T0179 |
Ticagrelor |
Ticagrelor is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. |
T0595 |
Naringin |
Naringin, a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibiti...
|
T0603 |
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...
|
T0660 |
Beta-Tetralone |
Beta-Tetralone is a ketone derivative of tetralin. |
T0679 |
Ketoconazole |
Ketoconazole, a CYP3A4 inhibitor, is an imidazole anti-fungal agent. |
T0792 |
(-)-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. |
T0920 |
Ambroxol |
Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. It is the active ingredient of Mucosol...
|
T1011 |
Itraconazole |
Itraconazole is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis. |
T10335 |
Antihistamine-1 |
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...
|
T10535 |
BI 653048 |
BI 653048 is a selective and orally active agonist of nonsteroidal glucocorticoid (IC50: 55 nM). BI 653048 is also an HCV NS3 protease inhibitor. |
T10535L |
BI 653048 phosphate |
BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM). |
T10688 |
Casopitant mesylate |
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 ant...
|
T10891 |
CRTH2-IN-1 |
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. |
T10923 |
CYP17-IN-1 |
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. |
T11065 |
DMU2105 |
DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively. |
T11066 |
DMU2139 |
DMU2139 is a potent and specific CYP1B1 inhibitor with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively. |
T1149 |
Fenofibrate |
Fenofibrate is a peroxisome proliferator receptor alpha agonist. Fenofibrate is a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic...
|
T1187 |
Bifonazole |
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 ...
|
T11964 |
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). |
T12146 |
N-Desmethyl Apalutamide |
N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite. |
T1274 |
Benzbromarone |
Uricosuric is an effective inhibitor of CYP2C9 used in the treatment of gout. |
T1415 |
Gemfibrozil |
Gemfibrozil interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an in...
|
T1443 |
Memantine hydrochloride |
Memantine hydrochloride is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent. |
T14678 |
BMS-819881 |
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 CYP3...
|
T1597 |
Proadifen hydrochloride |
Proadifen hydrochloride is an inhibitor of drug metabolism and cytochrome P-450 enzyme system activity. |
T16111 |
ML604086 |
ML604086 suppresses CCL1 mediated chemotaxis and enhances intracellular Ca2 concentrations. ML604086 is a selective inhibitor of CCR8. It also inhibiting CCL1 b...
|
T16739 |
RG-12525 |
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 pep...
|
T1704 |
Diosmetin |
Diosmetin has been found to act as a weak TrkB receptor agonist. |
T2143 |
Bergapten |
Bergapten, a psoralen, inhibits cell replication. |
T2175 |
Apigenin |
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 soothin...
|
T2532 |
Tauroursodeoxycholic Acid |
Tauroursodeoxycholic acid is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans. Tauroursodeox...
|
T2753 |
Avasimibe |
Avasimibe is an orally bioavailable inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT, IC50: 3.3 μM) that prevents cholesterol deposition in the ...
|
T2838 |
Naringenin |
Naringenin is a flavanone that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, antiinflammatory, carbohydrate m...
|
T2944 |
Sodium Danshensu |
Danshensu (sodium salt) is sodium salt of danshensu from the widely used Chinese herb Danshen. It can inhibited phenylephrine- and CaCl2-induced vasoconstrictio...
|
T2945 |
Germacrone |
Germacrone, a major active component found in Curcuma zedoaria oil product, shows anti-inflammatory, antiandrogenic, and antivirus activities. It also inhibits ...
|
T2946 |
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 ...
|
T2949 |
Alizarin |
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...
|
T2S0663 |
Humantenmine |
1. Humantenmine is a toxic compound isolated from Gelsemium elegans Benth . 2. Humantenmine and koumine may inhibit several CYP450 enzyme activities. |
T3002 |
Piperine |
Piperine (1-Piperoylpiperidine), a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders. |
T3355 |
Naloxegol oxalate |
Naloxegol oxalate is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation. |
T3401 |
Ginsenoside F1 |
Ginsenoside F1 is an enzymatically modified derivative of ginsenoside Rg1, showing competitive inhibition of the activity of CYP3A4 and a weaker inhibition of t...
|
T3411 |
Curdione |
Curdione inhibits CYP3A4 activity and the production of prostaglandin E2. Curdione inhibits proliferation of MCF-7 cells by inducing apoptosis. Curdione may be ...
|
T3417 |
Amentoflavone |
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 ...
|
T3585 |
TMS |
TMS is a very selective and potent competitive inhibitor of P450 1B1 (CYP1A1). |
T3669 |
Curcumenol |
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 us...
|
T3698 |
alpha-Asarone |
Alpha-Asarone is a psychoactive compound with antidepressant-like activity in mice. |
T3736 |
Olivetol |
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 o...
|
T3768 |
Epifriedelanol |
Epifriedelanol suppresses adriamycin-induced cellular senescence, replicative senescence in human fibroblasts (HDFs) and HUVECs. Because of Epifriedelanol can ...
|
T3776 |
Rhapontigenin |
Rhapontigenin is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic arom...
|
T3797 |
Isosilybin |
Isosilybin and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients. |
T3811 |
Ginsenoside C-K |
Ginsenoside C-K is a bacterial metabolite of G-Rb1 exhibiting anti-inflammatory effects by reducing iNOS and COX-2. |
T3886 |
Rosavin |
Rosavin has antidepressant and anxiolytic actions, helps balance all the neurotransmitters. |
T4188 |
SDZ285-428 |
NVP-VID-400 (SDZ285-428) is a CYP24A1 inhibitor. |
T4498 |
Stiripentol |
Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively)...
|
T4567 |
Sulfaphenazole |
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/CYP2...
|
T4S0800 |
Demethyleneberberine |
Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either...
|
T5594 |
Cedrol |
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, respecti...
|
T5715 |
FLAVOKAVAIN A(P) |
FLAVOKAVAIN A(P), a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-depende...
|
T5786 |
TETRAHYDROPIPERINE |
TETRAHYDROPIPERINE is a natural product derived from piperine, can be used to treat convulsion, epilepsy, relieve pain, and control insects. |
T5953 |
1-Aminobenzotriazole |
1-Aminobenzotriazole (ABT) is a non-specific cytochrome P450 (CYP) inhibitor. |
T5S0669 |
Bergamotine |
1. Bergamotine can significantly reduce blood glucose and increase glucose tolerance and insulin sensitivity in KK-A<sup>y</sup>diabetic mice. |
T5S2360 |
Corydaline |
1. Corydaline, an isoquinoline alkaloid, is one of the major active constituents in a new prokinetic botanical agent. 2. Corydaline promotes gastric emptying a...
|
T6030 |
XL388 |
XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases. |
T6215 |
Abiraterone Acetate |
Abiraterone acetate is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic...
|
T6216 |
Abiraterone |
Abiraterone (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17) inhibitor (IC50: 4 nM). |
T6246 |
Cobicistat |
Cobicistat is a carbamate and thiazole derivative that functions as a CYTOCHROME P450 CYP3A INHIBITOR to enhance the concentration of ANTI-HIV AGENTS, with whic...
|
T6509 |
Galeterone |
Galeterone is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhib...
|
T6S0630 |
Hypaconitine |
Hypaconitine, an active and highly toxic constituent derived from Aconitum species, has anti-inflammatory activity, is widely used to treat rheumatism. |
T6S1894 |
Linderane |
1. Linderane was characterized as a mechanism-based inactivator of CYP2C9. |
T7088 |
Difubenzuron |
Diflubenzuron is a benzoyl-urea insecticide, found to be a potent inhibitor of melanosome synthesis in mouse melanoma cells. Diflubenzuron has also been shown t...
|
T7190 |
Actein |
Actein has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis, it also can prevent oxidative damage to osteoblas...
|
T7370 |
Talarozole |
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 0.4...
|
T7410 |
Furafylline |
Furafylline is a selective inhibitor of human cytochrome P450 (CYP)1A2 (IC50 : 0.07 μM), |
T7427 |
1-Ethynylnaphthalene |
1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 IB1 |
T7472 |
7-Hydroxyflavone |
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-inflammat...
|
T7618 |
Pyributicarb |
Pyributicarb is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR). |
T8125 |
Quinidine sulfate |
Quinidine sulfate dihydrate is a potent and selective cytochrome P450db inhibitor |
T8182 |
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. |
T9113 |
Myristicin |
Myristicin has anti-cholinergic, antibacterial, and hepatoprotective effects, it also has anti-inflammatory properties related with its inhibition of NO, cytoki...
|
TC0039 |
Vasicinone |
Vasicinone may act as a hepatoprotective agent. (±)-Vasicinone has significant antitussive, expectorant, and bronchodilating activities, which can be used to t...
|
TMA0164 |
15-Hydroxydehydroabietic acid |
15-Hydroxydehydroabietic acid exhibits a promising alpha-glucosidase inhibitory activity, it also shows significant antibacterial activities. |
TMA2106 |
(-)-Sparteine |
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...
|
TN1011 |
Rhodionin |
Rhodionin and rhodionin can inhibit cytochrome P450 2D6 non-competitively with high specificity which could have implications for interactions with co-administe...
|
TN1023 |
Miltirone |
Miltirone is a CYPs inhibitor, it has been characterized as a low-affinity ligand for central benzodiazepine receptors. |
TN1027 |
beta-Amyrin |
beta-Amyrin has antiviral, hepatoprotective, antinociceptive, anti-inflammatory, it retard acute inflammation in rat model of periodontitis. |
TN1078 |
Seneciphylline |
Seneciphylline, one of the hepatotoxic pyrolizidine alkaloids, has mutagenic activity in Drosophila and their transfer into rat milk.Seneciphylline can signific...
|
TN1210 |
2-Hydroxy-1-Methoxyaporphine |
2-Hydroxy-1-Methoxyaporphine can inhibit CYP2D6 activity, it also increase the glucose consumption significantly as rosiglitazone. |
TN1343 |
8-Geranyloxypsoralen |
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 a...
|
TN1372 |
alpha-Amyrin |
Alpha-Amyrin is trypsin and chymotrypsin inhibitor,it has antineoplastic,it induces proliferation of human keratinocytes.Alpha-Amyrin can as a hepatomodulatory ...
|
TN1378 |
alpha-Viniferin |
Alpha-viniferin is a prostaglandin H2 synthase inhibitor, which has anti-inflammatory, anti-oxidant, anti-arthritis, and anti-tumor activities. |
TN1416 |
Ayanin |
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-trimethyleth...
|
TN1482 |
Chamaechromone |
Chamaechromone has anti-HBV and insecticidal activity. The hydroxylation of Chamaechromone is inhibited by α±-naphthoflavone, and predominantly catalyzed by r...
|
TN1526 |
Corydalmine |
Corydalmine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains.1-Corydalmine significantly inhibits spo...
|
TN1691 |
Glabrol |
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. |
TN1702 |
Glycycoumarin |
Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6. |
TN1748 |
Humantenirine |
Standard reference |
TN1828 |
Kahweol |
Kahweol has anticarcinogenic, anti-angiogenic,and anti-inflammatory activities, it can block the LPS-induced activation of NF-kappaB by preventing IkappaB degra...
|
TN1854 |
Lasiodin |
Lasiokaurin has anti-oxidative, and antineoplastic activities, it also shows antibacterial activity, esp. against Sarcina lutea. |
TN2144 |
Resveratroloside |
Resveratroloside has cardioprotective effect, it exhibits α±-glucosidase inhibitory activity, it also can inhibit hydroxylation of testosterone by CYP3A4. |
TN2147 |
Retrorsine |
Retrorsine selectively inhibits hepatocyte proliferation and following liver injury evokes small hepatocyte-like progenitor cells. |
TN2179 |
Saponarin |
Saponarin shows in vitro and in vivo hepatoprotective and antioxidant activity against CCl4-induced liver damage. |
TN2687 |
2,3',4,6-Tetrahydroxybenzophenone |
2,3',4,6-Tetrahydroxybenzophenone possesses significant antioxidant activity. |
TN3080 |
5,6,7-Trimethoxycoumarin |
5,6,7-Trimethoxycoumarin shows moderate inhibitory activity against Micrococcus luteus, it also displays an intermediate cytotoxic effects against brine shrimp ...
|
TN3147 |
6',7'-Dihydroxybergamottin |
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 inh...
|
TN3294 |
8alpha-(2-Methylacryloyloxy)hirsutinolide 13-O-acetate |
8alpha-(2-Methylacryloyloxy)hirsutinolide 13-O-acetate shows inhibitory activity toward CYP2A6 and MAO-A and MAO-B enzymes. |
TN3300 |
8alpha-Tigloyloxyhirsutinolide 13-O-acetate |
8alpha-Tigloyloxyhirsutinolide 13-O-acetate shows inhibitory activity toward CYP2A6 and MAO-A and MAO-B enzymes. 8alpha-Tigloyloxyhirsutinolide 13-O-acetate has...
|
TN3379 |
Allocryptopine |
Allocryptopine has certain effects on anti-injury for hepatocyte, ameliorating liver function, and prohibiting hepatic fibrosis; it increases mRNA levels of cyt...
|
TN3574 |
Canadine |
Canadine has antioxidant activity with low-toxic effect. |
TN3627 |
Chalepensin |
Chalepensin behaves as an energy transfer inhibitor at low concentration, it inhibits multiple P450s and that epoxidation activity is crucial for the potential ...
|
TN3875 |
Dipterocarpol |
Dipterocarpol is a dammarane-type triterpenoid, as are the major bioactive compounds of ginseng. Dipterocarpol A shows moderate acetylcholinesterase inhibitory ...
|
TN4130 |
Germacrone 4,5-epoxide |
(4S,5S)-(+)-Germacrone-4,5-epoxide inhibits certain subtypes of cytochrome P450 (CYP). |
TN4277 |
Isocupressic acid |
Isocupressic acid induces abortion in pregnant cows when ingested primarily during the last trimester, it decrease affects the angiogenesis of the female reprod...
|
TN4424 |
Lecanoric acid |
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 ...
|
TN4435 |
Licopyranocoumarin |
Licopyranocoumarin could as a potent neuroprotective drug via markedly blocked MPP+-induced neuronal PC12D cell death and disappearance of mitochondrial membran...
|
TN4800 |
Pisatin |
Pisatin is an isoflavonoid phytoalexin synthesized by pea (Pisum sativum L.). |
TN4928 |
Rutacridone |
Rutacridone has mutagenicity. |
TN5278 |
Zederone |
Zederone has anti-bacterial activity,it inhibits gram-positive bacteria activity. Zederone induces hepatotoxicity implicated the induction of Cyps, which leads ...
|
TQ0109 |
(-)-Cephaeline dihydrochloride |
(-)-Cephaeline (dihydrochloride) is an enantiomer of Cephaeline. Cephaeline is a selective CYP2D6 inhibitor (IC50: 121 μM). |
TQ0191 |
Dihydromethysticin |
Dihydromethysticin is one kavalactone found in Piper methysticum. It has marked activity on the induction of CYP3A23. |
TQ0217 |
Gomisin G |
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. |
TQ0276 |
Methysticin |
Methysticin, a major kavalactone extracted from kava, can induce CYP1A1. |
TQ0296 |
N-Nornuciferine |
N-Nornuciferine, an aporphine alkaloid in lotus leaf, significantly inhibits CYP2D6 (IC50: 3.76 μM, Ki: 2.34 μM). |