||Ticagrelor, produced by AstraZeneca, is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. The drug was approved f
||Naringin, a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibition of cytochrome P45
||Beta-Tetralone is a ketone derivative of tetralin.
||Ketoconazole, a CYP3A4 inhibitor, is an imidazole anti-fungal agent.
||(-)-Sparteine sulfate pentahydrate
||Sparteine sulfate pentahydrate is a class 1a antiarrhythmic agent and a sodium channel blocker. It can chelate the bivalents calcium and magnesium.
||Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. It is the active ingredient of Mucosolvan, Lasolvan or Muc
||Itraconazole is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.
||Fenofibrate is a peroxisome proliferator receptor alpha agonist. Fenofibrate is a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.
||Bifonazole acts to destabilize the fungal cytochrome p450 51 enzyme (also known as Lanosterol 14-alpha-demethylase). It works by inhibiting the production of a substance called erg
||Benzbromarone is a CYP2C9 inhibitor with Ki value of 19.3 nM.
||Proadifen hydrochloride is an inhibitor of drug metabolism and cytochrome P-450 enzyme system activity.
||Diosmetin has been found to act as a weak TrkB receptor agonist.
||Bergapten, a psoralen, inhibits cell replication.
||Chamomile is an aromatic oil extracted from the flowers or leaves of the daisy-like plants. Extracts, oils and teas made from chamomile are used for its soothing qualities as a sed
||Tauroursodeoxycholic acid is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans. Tauroursodeoxycholic acid, on the
||Avasimibe is an orally bioavailable inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT, IC50: 3.3 μM) that prevents cholesterol deposition in the arterial wall. It al
||Naringenin is a flavanone that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, antiinflammatory, carbohydrate metabolism promoter,
||Danshensu (sodium salt) is sodium salt of danshensu from the widely used Chinese herb Danshen. It can inhibited phenylephrine- and CaCl2-induced vasoconstriction in Ca2+-free mediu
||Alizarin, a red dye derived from the roots of plants of the madder genus, inhibits P450 isoform CYP1A1( IC50 = 6.2 μM), CYP1A2 (IC50 =10.0 μM )and CYP1B1(IC50 = 2.7 μM).
||Naloxegol oxalate is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation.
||Ginsenoside F1 is an enzymatically modified derivative of ginsenoside Rg1, showing competitive inhibition of the activity of CYP3A4 and a weaker inhibition of the activity of CYP2D
||Curdione inhibits CYP3A4 activity and the production of prostaglandin E2. Curdione inhibits proliferation of MCF-7 cells by inducing apoptosis. Curdione may be a candidate for anti
||Amentoflavone, as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflav
||TMS is a very selective and potent competitive inhibitor of P450 1B1 (CYP1A1).
||Curcumenol, one of the major components of Zedoary turmeric oil, is an antibiotic drug which has anti-Y, anti-inflammation activity. Curcumenol may be safely used without inducing
||Alpha-Asarone is a psychoactive compound with antidepressant-like activity in mice.
||Rhapontigenin is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons th
||Isosilybin and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients.
||Rosavin has antidepressant and anxiolytic actions, helps balance all the neurotransmitters.
||NVP-VID-400 (SDZ285-428) is a CYP24A1 inhibitor.
||XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases.
||TAK-700 (Orteronel) is a potent and highly selective human 17, 20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A
||Orteronel(TAK-700) was selected as a candidate for clinical evaluation. orteronel (TAK-700) is currently in phase III clinical trials for the treatment of castration-resistant pros
||Abiraterone acetate is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistan
||Abiraterone (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM).
||Cobicistat is a carbamate and thiazole derivative that functions as a CYTOCHROME P450 CYP3A INHIBITOR to enhance the concentration of ANTI-HIV AGENTS, with which it is used in comb
||Galeterone is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct m
||1. Humantenmine is a toxic compound isolated from Gelsemium elegans Benth . 2. Humantenmine and koumine may inhibit several CYP450 enzyme activities.
||1. Corydaline, an isoquinoline alkaloid, is one of the major active constituents in a new prokinetic botanical agent. 2. Corydaline promotes gastric emptying and small intestinal t
||1. Linderane was characterized as a mechanism-based inactivator of CYP2C9.
||Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59/0.5
||Sulfaphenazole is an inhibitor of CYP2C9 (Ki: 0.3 μM) that demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki: 63/29 μM for CYP2C8/CYP2C18, respectively, a
||Diflubenzuron is a benzoyl-urea insecticide, found to be a potent inhibitor of melanosome synthesis in mouse melanoma cells. Diflubenzuron has also been shown to inhibit TCDD-induc
||Epifriedelanol suppresses adriamycin-induced cellular senescence, replicative senescence in human fibroblasts (HDFs) and HUVECs. Because of Epifriedelanol can reduce cellular senes
||Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either in vitro or in vivo
||Germacrone, a major active component found in Curcuma zedoaria oil product, shows anti-inflammatory, antiandrogenic, and antivirus activities. It also inhibits the proliferation of
||Phthalic Acid Monooctyl Ester
||Phthalic acid mono-2-ethylhexyl ester (MEHP) is a major bioactive metabolite of diethylhexyl phthalate (DEHP), which inhibits the 17, 20 lyase activity of CYP17.
||Hypaconitine, an active and highly toxic constituent derived from Aconitum species, has anti-inflammatory activity, is widely used to treat rheumatism.
||Cedrol is a cedrane sesquiterpenoid and a tertiary alcohol,Cedrol inhibits the cytochrome P450 (CYP) isoforms CYP2B6 and CYP3A4 (Kis = 0.9 and 3.4 μM, respectively)
||TETRAHYDROPIPERINE is a natural product derived from piperine, can be used to treat convulsion, epilepsy, relieve pain, and control insects.
||FLAVOKAVAIN A(P), a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway
||1-Aminobenzotriazole (ABT) is a non-specific cytochrome P450 (CYP) inhibitor.
||1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 IB1
||Talarozole is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.T
||Furafylline is a selective inhibitor of human cytochrome P450 (CYP)1A2 (IC50 : 0.07 µM),
||7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2.with anti-inflammatory activity
||Pyributicarb is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
||(-)-Cephaeline (dihydrochloride) is an enantiomer of Cephaeline. Cephaeline is a selective CYP2D6 inhibitor (IC50: 121 μM).
||Dihydromethysticin is one kavalactone found in Piper methysticum. It has marked activity on the induction of CYP3A23.
||Methysticin, a major kavalactone extracted from kava, can induce CYP1A1.
||N-Nornuciferine, an aporphine alkaloid in lotus leaf, significantly inhibits CYP2D6 (IC50: 3.76 μM, Ki: 2.34 μM).
||Gomisin G is a natural compound and exhibits potent anti-HIV activity (EC50: 0.006 μg/mL; therapeutic index: 300). It is a good substrate of CYP2C9.
||Memantine hydrochloride is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.
||1. Bergamotine can significantly reduce blood glucose and increase glucose tolerance and insulin sensitivity in KK-A<sup>y</sup>diabetic mice.
||Gemfibrozil interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotei
||Tanshinone IIA sulfonate sodium
||Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human puriner
||Olivetol (5-pentylresorcinol, 5-pentyl-1,3-benzenediol) is an organic compound found in certain species of lichen; it is also a precursor in various syntheses of tetrahydrocannabin
||1. Bergaptol shows very good radical scavenging activity. 2. Bergaptol is a potent inhibitor of debenzylation activity of CYP3A4 enzyme.
||Ginsenoside C-K is a bacterial metabolite of G-Rb1 exhibiting anti-inflammatory effects by reducing iNOS and COX-2.
||Piperine (1-Piperoylpiperidine), a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders.
||Guan-fu base A
||Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.
||Quinidine sulfate dihydrate is a potent and selective cytochrome P450db inhibitor
||Rhodionin and rhodionin can inhibit cytochrome P450 2D6 non-competitively with high specificity which could have implications for interactions with co-administered drugs; they can
||Seneciphylline, one of the hepatotoxic pyrolizidine alkaloids, has mutagenic activity in Drosophila and their transfer into rat milk.Seneciphylline can significantly increased the
||2-Hydroxy-1-Methoxyaporphine can inhibit CYP2D6 activity, it also increase the glucose consumption significantly as rosiglitazone.
||Alpha-viniferin is a prostaglandin H2 synthase inhibitor, which has anti-inflammatory, anti-oxidant, anti-arthritis, and anti-tumor activities.
||Ayanin has vasorelaxant activity, it also may have the potential for use in treating allergic asthma.The IC(50) value of Ayanin (quercetin-3,7,4'-O-trimethylether) is 2.2microM for
||Corydalmine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains.1-Corydalmine significantly inhibits spore germination of al
||Glabrol is a PTP1B inhibitor, it is also a CYP1B1 inhibitor, it shows inhibition of CYP1B1 in live cell assay with the IC50 value of 15uM.
||Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6.
||Kahweol has anticarcinogenic, anti-angiogenic,and anti-inflammatory activities, it can block the LPS-induced activation of NF-kappaB by preventing IkappaB degradation and inhibitin
||Lasiokaurin has anti-oxidative, and antineoplastic activities, it also shows antibacterial activity, esp. against Sarcina lutea.
||Retrorsine selectively inhibits hepatocyte proliferation and following liver injury evokes small hepatocyte-like progenitor cells.
||Saponarin shows in vitro and in vivo hepatoprotective and antioxidant activity against CCl4-induced liver damage.
||beta-Amyrin has antiviral, hepatoprotective, antinociceptive, anti-inflammatory, it retard acute inflammation in rat model of periodontitis.
||8-Geranyloxypsoralen inhibits α²-secretase (BACE1) activity in non-competitive manner, with the IC(50) values <25.0 μM, it can induce vasorelaxation on rat arterial tissues. 8-G
||Alpha-Amyrin is trypsin and chymotrypsin inhibitor,it has antineoplastic,it induces proliferation of human keratinocytes.Alpha-Amyrin can as a hepatomodulatory potent to feasibilit
||Chamaechromone has anti-HBV and insecticidal activity. The hydroxylation of Chamaechromone is inhibited by α±-naphthoflavone, and predominantly catalyzed by recombinant human cyt
||Resveratroloside has cardioprotective effect, it exhibits α±-glucosidase inhibitory activity, it also can inhibit hydroxylation of testosterone by CYP3A4.
||N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite.
||CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.
||CYP17-IN-1 is an effective oral CYP17 inhibitor that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.
||DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
||DMU2139 is a potent and specific CYP1B1 inhibitor with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
||BI 653048 phosphate
||BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM).
||BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM and it also is selective and potent for CYP3A4 activity with an
||Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4 and 0.8 μM).
||BI 653048 is a selective and orally active agonist of nonsteroidal glucocorticoid (IC50: 55 nM). BI 653048 is also an HCV NS3 protease inhibitor.
||Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of antiemetics.
||ML604086 suppresses CCL1 mediated chemotaxis and enhances intracellular Ca2 concentrations. ML604086 is a selective inhibitor of CCR8. It also inhibiting CCL1 binding to CCR8 on ci
||RG-12525 is a PPAR-gamma agonist (IC50: appr 60 nM) and a potent inhibitor of CYP3A4 (Ki: 0.5 µM). RG-12525 is a specific and competitive antagonist of the peptidoleukotrienes, LT
||MCH-1 antagonist 1
||MCH-1 antagonist 1 also inhibits CYP3A4 (IC50: 10μM).MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist (Ki: 2.6 nM).
||Actein has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis, it also can prevent oxidative damage to osteoblasts in osteoporotic p
||Myristicin is a natural product found in spices and umbelliferous plants. Myristicin has anti-cholinergic, antibacterial, and hepatoprotective effects, it also has anti-inflammato
||Vasicinone may act as a hepatoprotective agent. (±)-Vasicinone has significant antitussive, expectorant, and bronchodilating activities, which can be used to treat respiratory dis
||15-Hydroxydehydroabietic acid exhibits a promising alpha-glucosidase inhibitory activity, it also shows significant antibacterial activities.
||2,3',4,6-Tetrahydroxybenzophenone possesses significant antioxidant activity.
||5,6,7-Trimethoxycoumarin shows moderate inhibitory activity against Micrococcus luteus, it also displays an intermediate cytotoxic effects against brine shrimp larvae. 5,6,7-Trimet
||6',7'-Dihydroxybergamottin(DHB), a well-known inhibitor of CYP3A4, the inhibition of CYP3A4 activity by DHB includes the inhibition of POR activity, DHB can inhibit nifedipine oxid
||8alpha-(2-Methylacryloyloxy)hirsutinolide 13-O-acetate shows inhibitory activity toward CYP2A6 and MAO-A and MAO-B enzymes.
||8alpha-Tigloyloxyhirsutinolide 13-O-acetate shows inhibitory activity toward CYP2A6 and MAO-A and MAO-B enzymes. 8alpha-Tigloyloxyhirsutinolide 13-O-acetate has anti-cancer activit
||Allocryptopine has certain effects on anti-injury for hepatocyte, ameliorating liver function, and prohibiting hepatic fibrosis; it increases mRNA levels of cytochromes P450 1A in
||Canadine has antioxidant activity with low-toxic effect.
||Chalepensin behaves as an energy transfer inhibitor at low concentration, it inhibits multiple P450s and that epoxidation activity is crucial for the potential drug interaction thr
||Dipterocarpol is a dammarane-type triterpenoid, as are the major bioactive compounds of ginseng. Dipterocarpol A shows moderate acetylcholinesterase inhibitory activity with the IC
||(4S,5S)-(+)-Germacrone-4,5-epoxide inhibits certain subtypes of cytochrome P450 (CYP).
||Isocupressic acid induces abortion in pregnant cows when ingested primarily during the last trimester, it decrease affects the angiogenesis of the female reproductive system, the d
||Lecanoric acid shows antioxidant activity with an IC50 value of 79-95 ug/ml, it at 100 ug/ml conc. shows high growth stimulating activity in terms of increased dry matter of biomas
||Licopyranocoumarin could as a potent neuroprotective drug via markedly blocked MPP+-induced neuronal PC12D cell death and disappearance of mitochondrial membrane potential, which w
||Pisatin is an isoflavonoid phytoalexin synthesized by pea (Pisum sativum L.).
||Rutacridone has mutagenicity.
||Sparteine is a class 1a antiarrhythmic agent, a sodium channel blocker. The deficient debrisoquine hydroxylation of Sparteine is due to the absence of P-450IID1 protein in the live
||Zederone has anti-bacterial activity,it inhibits gram-positive bacteria activity. Zederone induces hepatotoxicity implicated the induction of Cyps, which leads to the formation of
||Miltirone is a CYPs inhibitor, it has been characterized as a low-affinity ligand for central benzodiazepine receptors.
||Choline Fenofibrate is a choline formulation of fenofibrate, a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.
||Ginsenoside Rd may have properties that inhibit or prevent the growth of tumors.
||Gentiopicroside, a naturally occurring iridoid glycoside, extracted from Gentiana manshurica Kitag, inhibits P450 activity, with an IC50 and a Ki of 61 μM and 22.8 μM for CYP2A6;
||Naringin Dihydrochalcone(Naringin DC) is an inhibitor of CYP enzymes, used as an artificial sweetener.
||DMU2105 is a specific CYP1B1 inhibitor(CYP1B1 and CYP1A1 with IC50 of 10 nM and 742 nM, respectively)
||DMU2139 is a specific CYP1B1 inhibitor (CYP1B1 and CYP1A1 with IC50 of 9 nM and 795 nM, respectively).
||Tetrahydrocurcumin, a major metabolite of curcumin, has strong antioxidant and cardioprotective properties.
||N-Nornuciferine is an aporphine alkaloid in lotus leaf, significantly inhibits CYP2D6 (IC50: 3.76 μM, Ki: 2.34 μM).