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DHFR inhibitor
Methotrexate is a cytotoxic agent that inhibits thymidylate synthetase and de novo purine synthesis. -
Dehydrogenase inhibitor
Mono-ammonium glycyrrhizinate(AMGZ) is a unique product derived from Licorice root and has an extremely sweet taste. -
Protein kinase inhibitor
Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.
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Factor Xa inhibitor
BMS-740808 is a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
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PDE3 inhibitor
Cilostazol is a selective inhibitor of 3-type phosphodiesterase (PDE3) with therapeutic focus on cAMP. -
EGFR, PKA,PKC inhibitor
Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent. -
Carbonic anhydrase inhibitor
Diclofenamide (or dichlorphenamide) is a sulfonamide and a carbonic anhydrase inhibitor of the meta-Disulfamoylbenzene class. -
PDE inhibitor
Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. -
carbonic anhydrase inhibitor
Dorzolamide HCl is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent and topically applied in the form of eye drops. Dorzolamide HCl is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension. -
ACE inhibitor
Enalapril is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension and some types of chronic heart failure. -
RAAS inhibitor
Enalaprilat is the active metabolite of enalapril. It is the first dicarboxylate-containing ACE inhibitor and was developed partly to overcome these limitations of captopril. -
15-PGDH inhibitor
Glycyrrhetinic acid inhibits the enzymes (15-hydroxyprostaglandin dehydrogenase and delta-13-prostaglandin) that metabolize the prostaglandins PGE-2 and PGF-2α to their respective 15-keto-13,14-dihydro metabolites which are inactive. -
xanthine oxidase inhibitor
Febuxostat is a non-purine inhibitor of xanthine oxidase (Ki = 1.2 nM). -
HMG-CoA reductase inhibitor
Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. -
CYP2D6 inhibitor
Haloperidol (Haldol) is an antipsychotic and butyrophenone. -
PDE4 inhibitor
Hesperetin, a selective phosphodiesterase (PDE)4 inhibitor, is present in the traditional Chinese medicine, ?€?Chen Pi.?€? Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. It also is a potential therapy for carcinoid cancer. -
P450 inhibitor
As an antifungal, ketoconazole is structurally similar to imidazole, and interferes with the fungal synthesis of ergosterol, a constituent of fungal cell membranes, as well as certain enzymes. -
Dehydrogenase inhibitor
Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD (disease-modifying antirheumatic drug) class of drugs. Leflunomide is used to relieve symptoms caused by rheumatoid arthritis, such as inflammation, swelling, stiffness, and joint pain. -
PDE4 inhibitor
Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property. -
Hydroxylase Inhibitor
LX 1606 hippurate is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. -
PDE3 inhibitor
Milrinone(Primacor) is a a potent and selective phosphodiesterase 3 inhibitor with an IC50 of 0.42 μM for the inhibition of FIII PDE -
IMPDH inhibitor
Mycophenolate mofetil is a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) in purine biosynthesis (specifically guanine synthesis) which is necessary for the growth of T cells and B cells. -
dopamine beta-hydroxylase inhibitor
Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine. -
DHFR inhibitor
NSC 131463 is a dihydrofolate reductase potent inhibitor with an IC50 of 1 nM. -
TXAS inhibitor
Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM. -
PDE inhibitor
Pimobendan (Vetmedin) is a calcium sensitizer with positive inotropic and vasodilator effects. It is also a selective inhibitor of phosphodiesterase III (PDE3). -
CYP3A4 inhibitor
Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14?? demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours. -
MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. -
HMG-CoA reductase inhibitor
Rosuvastatin (Crestor) is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. Rosuvastatin is a competitive inhibitor of the enzyme HMG-CoA reductase, having a mechanism of action similar to that of other statins. -
PDE4 inhibitor
(S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells. -
MAO Inhibitor
Safinamide Mesylate is mesylate salt of Safinamide, which selectively and reversibly inhibits MAO-B with IC50 of 0.45 μM. -
PDE5 inhibitor
Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM. -
HMG-CoA reductase inhibitor
Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM. -
HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. -
Hydroxylase inhibitor
Tetrahydropapaverine, one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons. -
PDE-5 Inhibitor
Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction. -
CYP17 inhibitor
Voriconazole (Vfend) is a triazole antifungal agent that is available as a lyophilized powder for solution for intravenous infusion. -
CYP17A1 inhibitor
TAK-700 (Orteronel) is an oral, non-steroidal androgen synthesis inhibitor that selectively inhibits the 17,20 lyase enzyme. -
CYP17 inhibitor
Abiraterone acetate (CB7630) is an orally active acetate ester of the steroidal compound Abiraterone with antiandrogen activity. Abiraterone inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1). -
CETP inhibitor
Anacetrapib (MK-0859) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. -
MAO B inhibitor
Rasagiline is a selective irreversible inhibitor of MAO-B (monoamine oxidase-B).

