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COX inhibitor
Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions -
muscarinic acetylcholine receptor (mAChR) antagonist
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel. -
muscarinic receptor antagonist
Tolterodine tartrate (Detrol LA) is a muscarinic receptor antagonist which is used for the treatment of urinary incontinence. -
P2X7 modulator
GW791343 HCl acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2) and a positive allosteric modulator of rat P2X7. -
muscarinic receptor antagonist
5-hydroxymethyl tolterodine is a metabolite of Tolterodine, a muscarinic receptor antagonist used in the treatment of urinary incontinence.
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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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Nicotinic (α7) Receptor Modulator
PNU-120596 is a positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors.- Hugo R Arias, .et al. , Br J Pharmacol, 2022, Sep 9 PMID: 36082615
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muscarinic M3 receptor antagoinst
Solifenacin-succinate is a muscarinic M3 receptor antagoinst, used in treatment of urinary incontinence. -
α7 nAChR agonist
PNU 282987 (PNU-282,987)is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors. -
P2Y12 antagonist
Ticagrelor (AZD6140) is the first reversibly binding oral P2Y(12) receptor antagonist that blocks ADP-induced platelet aggregation. -
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 . -
GABA receptor agonist
Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction. -
γ-Secretase Inhibitor
BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease. -
M1/M3 receptor agonist
Cevimeline (AF-102B) is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome. -
gamma-secretase modulator
E 2012 is γ-secretase inhibitor.- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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Gamma-secretase modulator
gamma-secretase modulator 1 is a gamma-secretase modulator, gamma-secretase modulator 1 is useful for 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. -
Gamma-secretase modulator
gamma-secretase modulator 2 is a potent and selective gamma-secretase modulator for treatment of 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. -
neuronal nicotinic receptor agonist
Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM). -
Nicotinic receptor agonist
Metanicotine is a neuronal nicotinic receptor agonist, showing high selectivity for the ??4??2 subtype (Ki=26 nM); > 1,000 fold selectivity than ??7 receptors(Ki= 36000 nM). -
nAChR agonist
Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does. -
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
- Ticlopidine is an adenosine diphosphate (ADP) receptor inhibitor. It inhibits platelet aggregation by altering the function of platelet membranes by blocking ADP receptors. This prevents the conformational change of glycoprotein IIb/IIIa which allows platelet binding to fibrinogen.
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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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NMDA receptor antagonist
Memantine hydrochloride is an antagonist at the NMDA receptor, binding to the ion channel site. it was used in the treatment of Parkinsonism. -
NMDA receptor antagonist
Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker. -
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
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neuromuscular blocking agent
Cisatracurium besylate (51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission. -
COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist