General Information of Drug-Metabolizing Enzyme (DME) (ID: DEZDRQO)

DME Name Corticosteroid 11-beta-dehydrogenase 1 (HSD11B1)
Synonyms Corticosteroid 11-beta-dehydrogenase isozyme 1; Short chain dehydrogenase/reductase family 26C member 1; 11-beta-hydroxysteroid dehydrogenase 1; 11-DH; 11-beta-HSD1; HSD11; HSD11B1; HSD11L; SDR26C1
Gene Name HSD11B1
UniProt ID
DHI1_HUMAN
INTEDE ID
DME0199
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Gene ID
3290
EC Number EC: 1.1.1.146
Oxidoreductase
CH-OH donor oxidoreductase
NAD/NADP oxidoreductase
EC: 1.1.1.146
Lineage Species: Homo sapiens
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Sequence
MAFMKKYLLPILGLFMAYYYYSANEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAH
VVVTARSKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNH
ITNTSLNLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMV
AAYSASKFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEE
CALEIIKGGALRQEEVYYDSSLWTTLLIRNPCRKILEFLYSTSYNMDRFINK
Function This enzyme catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone and the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol.
KEGG Pathway
Chemical carcinogenesis (hsa05204 )
Metabolic pathways (hsa01100 )
Metabolism of xenobiotics by cytochrome P450 (hsa00980 )
Steroid hormone biosynthesis (hsa00140 )
Reactome Pathway
Glucocorticoid biosynthesis (R-HSA-194002 )

Molecular Interaction Atlas (MIA) of This DME

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DME
2 Approved Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cortisone Acetate DMG8K57 Acne vulgaris ED80 Approved [34]
Nabumetone DMAT2XH Osteoarthritis FA00-FA05 Approved [35]
1 Investigative Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dehydrocorticosterone DM48KMB N. A. N. A. Investigative [34]
Experimental Enzyme Kinetic Data of Drugs
Drug Name Indication Highest Status Kinetic Data REF
Cortisone Acetate Acne vulgaris [ED80] Approved Km = 0.00052 microM [34]

Molecular Expression Atlas (MEA) of This DME

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DME
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2B33.1 Bone marrow 5.56E-02 -5.91E-02 -2.68E-01
Alopecia ED70 Skin from scalp 4.38E-03 2.11E-01 2.68E-01
Alzheimer's disease 8A20 Entorhinal cortex 1.64E-01 1.14E-01 1.66E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 6.90E-01 -2.96E-01 -5.03E-01
Aortic stenosis BB70 Calcified aortic valve 7.79E-01 9.47E-02 5.75E-02
Apnea 7A40 Hyperplastic tonsil 5.85E-01 -8.19E-02 -1.55E-01
Arthropathy FA00-FA5Z Peripheral blood 6.51E-03 1.03E-01 8.54E-01
Asthma CA23 Nasal and bronchial airway 1.60E-04 1.07E-01 2.03E-01
Atopic dermatitis EA80 Skin 2.65E-08 -2.52E+00 -2.90E+00
Autism 6A02 Whole blood 9.92E-01 -5.65E-02 -3.31E-01
Autoimmune uveitis 9A96 Peripheral monocyte 4.97E-01 -1.13E-01 -8.95E-01
Autosomal dominant monocytopenia 4B04 Whole blood 4.16E-01 2.48E-03 2.38E-02
Bacterial infection of gingival 1C1H Gingival tissue 8.16E-17 1.10E+00 1.76E+00
Batten disease 5C56.1 Whole blood 9.57E-01 3.38E-02 1.43E-01
Behcet's disease 4A62 Peripheral blood 3.74E-01 8.89E-02 3.51E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 6.74E-01 -8.58E-02 -1.80E-01
Bladder cancer 2C94 Bladder tissue 1.60E-01 -8.07E-01 -7.57E-01
Breast cancer 2C60-2C6Z Breast tissue 1.22E-47 -1.80E+00 -1.25E+00
Cardioembolic stroke 8B11.20 Whole blood 1.06E-01 -1.25E-01 -2.95E-01
Cervical cancer 2C77 Cervical tissue 2.47E-04 4.00E-01 1.10E+00
Childhood onset rheumatic disease FA20.Z Peripheral blood 8.42E-01 -5.89E-04 -3.07E-03
Chronic hepatitis C 1E51.1 Whole blood 9.53E-01 -2.50E-02 -1.18E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 6.08E-01 2.78E-02 5.03E-02
Chronic obstructive pulmonary disease CA22 Small airway epithelium 4.19E-03 1.58E-01 5.83E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 2.05E-01 1.07E-01 9.04E-01
Colon cancer 2B90 Colon tissue 3.31E-53 6.87E-01 1.44E+00
Coronary artery disease BA80-BA8Z Peripheral blood 3.07E-01 -5.60E-02 -2.26E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 7.92E-01 -7.17E-03 -3.57E-02
Endometriosis GA10 Endometrium tissue 5.48E-05 6.21E-01 6.05E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 3.53E-01 1.12E-01 5.57E-01
Familial hypercholesterolemia 5C80.00 Whole blood 1.35E-01 -1.64E-01 -7.86E-01
Gastric cancer 2B72 Gastric tissue 2.36E-01 1.20E+00 1.14E+00
Glioblastopma 2A00.00 Nervous tissue 1.20E-78 -1.42E+00 -1.47E+00
Glioma 2A00.0Y-2A00.0Z Brain stem tissue 6.53E-01 -3.44E-01 -7.31E-01
Glioma 2A00.0Y-2A00.0Z White matter tissue 1.02E-01 9.67E-01 1.19E+00
Head and neck cancer 2D42 Head and neck tissue 1.89E-06 6.38E-01 7.03E-01
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 1.28E-01 -3.97E-01 -7.44E-01
Huntington's disease 8A01.10 Whole blood 7.72E-01 -2.99E-04 -2.33E-03
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 3.22E-02 -8.49E-01 -1.20E+00
Immunodeficiency 4A00-4A20 Peripheral blood 3.55E-01 1.54E-01 6.35E-01
Influenza 1E30 Whole blood 8.47E-01 -4.76E-01 -5.91E-01
Interstitial cystitis GC00.3 Bladder tissue 1.03E-02 1.91E+00 1.73E+00
Intracranial aneurysm 8B01.0 Intracranial artery 3.52E-01 1.04E+00 1.71E+00
Irritable bowel syndrome DD91.0 Rectal colon tissue 7.64E-01 2.60E-02 4.28E-02
Ischemic stroke 8B11 Peripheral blood 1.12E-01 1.26E-01 4.38E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 9.09E-01 -2.49E-02 -8.11E-02
Lateral sclerosis 8B60.4 Skin 2.46E-01 -2.06E-01 -5.64E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 2.10E-01 -2.06E-01 -5.91E-01
Liver cancer 2C12.0 Liver tissue 5.81E-30 -1.73E+00 -2.51E+00
Liver failure DB99.7-DB99.8 Liver tissue 7.26E-07 -2.92E+00 -7.62E+00
Lung cancer 2C25 Lung tissue 1.53E-68 -1.15E+00 -1.81E+00
Lupus erythematosus 4A40 Whole blood 4.48E-02 -8.91E-02 -2.44E-01
Major depressive disorder 6A70-6A7Z Hippocampus 3.36E-01 1.12E-01 2.38E-01
Major depressive disorder 6A70-6A7Z Whole blood 2.71E-01 2.69E-02 9.87E-02
Melanoma 2C30 Skin 1.28E-03 -3.49E+00 -1.39E+00
Multiple myeloma 2A83.1 Peripheral blood 5.27E-01 4.52E-02 2.93E-01
Multiple myeloma 2A83.1 Bone marrow 2.79E-05 2.30E-01 1.83E+00
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 4.13E-01 1.24E-01 4.85E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 1.38E-01 2.27E-02 1.12E-01
Myelofibrosis 2A20.2 Whole blood 8.39E-01 -4.86E-02 -3.15E-01
Myocardial infarction BA41-BA50 Peripheral blood 2.35E-07 -6.79E-01 -7.07E-01
Myopathy 8C70.6 Muscle tissue 4.35E-01 -1.85E-01 -5.55E-01
Neonatal sepsis KA60 Whole blood 9.86E-03 7.04E-02 2.85E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 1.92E-07 -1.30E+00 -3.48E+00
Non-alcoholic fatty liver disease DB92 Liver tissue 8.61E-01 1.05E-01 2.75E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 8.99E-01 -1.11E-01 -1.19E-01
Olive pollen allergy CA08.00 Peripheral blood 7.32E-01 -1.75E-01 -3.04E-01
Oral cancer 2B6E Oral tissue 3.60E-01 7.34E-02 1.28E-01
Osteoarthritis FA00-FA0Z Synovial tissue 5.68E-01 1.38E-02 2.46E-02
Osteoporosis FB83.1 Bone marrow 5.82E-01 -8.54E-02 -1.60E-01
Ovarian cancer 2C73 Ovarian tissue 2.14E-03 -2.18E+00 -1.51E+00
Pancreatic cancer 2C10 Pancreas 2.85E-01 5.09E-01 5.64E-01
Parkinson's disease 8A00.0 Substantia nigra tissue 4.81E-01 4.09E-01 4.15E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 9.05E-02 3.89E-02 1.91E-01
Pituitary cancer 2D12 Pituitary tissue 8.76E-11 -2.21E+00 -4.28E+00
Pituitary gonadotrope tumour 2D12 Pituitary tissue 2.82E-07 -2.91E+00 -5.44E+00
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 9.18E-01 -4.92E-02 -2.49E-01
Polycythemia vera 2A20.4 Whole blood 2.61E-05 7.61E-02 5.00E-01
Pompe disease 5C51.3 Biceps muscle 2.27E-01 -6.28E-01 -1.15E+00
Preterm birth KA21.4Z Myometrium 3.21E-01 -2.72E-01 -2.00E-01
Prostate cancer 2C82 Prostate 6.32E-02 2.20E-01 1.37E-01
Psoriasis EA90 Skin 1.58E-50 -2.36E+00 -3.65E+00
Rectal cancer 2B92 Rectal colon tissue 2.80E-01 1.03E-01 1.63E-01
Renal cancer 2C90-2C91 Kidney 8.61E-02 -1.36E+00 -1.23E+00
Retinoblastoma 2D02.2 Uvea 2.66E-01 -2.65E-01 -4.33E-01
Rheumatoid arthritis FA20 Synovial tissue 1.08E-03 5.67E-01 1.18E+00
Rhinovirus infection CA42.1 Nasal epithelium tissue 1.57E-02 1.80E-02 9.04E-02
Schizophrenia 6A20 Prefrontal cortex 4.13E-02 -3.92E-01 -4.32E-01
Schizophrenia 6A20 Superior temporal cortex 4.70E-04 -4.62E-01 -1.06E+00
Scleroderma 4A42.Z Whole blood 3.34E-04 -3.18E-01 -2.24E+00
Seizure 8A60-8A6Z Whole blood 9.31E-01 -2.31E-02 -1.24E-01
Sensitive skin EK0Z Skin 2.77E-01 -2.87E-01 -9.42E-01
Sepsis with septic shock 1G41 Whole blood 1.03E-11 1.43E-01 6.50E-01
Shwachman-Diamond syndrome 3A70.0 Bone marrow 1.08E-01 2.13E-01 7.71E-01
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 2.96E-01 2.13E-01 8.97E-01
Simpson golabi behmel syndrome LD2C Adipose tissue 6.25E-01 3.02E-01 6.55E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 4.49E-03 4.47E-01 2.46E+00
Skin cancer 2C30-2C3Z Skin 1.14E-133 -3.23E+00 -3.48E+00
Thrombocythemia 3B63 Whole blood 1.28E-01 1.37E-01 8.91E-01
Thrombocytopenia 3B64 Whole blood 4.80E-01 3.46E-01 5.77E-01
Thyroid cancer 2D10 Thyroid 9.15E-01 -2.13E-01 -2.94E-01
Tibial muscular dystrophy 8C75 Muscle tissue 1.14E-02 -7.86E-01 -1.01E+00
Tuberous sclerosis complex LD2D.2 Perituberal tissue 1.60E-03 -1.66E+00 -4.10E+00
Type 2 diabetes 5A11 Liver tissue 2.03E-01 -1.24E-02 -8.14E-02
Ureter cancer 2C92 Urothelium 6.48E-01 1.95E-02 1.07E-01
Uterine cancer 2C78 Endometrium tissue 9.46E-10 4.90E-01 6.91E-01
Vitiligo ED63.0 Skin 6.56E-01 -1.59E-01 -2.55E-01
------------------------------------------------------------------------------------
⏷ Show the Full List of DME Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DME

DME DTT Name Corticosteroid 11-beta-dehydrogenase 1 (HSD11B1) DTT Info
DME DTT Type Clinical trial
13 Clinical Trial Drug(s) Targeting This DTT
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) Targeting This DTT
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) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
HPP-851 DM69UZG Metabolic disorder 5C50-5D2Z Preclinical [13]
66 Investigative Drug(s) Targeting This DTT
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)

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.
34 Comparative enzymology of 11beta-hydroxysteroid dehydrogenase type 1 from six species. J Mol Endocrinol. 2005 Aug;35(1):89-101.
35 Reductive metabolism of nabumetone by human liver microsomal and cytosolic fractions: exploratory prediction using inhibitors and substrates as marker probes. Eur J Drug Metab Pharmacokinet. 2015 Jun;40(2):127-35.