-3-ylmethyl]aniline
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C21H18ClN3
 1
1 IC50 > 75000 nM
CP0068212
(3alpha,5beta)-3-hydroxycholan-24-oic acid
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C24H40O3
 3
1 Kd = 330 nM
2 Kd = 9520 nM
3 Kd = 18870 nM
CP0162322
(S)-3-(4-(3-(4-((S)-2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl)pentan-3-yl)-2-methylphenoxy)propane-1,2-diol
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C28H42O5
 1
1 Ki = 11 nM
CP0104937
(2S)-3-{4-[1-ethyl-1-(4-{[(2R)-2-hydroxy-3,3-dimethylbutyl]oxy}-3-methylphenyl)propyl]-2-methylphenoxy}propane-1,2-diol
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C28H42O5
 1
1 Ki = 12 nM
CP0064103
(R)-3-(4-(3-(4-((R)-2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl)pentan-3-yl)-2-methylphenoxy)propane-1,2-diol
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C28H42O5
 1
1 Ki = 320 nM
CP0105737
(R)-3-(4-(3-(4-((S)-2-hydroxy-3,3-dimethylbutoxy)-3-methylphenyl)pentan-3-yl)-2-methylphenoxy)propane-1,2-diol
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C28H42O5
 1
1 Ki = 740 nM
Clinical Information about the Protein
Target 1 ( Vitamin D3 receptor (VDR) )
Target Type Successful Target
Disease 8 Target-related Diseases  8
1 Vitamin D deficiency [ICD-11: 5B57]
2 Psoriasis vulgaris [ICD-11: EA90]
3 Congenital alopecia [ICD-11: LC30]
4 Chronic kidney disease [ICD-11: GB61]
5 Hypoparathyroidism [ICD-11: 5A50]
6 Hyperparathyroidism [ICD-11: 5A51]
7 Rickets [ICD-11: 5B57]
8 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Approved Drug(s) 7 Approved Drugs  7
1 Calcidiol Approved
Vitamin D deficiency
2 Calcipotriol Approved
Psoriasis vulgaris
3 Calcitriol Approved
Congenital alopecia
4 Cholecalciferol Approved
Vitamin D deficiency
5 Doxercalciferol Approved
Chronic kidney disease
6 Ergocalciferol Approved
Hypoparathyroidism
7 Paricalcitol Approved
Hyperparathyroidism
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Seocalcitol Phase 3
Rickets
Discontinued Drug(s) 1 Discontinued Drug  1
1 Lexacalcitol Discontinued in Phase 2
Solid tumour/cancer
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02576 Vitamin D3 receptor Rattus norvegicus, Rat
PT06288 Vitamin D3 receptor Mus musculus, Mouse