General Information of Drug-Metabolizing Enzyme (DME) (ID: DE492CE)

DME Name Prostaglandin G/H synthase 2 (COX-2)
Synonyms Prostaglandin H2 synthase 2; Prostaglandin-endoperoxide synthase 2; Cyclooxygenase-2; PGH synthase 2; COX-2; COX2; PGHS-2; PHS II; PTGS2
Gene Name PTGS2
UniProt ID
PGH2_HUMAN
INTEDE ID
DME0114
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Gene ID
5743
EC Number EC: 1.14.99.1
Oxidoreductase
Oxygen paired donor oxidoreductase
Oxygen paired donor oxidoreductase
EC: 1.14.99.1
Lineage Species: Homo sapiens
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Sequence
MLARALLLCAVLALSHTANPCCSHPCQNRGVCMSVGFDQYKCDCTRTGFYGENCSTPEFL
TRIKLFLKPTPNTVHYILTHFKGFWNVVNNIPFLRNAIMSYVLTSRSHLIDSPPTYNADY
GYKSWEAFSNLSYYTRALPPVPDDCPTPLGVKGKKQLPDSNEIVEKLLLRRKFIPDPQGS
NMMFAFFAQHFTHQFFKTDHKRGPAFTNGLGHGVDLNHIYGETLARQRKLRLFKDGKMKY
QIIDGEMYPPTVKDTQAEMIYPPQVPEHLRFAVGQEVFGLVPGLMMYATIWLREHNRVCD
VLKQEHPEWGDEQLFQTSRLILIGETIKIVIEDYVQHLSGYHFKLKFDPELLFNKQFQYQ
NRIAAEFNTLYHWHPLLPDTFQIHDQKYNYQQFIYNNSILLEHGITQFVESFTRQIAGRV
AGGRNVPPAVQKVSQASIDQSRQMKYQSFNEYRKRFMLKPYESFEELTGEKEMSAELEAL
YGDIDAVELYPALLVEKPRPDAIFGETMVEVGAPFSLKGLMGNVICSPAYWKPSTFGGEV
GFQIINTASIQSLICNNVKGCPFTSFSVPDPELIKTVTINASSSRSGLDDINPTVLLKER
STEL
Function This enzyme converts arachidonate to prostaglandin H2 (PGH2).
KEGG Pathway
Alzheimer's disease (hsa05010 )
Arachidonic acid metabolism (hsa00590 )
C-type lectin receptor signaling pathway (hsa04625 )
Chemical carcinogenesis (hsa05204 )
Human cytomegalovirus infection (hsa05163 )
Human papillomavirus infection (hsa05165 )
IL-17 signaling pathway (hsa04657 )
Kaposi sarcoma-associated herpesvirus infection (hsa05167 )
Leishmaniasis (hsa05140 )
Metabolic pathways (hsa01100 )
MicroRNAs in cancer (hsa05206 )
NF-kappa B signaling pathway (hsa04064 )
Ovarian steroidogenesis (hsa04913 )
Oxytocin signaling pathway (hsa04921 )
Pathways in cancer (hsa05200 )
Regulation of lipolysis in adipocytes (hsa04923 )
Retrograde endocannabinoid signaling (hsa04723 )
Serotonergic synapse (hsa04726 )
Small cell lung cancer (hsa05222 )
TNF signaling pathway (hsa04668 )
VEGF signaling pathway (hsa04370 )
Reactome Pathway
Biosynthesis of DPAn-3 SPMs (R-HSA-9025094 )
Biosynthesis of EPA-derived SPMs (R-HSA-9018679 )
Biosynthesis of electrophilic Omega-3 PUFA oxo-derivatives (R-HSA-9027604 )
Interleukin-10 signaling (R-HSA-6783783 )
Interleukin-4 and Interleukin-13 signaling (R-HSA-6785807 )
Nicotinamide salvaging (R-HSA-197264 )
Synthesis of 15-eicosatetraenoic acid derivatives (R-HSA-2142770 )
Synthesis of Prostaglandins (PG) and Thromboxanes (TX) (R-HSA-2162123 )
Biosynthesis of DHA-derived SPMs (R-HSA-9018677 )

Molecular Interaction Atlas (MIA) of This DME

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DME
6 Approved Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dapsone DM4LT8A Pneumocystis pneumonia CA40.20 Approved [130]
Eicosapentaenoic acid/docosa-hexaenoic acid DMMUCG4 Hypertriglyceridemia 5C80.1 Approved [131]
Epanova DMHEAGL Hypertriglyceridemia 5C80.1 Approved [132]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [133]
Gamma-homolinolenic acid DMSXKYG Malnutrition 5B50-5B71 Approved [131]
Gamolenic acid DMQN30Z Allergy 4A80-4A85 Approved [131]
⏷ Show the Full List of 6 Approved Drug(s)
1 Clinical Trial Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
Omega-6-FA DMBWY8V Attention deficit hyperactivity disorder 6A05.Z Phase 3 [134]
5 Investigative Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
Alpha-linolenic acid DMY64HE Discovery agent N.A. Investigative [131]
Arachidonic acid DMUOQZD Discovery agent N.A. Investigative [135]
BML3-C01 DMER2WS Discovery agent N.A. Investigative [131]
Eicosadienoic acid DMVJK9W Discovery agent N.A. Investigative [131]
Icosapentum DMF1CM7 Discovery agent N.A. Investigative [131]
Experimental Enzyme Kinetic Data of Drugs
Drug Name Indication Highest Status Kinetic Data REF
Alpha-linolenic acid Discovery agent [N.A.] Investigative Km = 0.0031 microM [131]
Arachidonic acid Discovery agent [N.A.] Investigative Km = 0.0017 microM [131]
Eicosapentaenoic acid/docosa-hexaenoic acid Hypertriglyceridemia [5C80.1] Approved Km = 0.0011 microM [131]
Gamma-homolinolenic acid Malnutrition [5B50-5B71] Approved Km = 0.002 microM [131]
Gamolenic acid Allergy [4A80-4A85] Approved Km = 0.0048 microM [131]

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 1.38E-09 -1.44E+00 -9.15E-01
Alopecia ED70 Skin from scalp 5.15E-04 1.49E-01 4.78E-01
Alzheimer's disease 8A20 Entorhinal cortex 7.93E-04 -2.88E-01 -3.44E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 9.00E-01 -6.26E-02 -2.65E-01
Aortic stenosis BB70 Calcified aortic valve 3.40E-03 -8.53E-01 -1.54E+00
Apnea 7A40 Hyperplastic tonsil 2.60E-01 -2.39E-01 -3.66E-01
Arthropathy FA00-FA5Z Peripheral blood 8.20E-02 2.19E-01 3.53E-01
Asthma CA23 Nasal and bronchial airway 1.50E-04 8.64E-01 6.35E-01
Atopic dermatitis EA80 Skin 1.62E-01 -3.10E-01 -1.11E+00
Autism 6A02 Whole blood 6.28E-01 8.65E-02 7.86E-02
Autoimmune uveitis 9A96 Peripheral monocyte 6.38E-01 -5.21E-01 -3.95E-01
Autosomal dominant monocytopenia 4B04 Whole blood 1.82E-02 -6.87E-01 -1.53E+00
Bacterial infection of gingival 1C1H Gingival tissue 1.97E-06 7.14E-01 8.33E-01
Batten disease 5C56.1 Whole blood 6.55E-02 6.91E-01 1.03E+00
Behcet's disease 4A62 Peripheral blood 6.30E-01 1.24E-01 6.12E-02
Bipolar disorder 6A60-6A6Z Prefrontal cortex 4.14E-01 5.95E-02 6.69E-02
Bladder cancer 2C94 Bladder tissue 5.95E-02 6.63E-01 7.42E-01
Breast cancer 2C60-2C6Z Breast tissue 1.55E-33 -1.09E+00 -8.69E-01
Cardioembolic stroke 8B11.20 Whole blood 1.59E-04 5.88E-01 1.00E+00
Cervical cancer 2C77 Cervical tissue 6.82E-03 1.44E+00 9.40E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 8.16E-01 -1.16E+00 -4.27E-01
Chronic hepatitis C 1E51.1 Whole blood 2.29E-01 2.55E-01 8.68E-02
Chronic obstructive pulmonary disease CA22 Lung tissue 1.95E-01 1.73E-01 1.60E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 1.21E-01 1.41E-01 1.99E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 8.63E-02 -1.18E+00 -1.25E+00
Colon cancer 2B90 Colon tissue 1.64E-44 1.57E+00 1.70E+00
Coronary artery disease BA80-BA8Z Peripheral blood 3.19E-01 2.19E+00 9.57E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 2.92E-01 -5.17E-02 -2.33E-01
Endometriosis GA10 Endometrium tissue 1.40E-01 -9.05E-01 -5.03E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 1.75E-01 1.16E-01 8.46E-01
Familial hypercholesterolemia 5C80.00 Whole blood 2.53E-03 -1.03E+00 -1.57E+00
Gastric cancer 2B72 Gastric tissue 3.16E-01 1.72E+00 8.08E-01
Glioblastopma 2A00.00 Nervous tissue 5.47E-01 -1.46E-01 -1.42E-01
Glioma 2A00.0Y-2A00.0Z Brain stem tissue 7.58E-02 3.46E-01 1.66E+00
Glioma 2A00.0Y-2A00.0Z White matter tissue 9.74E-01 2.26E-01 1.78E-01
Head and neck cancer 2D42 Head and neck tissue 6.31E-32 2.41E+00 2.47E+00
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 4.76E-02 1.27E-01 3.54E-01
Huntington's disease 8A01.10 Whole blood 1.73E-01 1.01E+00 9.22E-01
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 4.65E-02 -8.86E-01 -9.34E-01
Immunodeficiency 4A00-4A20 Peripheral blood 1.94E-03 5.72E-02 1.02E+00
Influenza 1E30 Whole blood 2.31E-01 -3.08E-01 -3.14E+00
Interstitial cystitis GC00.3 Bladder tissue 9.47E-03 1.08E+00 1.92E+00
Intracranial aneurysm 8B01.0 Intracranial artery 3.30E-01 6.96E-01 4.04E-01
Irritable bowel syndrome DD91.0 Rectal colon tissue 2.90E-02 5.40E-02 1.84E-01
Ischemic stroke 8B11 Peripheral blood 2.48E-02 1.17E+00 3.89E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 1.83E-08 9.57E-01 1.09E+00
Lateral sclerosis 8B60.4 Skin 1.02E-02 -8.42E-01 -2.67E+00
Lateral sclerosis 8B60.4 Cervical spinal cord 6.47E-01 5.38E-02 1.47E-01
Liver cancer 2C12.0 Liver tissue 4.32E-06 -1.04E+00 -1.03E+00
Liver failure DB99.7-DB99.8 Liver tissue 9.73E-01 4.92E-01 3.65E-01
Lung cancer 2C25 Lung tissue 2.54E-27 -1.16E+00 -9.90E-01
Lupus erythematosus 4A40 Whole blood 6.85E-03 4.86E-01 3.21E-01
Major depressive disorder 6A70-6A7Z Hippocampus 7.54E-01 -4.80E-01 -5.41E-01
Major depressive disorder 6A70-6A7Z Whole blood 5.95E-01 1.23E-01 1.79E-01
Melanoma 2C30 Skin 1.13E-01 3.14E-01 2.60E-01
Multiple myeloma 2A83.1 Peripheral blood 1.44E-01 4.65E-01 8.08E-01
Multiple myeloma 2A83.1 Bone marrow 2.06E-05 7.94E-01 2.10E+00
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 2.45E-01 1.05E+00 6.47E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 8.84E-02 4.60E-01 2.67E-01
Myelofibrosis 2A20.2 Whole blood 8.82E-01 9.93E-02 1.57E-01
Myocardial infarction BA41-BA50 Peripheral blood 2.57E-03 2.24E+00 9.11E-01
Myopathy 8C70.6 Muscle tissue 1.90E-01 1.22E-01 8.33E-01
Neonatal sepsis KA60 Whole blood 2.01E-04 2.50E-01 2.98E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 2.91E-03 -1.71E+00 -1.72E+00
Non-alcoholic fatty liver disease DB92 Liver tissue 7.59E-01 -1.82E-01 -2.77E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 8.98E-01 2.34E-01 2.27E-01
Olive pollen allergy CA08.00 Peripheral blood 1.33E-01 -2.69E+00 -1.13E+00
Oral cancer 2B6E Oral tissue 2.57E-20 2.15E+00 3.06E+00
Osteoarthritis FA00-FA0Z Synovial tissue 3.32E-01 1.67E+00 7.39E-01
Osteoporosis FB83.1 Bone marrow 1.11E-01 1.46E+00 2.30E+00
Ovarian cancer 2C73 Ovarian tissue 8.39E-01 -2.27E-01 -1.70E-01
Pancreatic cancer 2C10 Pancreas 4.99E-02 4.41E-01 3.23E-01
Parkinson's disease 8A00.0 Substantia nigra tissue 2.40E-01 1.26E-01 5.45E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 9.76E-02 4.17E-01 3.93E-01
Pituitary cancer 2D12 Pituitary tissue 2.05E-01 9.35E-01 8.00E-01
Pituitary gonadotrope tumour 2D12 Pituitary tissue 1.36E-01 1.73E+00 1.26E+00
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 3.82E-01 7.25E-02 9.30E-01
Polycythemia vera 2A20.4 Whole blood 8.03E-04 2.57E-01 4.02E-01
Pompe disease 5C51.3 Biceps muscle 8.74E-01 -1.92E-01 -3.11E-01
Preterm birth KA21.4Z Myometrium 9.92E-02 -1.47E+00 -1.30E+00
Prostate cancer 2C82 Prostate 1.12E-01 -3.62E-01 -2.28E-01
Psoriasis EA90 Skin 4.96E-01 3.15E-01 3.19E-01
Rectal cancer 2B92 Rectal colon tissue 2.03E-07 1.68E+00 3.86E+00
Renal cancer 2C90-2C91 Kidney 1.77E-01 3.04E-01 2.89E-01
Retinoblastoma 2D02.2 Uvea 3.15E-03 3.89E-01 3.17E+00
Rheumatoid arthritis FA20 Synovial tissue 9.92E-06 1.36E+00 2.49E+00
Rhinovirus infection CA42.1 Nasal epithelium tissue 3.87E-01 2.30E-01 2.32E-01
Schizophrenia 6A20 Prefrontal cortex 8.68E-03 -3.36E-02 -4.78E-02
Schizophrenia 6A20 Superior temporal cortex 2.21E-01 1.15E-01 4.67E-01
Scleroderma 4A42.Z Whole blood 2.73E-01 1.63E-01 9.41E-01
Seizure 8A60-8A6Z Whole blood 3.18E-01 -4.21E-01 -3.76E-01
Sensitive skin EK0Z Skin 2.69E-02 3.69E-01 3.31E+00
Sepsis with septic shock 1G41 Whole blood 1.26E-05 -2.08E-01 -2.48E-01
Shwachman-Diamond syndrome 3A70.0 Bone marrow 8.28E-01 2.24E-03 1.56E-03
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 1.81E-01 5.37E-02 5.83E-01
Simpson golabi behmel syndrome LD2C Adipose tissue 2.94E-04 1.04E+00 1.01E+01
Sjogren's syndrome 4A43.2 Salivary gland tissue 7.08E-03 1.82E-01 2.12E+00
Skin cancer 2C30-2C3Z Skin 2.41E-04 1.99E-01 2.40E-01
Thrombocythemia 3B63 Whole blood 2.32E-01 4.14E-01 6.58E-01
Thrombocytopenia 3B64 Whole blood 7.83E-01 2.92E-01 4.28E-01
Thyroid cancer 2D10 Thyroid 2.40E-04 5.50E-01 5.62E-01
Tibial muscular dystrophy 8C75 Muscle tissue 3.92E-01 7.80E-02 1.94E-01
Tuberous sclerosis complex LD2D.2 Perituberal tissue 8.32E-01 -2.00E-02 -1.02E-01
Type 2 diabetes 5A11 Liver tissue 2.08E-01 1.68E-03 2.72E-02
Ureter cancer 2C92 Urothelium 3.49E-01 4.23E-02 2.33E-02
Uterine cancer 2C78 Endometrium tissue 2.74E-06 7.36E-01 5.02E-01
Vitiligo ED63.0 Skin 1.60E-01 4.99E-01 5.73E-01
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⏷ Show the Full List of DME Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DME

DME DTT Name Prostaglandin G/H synthase 2 (COX-2) DTT Info
DME DTT Type Successful
27 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aminosalicylic acid DMENSL5 Inflammatory bowel disease DD72 Approved [1]
Carprofen DMHMP05 Pain MG30-MG3Z Approved [2]
Celecoxib DM6LOQU Rheumatoid arthritis FA20 Approved [3], [4], [5]
Diflunisal DM7EN8I Pain MG30-MG3Z Approved [6]
Eicosapentaenoic acid/docosa-hexaenoic acid DMMUCG4 Hypertriglyceridemia 5C80.1 Approved [7]
Etodolac DM6WJO9 Pain MG30-MG3Z Approved [8], [9]
Etoricoxib DM6A4NW Rheumatoid arthritis FA20 Approved [10], [11]
Fenbufen DMXGDFK Arthritis FA20 Approved [12]
Flufenamic Acid DMC8VNH Dysmenorrhea GA34.3 Approved [13]
Flurbiprofen DMGN4BY Rheumatoid arthritis FA20 Approved [14]
Ibuprofen DM8VCBE Pain MG30-MG3Z Approved [15], [16], [17]
Indomethacin DMSC4A7 Rheumatoid arthritis FA20 Approved [1]
Ketoprofen DMRKXPT Musculoskeletal pain MG30 Approved [18]
Lumiracoxib DM1S4AG Knee osteoarthritis FA01 Approved [19]
Meclofenamate sodium DMNL98G Arthritis FA20 Approved [20]
Mefenamic acid DMK7HFI Dysmenorrhea GA34.3 Approved [21]
Meloxicam DM2AR7L Arthritis FA20 Approved [22]
Nabumetone DMAT2XH Pain MG30-MG3Z Approved [23]
Naproxen DMZ5RGV Osteoarthritis FA00-FA05 Approved [24], [25]
Niflumic acid DMJ3I1Q Rheumatoid arthritis FA20 Approved [26]
Phenylbutazone DMAYL0T Chronic pain MG30 Approved [27]
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [5], [28], [29], [30], [31]
Tenoxicam DMVAZP9 Rheumatoid arthritis FA20 Approved [32], [33]
Tiaprofenic acid DM23D7J Pain MG30-MG3Z Approved [34]
Tolmetin DMWUIJE Rheumatoid arthritis FA20 Approved [15]
Valdecoxib DMAY7H4 Osteoarthritis FA00-FA05 Approved [35]
Imrecoxib DMVXLOD N. A. N. A. Phase 4 [36]
⏷ Show the Full List of 27 Approved Drug(s)
10 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(S)-FLURBIPROFEN DMF2O4T Myalgia FB56.2 Preregistration [37]
CG-100649 DMIKMA9 Arthritis FA20 Phase 3 [38]
Curcumin DMQPH29 Solid tumour/cancer 2A00-2F9Z Phase 3 [39]
ThermoProfen DMPGH7N Pain MG30-MG3Z Phase 3 [40]
Darbufelone DMYVKM5 Asthma CA23 Phase 2/3 [41]
CIMICOXIB DMTKSVA Pain MG30-MG3Z Phase 2 [42]
FK-3311 DML5AE4 Rheumatoid arthritis FA20 Phase 2 [43]
SC-75416 DM58HR7 Pain MG30-MG3Z Phase 2 [44]
CA102N DMYDNQ2 Solid tumour/cancer 2A00-2F9Z Phase 1 [45]
RWJ-67657 DM6YAGE Arthritis FA20 Phase 1 [46]
⏷ Show the Full List of 10 Clinical Trial Drug(s)
2 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Carbamate derivative 2 DMEWPQ6 N. A. N. A. Patented [47]
PMID29130358-Compound-LonimacranthoideVI DMTJEU5 N. A. N. A. Patented [48]
32 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
INDOPROFEN DM5QSKN Gout FA25 Withdrawn from market [37]
GW-406381 DMJ4KQS Neuropathic pain 8E43.0 Discontinued in Phase 3 [49]
PMI-001 DMDZBIQ Lupus 4A40 Discontinued in Phase 3 [50]
PRINOMIDE TROMETHAMINE DMI02PF Inflammation 1A00-CA43.1 Discontinued in Phase 3 [51], [52]
Apricoxib DMR3Q82 Non-small-cell lung cancer 2C25.Y Discontinued in Phase 2 [53]
CRx-401 DM39N7W Type-2 diabetes 5A11 Discontinued in Phase 2 [54]
GSK-644784 DMUC9OS Neuropathic pain 8E43.0 Discontinued in Phase 2 [49]
R-ketoprofen DMHSUQ1 N. A. N. A. Discontinued in Phase 2 [37]
RQ-00317076 DM4GVZ9 Pain MG30-MG3Z Discontinued in Phase 2 [55]
S-2474 DMMSZ1A Rheumatoid arthritis FA20 Discontinued in Phase 2 [56]
TEBUFELONE DMMUE8P Pain MG30-MG3Z Discontinued in Phase 2 [57]
Tilmacoxib DMPWSRA Colon polyp DB35 Discontinued in Phase 2 [58]
DUP 697 DMUMAHC Pain MG30-MG3Z Discontinued in Phase 1 [59]
E-6087 DM79MI4 Pain MG30-MG3Z Discontinued in Phase 1 [60], [52]
GR-253035 DMWY2F6 Alzheimer disease 8A20 Discontinued in Phase 1 [61]
SC-57666 DMIVRWS Rheumatoid arthritis FA20 Discontinued in Phase 1 [57]
ATLIPROFEN METHYL ESTER DMS2FB3 Inflammation 1A00-CA43.1 Terminated [1]
Flosulide DM6OIJ1 Pain MG30-MG3Z Terminated [62]
FR-123826 DM0582D Rheumatoid arthritis FA20 Terminated [63]
L-745337 DMOQIWH Asthma CA23 Terminated [64]
L-768277 DM7J6QH Hyperthermia MG26 Terminated [65]
Nimesulide DMR1NMD Metastatic colorectal cancer 2B91 Terminated [66]
NMI-150 DMX6DNZ Pain MG30-MG3Z Terminated [67]
NS398 DMINUWH Endometriosis GA10 Terminated [25]
ON-09300 DMMLXRG Solid tumour/cancer 2A00-2F9Z Terminated [1]
RPR 200765A DM1U0TB Rheumatoid arthritis FA20 Terminated [68]
RWJ-63556 DMUDE1T Arthritis FA20 Terminated [69]
S-33516 DMF710M Arthritis FA20 Terminated [70]
SB 203580 DMAET6F N. A. N. A. Terminated [71]
SC-236 DMO1URE Solid tumour/cancer 2A00-2F9Z Terminated [72]
SC-58125 DM874YU N. A. N. A. Terminated [73]
SC-58451 DMVGK24 N. A. N. A. Terminated [74]
⏷ Show the Full List of 32 Discontinued Drug(s)
126 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(11H-Dibenzo[b,e][1,4]dioxepin-2-yl)-acetic acid DMSUPVE Discovery agent N.A. Investigative [75]
(11H-Dibenzo[b,e][1,4]dioxepin-7-yl)-acetic acid DM5ZTXL Discovery agent N.A. Investigative [75]
(11H-Dibenzo[b,e][1,4]dioxepin-8-yl)-acetic acid DMBY623 Discovery agent N.A. Investigative [75]
(E)-2-(4-(methylsulfonyl)styryl)furan DMH2U4Z Discovery agent N.A. Investigative [76]
(E)-2-(4-(methylsulfonyl)styryl)thiophene DMDFE1R Discovery agent N.A. Investigative [76]
(E)-3-(4-(methylsulfonyl)styryl)thiophene DMUS0D8 Discovery agent N.A. Investigative [76]
(E)-4-(2-(furan-2-yl)vinyl)benzenesulfonamide DMDF7M4 Discovery agent N.A. Investigative [76]
(E)-4-(2-(thiophen-2-yl)vinyl)benzenesulfonamide DM7204O Discovery agent N.A. Investigative [76]
(E)-4-(2-(thiophen-3-yl)vinyl)benzenesulfonamide DMTAB8W Discovery agent N.A. Investigative [76]
(R)-2-(4-Isobutyl-phenyl)-N-phenyl-propionamide DMAD4JY Discovery agent N.A. Investigative [37]
(Z)-2'-des-methyl sulindac sulfide DM0OEQJ Discovery agent N.A. Investigative [77]
1,2-dihydro-3-(2,3,4-trimethoxyphenyl)naphthalene DMST60D Discovery agent N.A. Investigative [78]
1,3-bis(nitrooxy)propan-2-yl 2-acetoxybenzoate DMIK7XV Discovery agent N.A. Investigative [79]
1-(2-hydroxyphenyl)-3-p-tolylprop-2-en-1-one DMAFS7J Discovery agent N.A. Investigative [80]
1-(4-(methylsulfonyl)phenyl)-1H-indole DMCE7G0 Discovery agent N.A. Investigative [81]
1-(4-(methylsulfonyl)phenyl)-1H-pyrrole DMYFBRQ Discovery agent N.A. Investigative [81]
1-(4-(methylsulfonyl)phenyl)-3-p-tolylurea DMMSQLC Discovery agent N.A. Investigative [82]
1-(4-(methylsulfonyl)phenyl)-3-phenylurea DMH7RY0 Discovery agent N.A. Investigative [82]
1-(4-aminosulfonylphenyl)-2-(2-pyridyl)acetylene DMWA6G1 Discovery agent N.A. Investigative [83]
2'-hydroxy-3,4,5-trimethoxychalcone DM5ACNU Discovery agent N.A. Investigative [80]
2'-Hydroxychalcone DM8RTBS Discovery agent N.A. Investigative [80]
2,3-dimethoxy-2'-hydroxychalcone DML92OK Discovery agent N.A. Investigative [80]
2,4'-Dimethoxy-5,3'-di-(2-propenyl)-biphenyl DMWNJ84 Discovery agent N.A. Investigative [84]
2,4'-Dimethoxy-5,3'-dipropyl-biphenyl DM94NM7 Discovery agent N.A. Investigative [84]
2,4-dimethoxy-2'-hydroxychalcone DMP9BZU Discovery agent N.A. Investigative [80]
2,6-dihydroxy-1,7-dimethoxyxanthone DM5QEUC Discovery agent N.A. Investigative [85]
2-(2,3,4-trimethoxyphenyl)-1H-indene DMFU1PK Discovery agent N.A. Investigative [78]
2-(2-(2,6-dimethylphenylamino)phenyl)acetic acid DMJ2DE4 Discovery agent N.A. Investigative [86]
2-(3-Phenyl-propyl)-1,2-dihydro-indazol-3-one DMIQBXD Discovery agent N.A. Investigative [87]
2-(4-(methylsulfonyl)phenyl)-3-phenylquinoline DMVD6HE Discovery agent N.A. Investigative [88]
2-(4-(methylsulfonyl)phenyl)pyridine DM1TZNK Discovery agent N.A. Investigative [81]
2-(N-(2-Ffuorophenyl)pyrrol-3-yl) acetic acid DMRNOM6 Discovery agent N.A. Investigative [89]
2-(N-(2-fluorophenyl)pyrrol-2-yl) acetic acid DMCL9E6 Discovery agent N.A. Investigative [89]
2-(p-Methylsulfonylbenzoyl)furan DMLT635 Discovery agent N.A. Investigative [81]
2-Benzyl-1,2-dihydro-indazol-3-one DM1CB5J Discovery agent N.A. Investigative [87]
2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-one DMQIRY7 Discovery agent N.A. Investigative [87]
2-Methyl-1,2-dihydro-indazol-3-one DMDJHFQ Discovery agent N.A. Investigative [87]
2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-one DM1EJ6W Discovery agent N.A. Investigative [87]
2-Phenethyl-1,2-dihydro-indazol-3-one DM0WMBC Discovery agent N.A. Investigative [87]
2-Phenyl-1,2-dihydro-indazol-3-one DM28CLZ Discovery agent N.A. Investigative [87]
3 beta-O-acetyloleanolic acid DM1L5IJ Discovery agent N.A. Investigative [90]
3,4-dibenzyloxy-2'-hydroxychalcone DMBUT8A Discovery agent N.A. Investigative [80]
3,4-dihydroxyxanthone DMTQX92 Discovery agent N.A. Investigative [85]
3-(4-Methanesulfonyl-phenyl)-1-phenyl-propynone DMSR2O3 Discovery agent N.A. Investigative [91]
3-benzyloxy-4-methoxy-2'-hydroxychalcone DMKD874 Discovery agent N.A. Investigative [80]
3-Bromo-2'-hydroxy-4-methoxychalcone DM1BALV Discovery agent N.A. Investigative [80]
4,5-Bis(4-chlorophenyl)-1,2-selenazole DMIO254 Discovery agent N.A. Investigative [92]
4,5-Bis(4-chlorophenyl)isothiazole DMENLFY Discovery agent N.A. Investigative [93]
4,5-Bis(4-methoxyphenyl)-1,2-selenazole DMKHD1M Discovery agent N.A. Investigative [92]
4,5-Bis(4-methoxyphenyl)-3H-1,2-dithiol-3-one DMI39QT Discovery agent N.A. Investigative [93]
4,5-Bis(4-methoxyphenyl)isothiazole DM90DV6 Discovery agent N.A. Investigative [93]
4-((4-methoxyphenyl)diazenyl)benzenesulfonamide DMNAT1D Discovery agent N.A. Investigative [94]
4-(3-hydroxy-benzylideneamino)-benzenesulfonamide DMY2OVL Discovery agent N.A. Investigative [95]
4-(3-methoxy-benzylideneamino)-benzenesulfonamide DMO8SQA Discovery agent N.A. Investigative [95]
4-(3-nitro-benzylideneamino)-benzenesulfonamide DMD94OB Discovery agent N.A. Investigative [95]
4-(4-Chlorophenyl)-5-p-tolyl-1,2-selenazole DMZBEYO Discovery agent N.A. Investigative [92]
4-(4-fluoro-benzylideneamino)-benzenesulfonamide DMRJD75 Discovery agent N.A. Investigative [95]
4-(4-fluoro-phenyliminomethyl)-benzenesulfonamide DMK8DCF Discovery agent N.A. Investigative [95]
4-(4-hydroxy-benzylideneamino)-benzenesulfonamide DMNY0I5 Discovery agent N.A. Investigative [95]
4-(4-methoxy-benzylideneamino)-benzenesulfonamide DM2OR8E Discovery agent N.A. Investigative [95]
4-(4-methyl-benzylideneamino)-benzenesulfonamide DMZSQ04 Discovery agent N.A. Investigative [95]
4-(4-methyl-phenyliminomethyl)-benzenesulfonamide DMV0S4U Discovery agent N.A. Investigative [95]
4-(4-nitro-benzylideneamino)-benzenesulfonamide DMM86YK Discovery agent N.A. Investigative [95]
4-(benzylideneamino)benzenesulfonamide DM03BQD Discovery agent N.A. Investigative [95]
4-amino-N-(4-chlorophenyl)benzenesulfonamide DMCUSD4 Discovery agent N.A. Investigative [96]
4-amino-N-(4-iodophenyl)benzenesulfonamide DMN19QP Discovery agent N.A. Investigative [96]
4-benzyloxy-2'-hydroxychalcone DMDC7TL Discovery agent N.A. Investigative [80]
4-fluoro-N-(4-(methylsulfonyl)phenyl)aniline DMV6M5U Discovery agent N.A. Investigative [81]
4-phenyliminomethyl-benzenesulfonamide DM9J5TZ Discovery agent N.A. Investigative [95]
5,3'-Dipropyl-biphenyl-2,4'-diol DMJRXLD Discovery agent N.A. Investigative [84]
5-(2-Imidazol-1-yl-ethyl)-7,8-dihydro-quinoline DMCP5U8 Discovery agent N.A. Investigative [97]
5-(4-Chlorophenyl)-4-p-tolyl-1,2-selenazole DMY0P86 Discovery agent N.A. Investigative [92]
5-(4-Methoxyphenyl)-4-p-tolyl-1,2-selenazole DMEV8WS Discovery agent N.A. Investigative [92]
5-Ethyl-3,4-diphenyl-isoxazole DMRIGXA Discovery agent N.A. Investigative [98]
5-methoxy-2-(4-(methylsulfonyl)phenyl)-1H-indole DMG2HSU Discovery agent N.A. Investigative [99]
5-Methyl-3,4-diphenyl-isoxazole DM0G2N5 Discovery agent N.A. Investigative [98]
5-Phenyl-pentanoic acid benzyl-hydroxy-amide DM3B6A8 Discovery agent N.A. Investigative [100]
5-thia-8,11,14,17-eicosatetraenoic acid DMF4RGW Discovery agent N.A. Investigative [7]
6,7'-oxybis(2-phenyl-4H-chromen-4-one) DMT09YC Discovery agent N.A. Investigative [101]
8alpha,19-dihydroxylabd-13 E-en-15-oic acid DM7K2DN Discovery agent N.A. Investigative [102]
Alpha-linolenic acid DMY64HE Discovery agent N.A. Investigative [7]
B-Octylglucoside DMMO75G Discovery agent N.A. Investigative [103]
Bimetopyrole DMPR14J Pain MG30-MG3Z Investigative [59]
C-myb DMA5Z2G Pain MG30-MG3Z Investigative [104]
CLEMATOMANDSHURICA SAPONIN A DM4SKYA Discovery agent N.A. Investigative [105]
CLEMATOMANDSHURICA SAPONIN B DMNWXOC Discovery agent N.A. Investigative [105]
CR-4174 DM3M5AW Inflammation 1A00-CA43.1 Investigative [106]
CX-9051 DM526C9 Solid tumour/cancer 2A00-2F9Z Investigative [106]
DFU DMUM84K Pain MG30-MG3Z Investigative [107]
Firocoxib DMP6GNY Discovery agent N.A. Investigative [108]
Fluoro loxoprofen DMJS62X Discovery agent N.A. Investigative [109]
Furan-3-yl(4-(methylsulfonyl)phenyl)methanone DMPC6YL Discovery agent N.A. Investigative [81]
GW-637185X DMX59A0 Discovery agent N.A. Investigative [110]
Heme DMGC287 Discovery agent N.A. Investigative [111]
HONOKIOL DMJWT3X Discovery agent N.A. Investigative [84]
L-748780 DMJZXAF Discovery agent N.A. Investigative [112]
L-761000 DM0A2MG Discovery agent N.A. Investigative [112]
LM-4108 DMWLMTD Discovery agent N.A. Investigative [113]
METHYLHONOKIOL DM9YE6K Discovery agent N.A. Investigative [84]
Microxine DM7Y9AD Pain MG30-MG3Z Investigative [114]
N-(1H-indazol-5-yl)acetamide DMIMJNU Discovery agent N.A. Investigative [115]
N-(3-(phenylthio)pyridin-4-yl)methanesulfonamide DMSJX1H Discovery agent N.A. Investigative [116]
N-(3-phenoxy-4-pyridinyl)ethanesulfonamide DMXF46V Discovery agent N.A. Investigative [117]
N-(3-phenylamino-4-pyridinyl)methanesulfonamide DMJB7SE Discovery agent N.A. Investigative [116]
Nectamazin C DMO0Q1F Discovery agent N.A. Investigative [118]
NEOLIGNAN 9-NOR-7,8-DEHYDRO-ISOLICARIN B DMKFPA9 Discovery agent N.A. Investigative [118]
Nitroflurbiprofen DMWCV48 Discovery agent N.A. Investigative [119], [14], [120]
NSC-27236 DMANZIE Discovery agent N.A. Investigative [94]
OCOPHYLLALS A DMT59UG Discovery agent N.A. Investigative [118]
Ocophyllals b DMEUPVF Discovery agent N.A. Investigative [118]
Oxametacin DMWVLG1 Discovery agent N.A. Investigative [121]
Oxindole 94 DMPFD6Y Pain MG30-MG3Z Investigative [122]
PAC-10649 DMKL6IC Arthritis FA20 Investigative [123]
PHENIDONE DMJD8XN Discovery agent N.A. Investigative [87]
Prifelone DMLI4RF Discovery agent N.A. Investigative [124]
Primary alcohol metabolite of celecoxib DMA8GI6 Discovery agent N.A. Investigative [125]
Prostaglandin G2 DME74SP Discovery agent N.A. Investigative [111]
Resveratrol Potassium3-Sulfate DMN1RLA Discovery agent N.A. Investigative [126]
Resveratrol Potassium4,-Sulfate DMMFP57 Discovery agent N.A. Investigative [126]
SB 239063 DM201Q7 Pain MG30-MG3Z Investigative [127]
SC-558 DMAZLKX Discovery agent N.A. Investigative [128]
Silicon-modified indomethacin DM5ZILV Arthritis FA20 Investigative [106]
TENOSAL DMMLSZ4 Rheumatoid arthritis FA20 Investigative [129], [52]
THIOCTIC ACID DMNFCXW Discovery agent N.A. Investigative [92]
Wogonin DMGCF51 Discovery agent N.A. Investigative [80]
XGP-110 DM96FTS Arthritis FA20 Investigative [106]
⏷ Show the Full List of 126 Investigative Drug(s)

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99 Synthesis and biological evaluation of new 4-carboxyl quinoline derivatives as cyclooxygenase-2 inhibitors. Bioorg Med Chem. 2009 Jul 15;17(14):5312-7.
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102 Cyclooxygenase (COX)-1 and -2 inhibitory labdane diterpenes from Crassocephalum mannii. J Nat Prod. 2008 Jun;71(6):1070-3.
103 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
104 Cyclooxygenase-2, a colorectal cancer nonsteroidal anti-inflammatory drug target, is regulated by c-MYB. Cancer Res. 2000 Apr 1;60(7):1805-9.
105 Triterpene saponins from clematis mandshurica. J Nat Prod. 2006 Nov;69(11):1591-5.
106 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: 1376).
107 Inhibition of cyclooxygenase-2 improves cardiac function in myocardial infarction. Biochem Biophys Res Commun. 2000 Jul 5;273(2):772-5.
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