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COX inhibitor
Acetaminophen (paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic drug. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
COX-2 inhibitor
Celecoxib is a sulfa non-steroidal anti-inflammatory drug (NSAID) and selective COX-2 inhibitor used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis.
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Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. -
Gamma secretase inhibitor
DAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively.- Kubra Telli, .et al. , Turkish Journal of Biochemistry, 2023, February 6
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
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COX inhibitor
Diclofenac Sodium is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation. -
AChE inhibitor
Donepezil is a centrally acting reversible acetylcholinesterase inhibitor. -
COMT inhibitor
Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. -
COX inhibitor
Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX (IC50=53.5 nM).- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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AChE inhibitor
Galanthamine is an AChE inhibitor with IC50 of 14 nM. -
COX-1 inhibitor
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) targeting COX-1 with an IC50 of 13 μM.- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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COX-1 inhibitor
Ibuprofen Lysine(Motrin) is a non-steroidal anti-inflammatory drug. -
COX inhibitor
Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively. Indomethacin(Indocid, Indocin) is a non-steroidal anti-inflammatory compound commonly used to reduce fever, pain, stiffness, and swelling.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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COX-1/COX-2 inhibitor
Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively. -
BACE1 inhibitor
LY2886721 is a novel potent agent that is used to treat Alzheimer's Disease in preclinical experiments.- Naomi Ito, .et al. , Br J Pharmacol, 2017, Mar; 174(5): 386-395 PMID: 28012171
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COX inhibitor
Naproxen sodium is a non-selective cyclooxygenase (COX) inhibitor that displays anti-inflammatory, antipyretic and analgesic effects. Has a neuroprotective role against colchicine-induced cognitive impairment and oxidative stress. -
AChE inhibitor
Neostigmine bromide is a reversible acetylcholine esterase inhibitor that binds to the anionic binding site of AChE. -
α-adrenergic (AR) antagonist/CaM inhibitor
Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor. -
COX inhibitor
Phenylbutazone is a compound of research interest as an anti-inflammatory and anti-proliferative agent. -
COX inhibitor
Piroxicam is an effective and potent inhibitor of prostaglandin synthesis and a Cox-1 and Cox-2 inhibitor. -
platelet inhibitor
Prasugrel is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI. -
COX inhibitor
Pravadoline (WIN 48,098) is antiinflammatory and prostaglandin synthesis inhibitor, acting through inhibition of the enzyme cyclooxygenase (COX).- Sharma P, .et al. , Org Lett, 2016, Feb 5;18(3):412-5 PMID: 26745849
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Gamma-secretase inhibitor
RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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Gamma-secretase inhibitor
Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM.- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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GABA uptake inhibitor
SKF 89976A hydrochloride is a potent inhibitor of GABA uptake with IC50 of 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively. -
COX inhibitor
Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions -
γ-secretase inhibitor
YO-01027 is a dipeptidic γ-secretase inhibitor, an antiAlzheimer agent.- Weijun Zhang, .et al. , Stem Cell Rev Rep, 2023, Jan 7 PMID: 36609902
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Gamma secretase inhibitor
LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.
- Haiwen Yu, .et al. , Immunol Invest, 2023, Feb;52(2):241-255 PMID: 36562737
- Wojciech J Szlachcic, .et al. , iScience, 2022, Jul 15;25(7) PMID: 35756892
- Zhang ZH, .et al. , APMIS, 2019, Jul 5 PMID: 31274210
- Bo Pang, .et al. , Biosci Rep, 2018, Dec 21; 38(6): BSR20181922 PMID: 30473538
- Shuo Li, .et al. , Int Immunopharmacol, 2018, Oct;63:129-136 PMID: 30086535
- Jiang BC, .et al. , Viral Immunol, 2017, Sep;30(7):522-532 PMID: 28410452
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γ-secretase inhibitor
Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. -
γ-secretase inhibitor
PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM . -
γ-Secretase Inhibitor
BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease. -
Amyloid-β production inhibitor
gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor. gamma-Secretase Modulators is useful for Alzheimer's disease. -
COX-2 inhibitor
Iguratimod(T 614) is one of a series of 4H-1-benzopyran-4-ones which has potent anti-inflammatory, analgesic and antipyretic activity. Iguratimod(T 614) is a selective inhibitor of cyclo-oxygenase-2 (COX-2), and inhibits the production of interleukin-1 (IL-1), IL-6, IL-8 and tumour necrosis factor. -
LKB1/AAK1 dual inhibitor
Pim1/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK. -
COX inhibitor
Pranoprofen is a non-steroidal anti-inflammatory drug used in ophthalmology -
COX inhibitor
Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity.- Yukari Nakajima, .et al. , Sci Rep, 2018, 8: 7078 PMID: 29728629
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COX inhibitor
Acemetacin is a glycolic acid ester of indometacin. It is metabolized to indometacin, which then acts as an inhibitor of cyclooxygenase, producing the anti-inflammatory effects. -
COX-2 inhibitor
Tolfenamic Acid is a COX-2 inhibitor with IC50 of 0.2 μM. It is one of the class of non-steroidal anti-inflammatory drugs (NSAIDs). It is used to treat the symptoms of migraine. -
COX-2 inhibitor
Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. -
COX inhibitor
Lornoxicam is a non-steroidal COX-1/COX-2 inhibitor. It is a non-steroidal anti-inflammatory drug (NSAID) of the oxicam class with analgesic (pain relieving), anti-inflammatory and antipyretic (fever reducing) properties. -
COX/LOX inhibitor
Licofelone is a dual COX/LOX inhibitor, being considered as a treatment for osteoarthritis. It may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase). Licofelone is the first drug to inhibit both.- Silke Neumann, .et al. , Front Immunol, 2016, 7: 537 PMID: 27994586
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AChR inhibitor
Adiphenine HCl is a nicotinic receptor inhibitor with IC50 of 15 μM, used as an antispasmodic drug -
AChE inhibitor
Rivastigmine tartrate is a dual cholinesterase inhibitor (ChEI). It inhibits both butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). -
Hsp90/SRC/COX-2 Inhibitor
Radicicol is a potent inhibitor of Hsp90, SRC, and Cox-2- Guangsen Li, .et al. , Pharm Biol, 2023, 61(1): 271-280 PMID: 36655371