Target Validation Information
TTD ID T65200
Target Name Corticosteroid 11-beta-dehydrogenase 1 (HSD11B1)
Type of Target
Clinical trial
Drug Potency against Target INCB13739 Drug Info IC50 = 3~70 nM
(4-methoxyphenyl)(4-phenylazepan-1-yl)methanone Drug Info IC50 = 9 nM [12]
1,1-diphenyl-3-(phenylsulfonyl)propan-2-one Drug Info IC50 = 2900 nM [3]
1-(1-phenyl-1H-tetrazol-5-ylthio)propan-2-one Drug Info IC50 = 14500 nM [16]
1-(2-adamantyl)-3-benzylpyrrolidin-2-one Drug Info IC50 = 64 nM [1]
1-(3,4-dichlorophenyl)-2-(phenylsulfonyl)ethanone Drug Info IC50 = 101 nM [3]
1-(3,5-dimethylphenyl)-2-(phenylsulfonyl)ethanone Drug Info IC50 = 1200 nM [3]
1-(3-chloropyridin-2-yl)-4-tosylpiperazine Drug Info IC50 = 146 nM [8]
1-(3-methoxyphenyl)-2-(phenylsulfonyl)ethanone Drug Info IC50 = 60 nM [3]
1-(3-methylpyridin-2-yl)-4-tosylpiperazine Drug Info IC50 = 240 nM [8]
1-(3-nitropyridin-2-yl)-4-tosylpiperazine Drug Info IC50 = 291 nM [8]
1-(4-chlorophenyl)-2-(phenylsulfonyl)ethanone Drug Info IC50 = 200 nM [3]
1-(4-chlorophenylsulfonyl)-4-phenylazepan-4-ol Drug Info IC50 = 2721 nM [12]
1-(4-ethylphenylsulfonyl)-4-phenylazepan-4-ol Drug Info IC50 = 1406 nM [12]
1-(4-ethylpiperazin-1-yl)-2-phenylethanone Drug Info IC50 = 7200 nM [2]
1-(4-fluorophenyl)-2-(phenylsulfonyl)ethanone Drug Info IC50 = 90 nM [3]
1-(4-fluorophenyl)-3-(phenylsulfonyl)propan-1-one Drug Info IC50 = 19600 nM [3]
1-(4-methoxyphenyl)-2-(phenylsulfonyl)ethanone Drug Info IC50 = 75 nM [3]
1-(4-methoxyphenylsulfonyl)-4-phenylazepan-4-ol Drug Info IC50 = 1981 nM [12]
1-(4-nitrophenyl)-2-(phenylsulfonyl)ethanone Drug Info IC50 = 1310 nM [3]
1-(4-tert-butylphenylsulfonyl)-4-methoxyazepane Drug Info IC50 = 165 nM [12]
1-(4-tert-butylphenylsulfonyl)azepan-4-ol Drug Info IC50 = 629 nM [12]
1-(phenylsulfonyl)butan-2-one Drug Info IC50 = 15000 nM [3]
1-phenyl-2-(1-phenyl-1H-tetrazol-5-yloxy)ethanone Drug Info IC50 = 971 nM [16]
1-phenyl-3-(phenylsulfonyl)propan-1-one Drug Info IC50 = 17400 nM [3]
1-phenyl-4-(1-phenyl-1H-tetrazol-5-yl)butan-2-one Drug Info IC50 = 820 nM [16]
11-keto-ursolic acid Drug Info IC50 = 2060 nM [13]
2-(2-chlorophenylamino)-5-methylthiazol-4(5H)-one Drug Info Ki = 350 nM [5]
2-(4-tosylpiperazin-1-yl)nicotinonitrile Drug Info IC50 = 628 nM [8]
2-(adamantan-1-ylamino)-5,5-diethyl-oxazol-4-one Drug Info Ki = 4 nM [4]
2-(benzylamino)-5,5-diethyloxazol-4(5H)-one Drug Info Ki = 1761 nM [4]
2-(cyclooctylamino)-5,5-diethyloxazol-4(5H)-one Drug Info Ki = 10 nM [4]
2-(o-toluidino)-5-ethylthiazol-4(5H)-one Drug Info Ki = 189 nM [6]
2-(o-toluidino)-5-isopropylthiazol-4(5H)-one Drug Info IC50 = 1.3 nM [5]
2-(phenylsulfonyl)-1-(thiophen-3-yl)ethanone Drug Info IC50 = 345 nM [3]
2-(phenylsulfonyl)-1-p-tolylethanone Drug Info IC50 = 102 nM [3]
3-acetyl-11-keto-ursolic acid Drug Info IC50 = 1350 nM [13]
3-benzyl-1-cyclohexylpyrrolidin-2-one Drug Info IC50 = 107 nM [1]
3-epicorosolic acid methyl ester Drug Info IC50 = 5200 nM [13]
5,5-diethyl-2-(phenethylamino)oxazol-4(5H)-one Drug Info Ki = 6451 nM [4]
5-isopropyl-2-(phenylamino)thiazol-4(5H)-one Drug Info IC50 = 310 nM [5]
Adamantan-1-yl-(4-ethyl-piperazin-1-yl)-methanone Drug Info IC50 = 300 nM [2]
Adamantan-1-yl-piperazin-1-yl-methanone Drug Info IC50 = 8200 nM [2]
Adamantan-1-yl-piperidin-1-yl-methanone Drug Info IC50 = 134 nM [2]
Adamantan-1-yl-pyrrolidin-1-yl-methanone Drug Info IC50 = 498 nM [2]
Adamantan-2-yl-piperidin-1-yl-methanone Drug Info IC50 = 200 nM [2]
AMG-221 Drug Info IC50 = 10.1 nM [17]
BVT.2733 Drug Info IC50 = 52 nM [14]
Corosolic acid Drug Info IC50 = 810 nM [13]
FIG 1 Drug Info IC50 = 109 nM [7]
GLYCYRRHIZIN Drug Info IC50 = 8 nM [10]
GLYCYRRHIZIN Drug Info IC50 = 15 nM [11]
MERCK-544 Drug Info IC50 = 97 nM [14]
N-benzyl-N-(phenylsulfonyl)benzamide Drug Info IC50 = 5700 nM [3]
PF-877423 Drug Info IC50 = 4.15 nM [15]
PF-915275 Drug Info Ki = 750 nM [9]
Piperidine-1-carboxylic acid adamantan-2-yl ester Drug Info IC50 = 53 nM [18]
Piperidine-1-carboxylic acid adamantan-2-ylamide Drug Info IC50 = 32 nM [18]
Tormentic acid methyl ester Drug Info IC50 = 9400 nM [13]
URSOLIC ACID Drug Info IC50 = 1900 nM [13]
Action against Disease Model BVT.2733 Drug Info BVT.2733 has an IC50 of 96 nM for mouse 11 beta-HSD1. [19]
References
REF 1 Discovery of orally active butyrolactam 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5555-60.
REF 2 Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2007 May 15;17(10):2838-43.
REF 3 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.
REF 4 Oxazolones as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4837-40.
REF 5 The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6056-61.
REF 6 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.
REF 7 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.
REF 8 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.
REF 9 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.
REF 10 4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabeti... Bioorg Med Chem Lett. 2009 Aug 1;19(15):4455-8.
REF 11 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.
REF 12 The discovery of azepane sulfonamides as potent 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4563-5.
REF 13 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.
REF 14 Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1551-4.
REF 15 The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2010 May 1;20(9):2897-902.
REF 16 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.
REF 17 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.
REF 18 Discovery and optimization of adamantyl carbamate inhibitors of 11-HSD1. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6725-9.
REF 19 Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res. 2008 Nov 15;14(22):7272-83.

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