General Information of DTT (ID: TTN7BL9)

DTT Name Corticosteroid 11-beta-dehydrogenase 1 (HSD11B1) DTT Info
Gene Name HSD11B1

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Investigative Drug(s)
13 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
BVT.2733 DM6RUKX Lupus 4A40 Phase 3 [1]
GLYCYRRHIZIN DM8M2N3 Influenza virus infection 1E30-1E32 Phase 3 [2]
INCB13739 DMLQ3PO Type-2 diabetes 5A11 Phase 2a [3]
AZD-4017 DML9M5S Ocular hypertension 9C61.01 Phase 2 [4]
BMS-770767 DMTVGY7 Hypercholesterolaemia 5C80.0 Phase 2 [4]
JTT-654 DM50M2R Type-2 diabetes 5A11 Phase 2 [4]
RG-4929 DMT4QRD Metabolic disorder 5C50-5D2Z Phase 2 [4]
UE-2343 DMIERPK Alzheimer disease 8A20 Phase 2 [5]
URSOLIC ACID DM4SOAW Metabolic syndrome x 5C50-5D2Z Phase 2 [6]
Xanamem DM580GT Alzheimer disease 8A20 Phase 1/2 [7]
AZD8329 DMTD57A Diabetic complication 5A2Y Phase 1 [8]
BI-135585 DMLJOAF Type-2 diabetes 5A11 Phase 1 [4]
BMS-816336 DM2WMJ7 Lipid metabolism disorder 5C52.Z Phase 1 [9]
------------------------------------------------------------------------------------
⏷ Show the Full List of 13 Clinical Trial Drug(s)
4 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
LY-2523199 DMGE9OA Type-2 diabetes 5A11 Discontinued in Phase 2 [10]
AMG-221 DMFCKJ1 Metabolic disorder 5C50-5D2Z Discontinued in Phase 1 [11]
PF-915275 DMB7EIN Non-insulin dependent diabetes 5A11 Discontinued in Phase 1 [12]
BVT-3498 DMOZQHX Metabolic disorder 5C50-5D2Z Terminated [14]
------------------------------------------------------------------------------------
1 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
HPP-851 DM69UZG Metabolic disorder 5C50-5D2Z Preclinical [13]
------------------------------------------------------------------------------------
66 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE DMTPQ84 Discovery agent N.A. Investigative [15]
(4-methoxyphenyl)(4-phenylazepan-1-yl)methanone DMZD0KG Discovery agent N.A. Investigative [16]
1,1-diphenyl-3-(phenylsulfonyl)propan-2-one DM7SQ4H Discovery agent N.A. Investigative [17]
1-(1-phenyl-1H-tetrazol-5-ylthio)propan-2-one DMSUC85 Discovery agent N.A. Investigative [18]
1-(2-adamantyl)-3-benzylpyrrolidin-2-one DMRHY2M Discovery agent N.A. Investigative [19]
1-(3,4-dichlorophenyl)-2-(phenylsulfonyl)ethanone DM4YWEL Discovery agent N.A. Investigative [17]
1-(3,5-dimethylphenyl)-2-(phenylsulfonyl)ethanone DMYJ4EG Discovery agent N.A. Investigative [17]
1-(3-chloropyridin-2-yl)-4-tosylpiperazine DM6LWR2 Discovery agent N.A. Investigative [20]
1-(3-methoxyphenyl)-2-(phenylsulfonyl)ethanone DMR0ICB Discovery agent N.A. Investigative [17]
1-(3-methylpyridin-2-yl)-4-tosylpiperazine DMYH9M0 Discovery agent N.A. Investigative [20]
1-(3-nitropyridin-2-yl)-4-tosylpiperazine DM3FP6J Discovery agent N.A. Investigative [20]
1-(4-chlorophenyl)-2-(phenylsulfonyl)ethanone DMQHTR4 Discovery agent N.A. Investigative [17]
1-(4-chlorophenylsulfonyl)-4-phenylazepan-4-ol DMEJXWG Discovery agent N.A. Investigative [16]
1-(4-ethylphenylsulfonyl)-4-phenylazepan-4-ol DMXUIS2 Discovery agent N.A. Investigative [16]
1-(4-ethylpiperazin-1-yl)-2-phenylethanone DMRK0Z1 Discovery agent N.A. Investigative [21]
1-(4-fluorophenyl)-2-(phenylsulfonyl)ethanone DMZLNAP Discovery agent N.A. Investigative [17]
1-(4-fluorophenyl)-3-(phenylsulfonyl)propan-1-one DMKATOJ Discovery agent N.A. Investigative [17]
1-(4-methoxyphenyl)-2-(phenylsulfonyl)ethanone DMRC7V8 Discovery agent N.A. Investigative [17]
1-(4-methoxyphenylsulfonyl)-4-phenylazepan-4-ol DMG7PKA Discovery agent N.A. Investigative [16]
1-(4-nitrophenyl)-2-(phenylsulfonyl)ethanone DM1M67Q Discovery agent N.A. Investigative [17]
1-(4-tert-butylphenylsulfonyl)-4-methoxyazepane DMM7IJZ Discovery agent N.A. Investigative [16]
1-(4-tert-butylphenylsulfonyl)azepan-4-ol DMQECWT Discovery agent N.A. Investigative [16]
1-(phenylsulfonyl)butan-2-one DMRGD8W Discovery agent N.A. Investigative [17]
1-phenyl-2-(1-phenyl-1H-tetrazol-5-yloxy)ethanone DMZM9AI Discovery agent N.A. Investigative [18]
1-phenyl-3-(phenylsulfonyl)propan-1-one DM8ZBHF Discovery agent N.A. Investigative [17]
1-phenyl-4-(1-phenyl-1H-tetrazol-5-yl)butan-2-one DMKV17L Discovery agent N.A. Investigative [18]
11-keto-beta-boswellicacid DMM6CJI Discovery agent N.A. Investigative [6]
11-keto-ursolic acid DM1WPE3 Discovery agent N.A. Investigative [6]
2'-Monophosphoadenosine 5'-Diphosphoribose DME9S8M Discovery agent N.A. Investigative [22]
2-(2-chlorophenylamino)-5-methylthiazol-4(5H)-one DMJ38LE Discovery agent N.A. Investigative [23]
2-(4-tosylpiperazin-1-yl)nicotinonitrile DMED9FL Discovery agent N.A. Investigative [20]
2-(adamantan-1-ylamino)-5,5-diethyl-oxazol-4-one DMB3YXG Discovery agent N.A. Investigative [24]
2-(benzylamino)-5,5-diethyloxazol-4(5H)-one DMW27AC Discovery agent N.A. Investigative [24]
2-(cyclooctylamino)-5,5-diethyloxazol-4(5H)-one DMAPW5K Discovery agent N.A. Investigative [24]
2-(N-Morpholino)-Ethanesulfonic Acid DMZVHSB Discovery agent N.A. Investigative [22]
2-(o-toluidino)-5-ethylthiazol-4(5H)-one DM3RCA9 Discovery agent N.A. Investigative [25]
2-(o-toluidino)-5-isopropylthiazol-4(5H)-one DMYTJX4 Discovery agent N.A. Investigative [23]
2-(phenylsulfonyl)-1-(thiophen-3-yl)ethanone DMCF75U Discovery agent N.A. Investigative [17]
2-(phenylsulfonyl)-1-p-tolylethanone DM93XJT Discovery agent N.A. Investigative [17]
3-acetyl-11-keto-beta-boswellic acid DMGO2D7 Discovery agent N.A. Investigative [6]
3-acetyl-11-keto-ursolic acid DMHRZ2V Discovery agent N.A. Investigative [6]
3-benzyl-1-cyclohexylpyrrolidin-2-one DMNG0TY Discovery agent N.A. Investigative [19]
3-epicorosolic acid methyl ester DMQ8VIU Discovery agent N.A. Investigative [6]
5,5-diethyl-2-(phenethylamino)oxazol-4(5H)-one DMWL1UY Discovery agent N.A. Investigative [24]
5-isopropyl-2-(phenylamino)thiazol-4(5H)-one DM2TNWO Discovery agent N.A. Investigative [23]
A-849531 DMJBPR3 Metabolic disorder 5C50-5D2Z Investigative [26]
Abietic acid DMW1Y2G Discovery agent N.A. Investigative [27]
Adamantan-1-yl-(4-ethyl-piperazin-1-yl)-methanone DM4S279 Discovery agent N.A. Investigative [21]
Adamantan-1-yl-piperazin-1-yl-methanone DM5K0EI Discovery agent N.A. Investigative [21]
Adamantan-1-yl-piperidin-1-yl-methanone DMTUL9J Discovery agent N.A. Investigative [21]
Adamantan-1-yl-pyrrolidin-1-yl-methanone DMAEN9Y Discovery agent N.A. Investigative [21]
Adamantan-2-yl-piperidin-1-yl-methanone DMBRAV5 Discovery agent N.A. Investigative [21]
Carbenoxolone DMO648T Discovery agent N.A. Investigative [28]
CNX-010 DMDK5BL Non-insulin dependent diabetes 5A11 Investigative [26]
Corosolic acid DM563PZ Discovery agent N.A. Investigative [6]
EQ-1280 DM2KMNU Diabetic complication 5A2Y Investigative [26]
FIG 1 DM29TVC Discovery agent N.A. Investigative [29]
Flavanone DMNWIYM Discovery agent N.A. Investigative [27]
MERCK-544 DMD25I6 Discovery agent N.A. Investigative [30]
N-benzyl-N-(phenylsulfonyl)benzamide DMT2GSI Discovery agent N.A. Investigative [17]
PF-877423 DM49MYE Discovery agent N.A. Investigative [31]
Piperidine-1-carboxylic acid adamantan-2-yl ester DMF375O Discovery agent N.A. Investigative [32]
Piperidine-1-carboxylic acid adamantan-2-ylamide DMHZFK1 Discovery agent N.A. Investigative [32]
SKI-2852 DMJL6HX Metabolic syndrome x 5C50-5D2Z Investigative [26]
Tormentic acid methyl ester DMDG0HK Discovery agent N.A. Investigative [6]
[(125)I] RB129 DMX0G7E Discovery agent N.A. Investigative [33]
------------------------------------------------------------------------------------
⏷ Show the Full List of 66 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Selective inhibition of 11 beta-hydroxysteroid dehydrogenase type 1 improves hepatic insulin sensitivity in hyperglycemic mice strains. Endocrinology. 2003 Nov;144(11):4755-62.
2 Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes. Bioorg Med Chem. 2009 Aug 1;17(15):5722-32.
3 Incyte's Selective Oral Inhibitor Of 11beta-HSD1 Demonstrates Improvements In Insulin Sensitivity And Lowers Cholesterol Levels In Type 2 Diabetics. Incyte. 2008.
4 New Therapeutic Strategies for Type 2 Diabetes: Small Molecule Approaches. 2012. Chapter 5. Page(131).
5 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
6 11beta-Hydroxysteroid dehydrogenase 1 inhibiting constituents from Eriobotrya japonica revealed by bioactivity-guided isolation and computational a... Bioorg Med Chem. 2010 Feb 15;18(4):1507-15.
7 Selection and early clinical evaluation of the brain-penetrant 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor UE2343 (Xanamem?). Br J Pharmacol. 2017 Mar;174(5):396-408.
8 Clinical pipeline report, company report or official report of AstraZeneca (2011).
9 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027626)
10 Repurposing Diabetes Drugs for Brain Insulin Resistance in Alzheimer Disease. before print June 15, 2014.
11 Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-b... J Med Chem. 2010 Jun 10;53(11):4481-7.
12 N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7.
13 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027759)
14 Current and future drug targets in weight management. Pharm Res. 2011 Aug;28(8):1792-818.
15 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
16 The discovery of azepane sulfonamides as potent 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4563-5.
17 beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action. Bioorg Med Chem. 2007 Jul 1;15(13):4396-405.
18 Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3265-71.
19 Discovery of orally active butyrolactam 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5555-60.
20 Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). Bioorg Med Chem Lett. 2008 Jun 15;18(12):3513-6.
21 Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2007 May 15;17(10):2838-43.
22 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
23 The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6056-61.
24 Oxazolones as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4837-40.
25 2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure an... J Med Chem. 2008 May 22;51(10):2933-43.
26 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2763).
27 A rapid screening assay for inhibitors of 11beta-hydroxysteroid dehydrogenases (11beta-HSD): flavanone selectively inhibits 11beta-HSD1 reductase activity. Mol Cell Endocrinol. 2003 Dec 30;212(1-2):41-9.
28 Selective inhibition of 11beta-hydroxysteroid dehydrogenase 1 by 18alpha-glycyrrhetinic acid but not 18beta-glycyrrhetinic acid. J Steroid Biochem Mol Biol. 2009 Feb;113(3-5):248-52.
29 4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3405-11.
30 Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1551-4.
31 The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2010 May 1;20(9):2897-902.
32 Discovery and optimization of adamantyl carbamate inhibitors of 11-HSD1. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6725-9.
33 Rapid hepatic metabolism of 7-ketocholesterol by 11beta-hydroxysteroid dehydrogenase type 1: species-specific differences between the rat, human, a... J Biol Chem. 2004 Apr 30;279(18):18415-24.