General Information of the Protein
Protein ID
PT01109
Protein Name
11-beta-hydroxysteroid dehydrogenase 1
Secondarily
Protein Name
11-beta-hydroxysteroid dehydrogenase/microsomal carbonyl reductase
11beta-HSD1A
7-oxosteroid reductase
Corticosteroid 11-beta-dehydrogenase isozyme 1
liver-type 11-beta-HSD
Gene Name
HSD11B1
Secondarily
Gene Name
Hsd11
Sequence
MAVMKNYLLPILVLFLAYYYYSTNEEFRPEMLQGKKVIVTGASKGIGREMAYHLSKMGAHVVLTARSEEGLQKVVSRCLELGAASAHYIAGTMEDMTFAEQFIVKAGKLMGGLDMLILNHITQTSLSLFHDDIHSVRRVMEVNFLSYVVMSTAALPMLKQSNGSIAVISSLAGKMTQPMIAPYSASKFALDGFFSTIRTELYITKVNVSITLCVLGLIDTETAMKEISGIINAQASPKEECALEIIKGTALRKSEVYYDKSPLTPILLGNPGRKIMEFFSLRYYNKDMFVSN
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Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Oxidoreductase
Function
Controls the reversible conversion of biologically active glucocorticoids such as 11-dehydrocorticosterone to corticosterone in the presence of NADP(H) (PubMed:9405715, PubMed:23415904, PubMed:30902677). Participates in the corticosteroid receptor-mediated anti-inflammatory response, as well as metabolic and homeostatic processes (PubMed:9405715). Bidirectional in vitro, predominantly functions as a reductase in vivo, thereby increasing the concentration of active glucocorticoids (PubMed:23415904). It has broad substrate specificity, besides glucocorticoids, it accepts other steroid and sterol substrates (PubMed:23415904). Interconverts 7-oxo- and 7-hydroxy-neurosteroids such as 7-oxopregnenolone and 7beta-hydroxypregnenolone, 7-oxodehydroepiandrosterone (3beta-hydroxy-5-androstene-7,17-dione) and 7beta-hydroxydehydroepiandrosterone (3beta,7beta-dihydroxyandrost-5-en-17-one), among others (By similarity). Catalyzes the stereo-specific conversion of the major dietary oxysterol, 7-ketocholesterol (7-oxocholesterol), into the more polar 7-beta-hydroxycholesterol metabolite (PubMed:23415904). 7-oxocholesterol is one of the most important oxysterols, it participates in several events such as induction of apoptosis, accumulation in atherosclerotic lesions, lipid peroxidation, and induction of foam cell formation (By similarity). Mediates the 7-oxo reduction of 7-oxolithocholate mainly to chenodeoxycholate, and to a lesser extent to ursodeoxycholate, both in its free form and when conjugated to glycine or taurine, providing a link between glucocorticoid activation and bile acid metabolism (By similarity). Catalyzes the synthesis of 7-beta-25-dihydroxycholesterol from 7-oxo-25-hydroxycholesterol in vitro, which acts as a ligand for the G-protein-coupled receptor (GPCR) Epstein-Barr virus-induced gene 2 (EBI2) and may thereby regulate immune cell migration (PubMed:30902677).
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Uniprot ID
P50172
Ensembl ID
ENSG00000117594
Subcellular Location
Endoplasmic reticulum membrane
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: CL000384 , 3T3-L1
Compound ID Compound Name Compound Formula
CP0105606
3-[1-(4-chlorophenyl)cyclopropyl]-8-cyclopropyl-[1,2,4]triazolo[4,3-a]pyridine
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C18H16ClN3
 1
1
IC50 = 293 nM
   TI
   LI
   LO
   TS
CP0323516
1-[(2-chlorophenyl)methoxy]-7-fluoro-3-oxo-2H-isoquinoline-4-carbonitrile
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C17H10ClFN2O2
 1
1
IC50 = 2162 nM
   TI
   LI
   LO
   TS
CP0169237
1-[(2-chlorophenyl)methylsulfanyl]-7-fluoro-3-oxo-2H-isoquinoline-4-carbonitrile
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C17H10ClFN2OS
 1
1
IC50 = 2254 nM
   TI
   LI
   LO
   TS
CP0132715
2-[(2-chlorophenyl)methylsulfanyl]-6-oxo-4-phenyl-1H-pyrimidine-5-carbonitrile
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C18H12ClN3OS
 1
1
IC50 = 2854 nM
   TI
   LI
   LO
   TS
CP0335646
1-[(2-chlorophenyl)methylsulfanyl]-3-oxo-5,6,7,8-tetrahydro-2H-isoquinoline-4-carbonitrile
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C17H15ClN2OS
 1
1
IC50 = 3508 nM
   TI
   LI
   LO
   TS
CP0335642
8-[(2-cyanopyridin-3-yl)methylsulfanyl]-6-oxo-1,3,4,7-tetrahydropyrano[3,4-c]pyridine-5-carbonitrile
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C16H12N4O2S
 1
1
IC50 = 3966 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0265849
3-(3-chloro-4-(5-(1-(4-chlorophenyl)cyclobutyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)pyridine
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C24H20Cl2N4
 1
1 IC50 = 1.3 nM
CP0194646
CHEMBL2152223
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C23H31ClN2O4S
 1
1 IC50 = 1.3 nM
CP0112130
CHEMBL2036234
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C23H29Cl3N4O4S
 1
1 IC50 = 2 nM
CP0050383
4-methyl-3-(4-pentylbicyclo[2.2.2]octan-1-yl)-5-(2-(trifluoromethyl)phenyl)-4H-1,2,4-triazole
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C23H30F3N3
 1
1 IC50 = 3 nM
CP0221520
3-(4-pentylbicyclo[2.2.2]octan-1-yl)-5,6,7,8,9,10-hexahydro-[1,2,4]triazolo[4,3-a]azocine
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C21H35N3
 1
1 IC50 = 3 nM
CP0129718
3-Biphenyl-4-yl-5-[1-(4-chloro-phenyl)-cyclobutyl]-4-methyl-4H-[1,2,4]triazole
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C25H22ClN3
 1
1 IC50 = 4 nM
CP0335646
1-[(2-chlorophenyl)methylsulfanyl]-3-oxo-5,6,7,8-tetrahydro-2H-isoquinoline-4-carbonitrile
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C17H15ClN2OS
 1
1 IC50 = 5 nM
CP0169237
1-[(2-chlorophenyl)methylsulfanyl]-7-fluoro-3-oxo-2H-isoquinoline-4-carbonitrile
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C17H10ClFN2OS
 1
1 IC50 = 7 nM
CP0052039
18beta-glycyrrhetic acid
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C30H46O4
 1
1 IC50 = 10.58 nM
CP0138700
1-[3-({(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl}sulfonyl)phenyl]pyrrolidin-3-ol
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C22H25F4N3O3S
 1
1 IC50 = 11 nM
CP0253466
CHEMBL2152237
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C25H31N3O4S
 1
1 IC50 = 11 nM
CP0218773
(3R)-1-[3-({(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl}sulfonyl)phenyl]pyrrolidin-3-ol
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C22H25F4N3O3S
 1
1 IC50 = 13 nM
CP0096258
3-(1-(4-chlorophenyl)cyclobutyl)-5,6,7,8,9,10-hexahydro-[1,2,4]triazolo[4,3-a]azocine
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C18H22ClN3
 2
1 IC50 = 13.5 nM
2 IC50 = 14 nM
CP0346549
1-[3-({(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl}sulfonyl)phenyl]pyrrolidine-3-carboxamide
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C23H26F4N4O3S
 1
1 IC50 = 14 nM
CP0323516
1-[(2-chlorophenyl)methoxy]-7-fluoro-3-oxo-2H-isoquinoline-4-carbonitrile
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C17H10ClFN2O2
 1
1 IC50 = 21 nM
CP0138702
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-{[3-(4-methylpiperazin-1-yl)phenyl]sulfonyl}piperazine
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C23H28F4N4O2S
 1
1 IC50 = 28 nM
CP0346548
1-(3-((R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)pyrrolidine-2-carboxylic acid
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C23H25F4N3O4S
 1
1 IC50 = 32 nM
CP0102795
3-Adamantan-1-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
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C17H25N3
 3
1 IC50 = 35 nM
2 IC50 = 97 nM
3 IC50 = 98 nM
CP0302962
(3S)-1-[3-({(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl}sulfonyl)phenyl]pyrrolidin-3-ol
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C22H25F4N3O3S
 1
1 IC50 = 41 nM
CP0040668
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-{[3-(1H-1,2,4-triazol-1-yl)phenyl]sulfonyl}piperazine
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C20H19F4N5O2S
 1
1 IC50 = 42 nM
CP0346551
(2R)-1-{[3-(4-ethylpiperazin-1-yl)phenyl]sulfonyl}-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
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C24H30F4N4O2S
 1
1 IC50 = 45 nM
CP0172956
3-(1-(4-chlorophenyl)cyclobutyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
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C19H18ClN3
 1
1 IC50 = 52 nM
CP0256078
methyl 1-[3-[(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonylphenyl]pyrrolidine-3-carboxylate
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C24H27F4N3O4S
 1
1 IC50 = 55 nM
CP0236339
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[(3-pyrrolidin-1-ylphenyl)sulfonyl]piperazine
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C22H25F4N3O2S
 1
1 IC50 = 56 nM
CP0256079
4-[3-({(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl}sulfonyl)phenyl]morpholine
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C22H25F4N3O3S
 1
1 IC50 = 56 nM
CP0132715
2-[(2-chlorophenyl)methylsulfanyl]-6-oxo-4-phenyl-1H-pyrimidine-5-carbonitrile
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C18H12ClN3OS
 1
1 IC50 = 58 nM
CP0333759
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[(3-piperidin-1-ylphenyl)sulfonyl]piperazine
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C23H27F4N3O2S
 1
1 IC50 = 67 nM
CP0158847
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-{[3-(1H-pyrazol-1-yl)phenyl]sulfonyl}piperazine
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C21H20F4N4O2S
 1
1 IC50 = 73 nM
CP0166536
1-[3-({(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl}sulfonyl)phenyl]pyrrolidine-3-carboxylic acid
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C23H25F4N3O4S
 1
1 IC50 = 90 nM
CP0213664
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-{[3-(1H-pyrazol-1-yl)phenyl]sulfonyl}piperazine
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C21H20F4N4O2S
 1
1 IC50 = 100 nM
CP0335642
8-[(2-cyanopyridin-3-yl)methylsulfanyl]-6-oxo-1,3,4,7-tetrahydropyrano[3,4-c]pyridine-5-carbonitrile
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C16H12N4O2S
 1
1 IC50 = 105 nM
CP0062733
3beta-O-Succinyl-18-beta-glycyrrhetinic acid
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C34H50O7
 1
1 IC50 = 108 nM
CP0247593
3-Adamantan-1-yl-4-methyl-5-phenyl-4H-[1,2,4]triazole
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C19H23N3
 1
1 IC50 = 109 nM
CP0346546
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-{[3-(4H-1,2,4-triazol-4-yl)phenyl]sulfonyl}piperazine
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C20H19F4N5O2S
 1
1 IC50 = 120 nM
CP0043733
arylsulfonylpiperazine, 2
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C16H16F3N3O2S
 1
1 IC50 = 122 nM
CP0138630
2-[3-({(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl}sulfonyl)phenoxy]-2-methylpropanoic acid
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C22H24F4N2O5S
 1
1 IC50 = 130 nM
CP0138701
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[(3-piperazin-1-ylphenyl)sulfonyl]piperazine
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C22H26F4N4O2S
 1
1 IC50 = 190 nM
CP0166537
methyl 4-[3-[(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonylphenyl]piperazine-1-carboxylate
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C24H28F4N4O4S
 1
1 IC50 = 220 nM
CP0236340
N-ethyl-4-[3-[(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonylphenyl]piperazine-1-carboxamide
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C25H31F4N5O3S
 1
1 IC50 = 220 nM
CP0166538
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-1-{[3-(4-isopropylpiperazin-1-yl)phenyl]sulfonyl}-2-methylpiperazine
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C25H32F4N4O2S
 1
1 IC50 = 250 nM
CP0181142
2-(3-Benzoyl-4-hydroxy-1,1-dioxo-1H-1lambda*6*-benzo[e][1,2]thiazin-2-yl)-1-phenyl-ethanone
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C23H17NO5S
 1
1 IC50 = 7800 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00619 11-beta-hydroxysteroid dehydrogenase 1 Canis lupus familiaris, Dog, Canis familiaris
PT01107 11-beta-hydroxysteroid dehydrogenase 1 Homo sapiens, Human
PT03061 11-beta-hydroxysteroid dehydrogenase 1 Rattus norvegicus, Rat