CYP3A4-IN-1 is a potent inhibitor of cytochrome P450 3A4 (CYP3A4) (IC50: 0.085 μM).

CYP3A4-IN-2 is a specific inhibitor of cytochrome P450 3A4 (CYP3A4) (IC50: 0.055 μM). CYP3A4-IN-2 is a ritonavir analogue with a more hydrophobic R2 side group and stronger inhibition than ritonavir. CYP3A4-IN-2 is capable of acting as an immunosuppressive and antiviral agent.

CYP3A4-IN-3 is a specific, highly affinity cytochrome P450 3A4 (CYP3A4) (cytochrome P450 3A4 (CYP3A4)) inhibitor (IC50: 0.075 μM). CYP3A4-IN-3 is an analogue of ritonavir with a simpler structure and twice as much inhibition as ritonavir. CYP3A4-IN-3 can be used as an antiviral agent and immunosuppressant.

Esomeprazole Sodium ((S)-Omeprazole sodium) is the S-isomer of omeprazole with selective and irreversible proton pump inhibitor activity.Esomeprazole acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H+-ATPases

1. Bergaptol (4-Hydroxybergapten) shows very good radical scavenging activity. 2. Bergaptol is a potent inhibitor of debenzylation activity of CYP3A4 enzyme.

Amentoflavone (3',8''-Biapigenin), 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. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

Fenofibrate (Lipanthyl) is a peroxisome proliferator receptor alpha agonist. Fenofibrate is a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.

RO6889678 is HBV inhibitor with a complex ADME profile.

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a K i of 0.66 nM. Rolapitant hydrochloride (Rolapitant HCl) does not interact with CYP3A4. Rolapitant hydrochloride shows potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2].

Aβ-IN-1 is a novel, potent and orally active γ-secretase modulator (GSM). Aβ-IN-1 potently reduced Aβ42 levels with an IC 50 value of 0.091 μM in cultured cells without inhibiting CYP3A4. Aβ-IN-1 shows a sustained pharmacokinetic profile.

K777 is a potent, orally active and irreversible inhibitor of cysteine protease. K777 is a potent CYP3A4 inhibitor (IC50= 60 nM). K777 is also a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, which is the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 targets cathepsin-mediated cell entry and wxibits a broad-spectrum antiviral activity. K777 inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

PF-4981517 (CYP3cide) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for CYP3A activity are 0.03 μM,17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. PF-4981517 is able to be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug Metabolism.

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.

Praeruptorin B is an inhibitor of sterol regulatory element-binding proteins (SREBPs). It can also significantly up-regulate CYP3A4 expression and activity via the PXR-mediated pathway.

hCYP3A4-IN-1 (compound C6) is a potent, orally active inhibitor of hCYP3A4, exhibiting IC50 values of 43.93 nM in human liver microsomes (HLMs) and 153.00 nM in the CHO-3A4 stably transfected cell line. It competitively inhibits the CYP3A4-mediated hydroxylation of N-ethyl-1,8-naphthalimide (NEN) with a Ki of 30.00 nM [1].

Isavuconazole (RO-0094815)(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557 with MIC(50)s/MIC(90)s ranged from 0.002/0.004 mg/liter for C. albicans to 0.25/0.5 mg/liter for C. glabrata.

Stiripentol (BCX2600) (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59/0.516 μM and IC50 of 1.58/3.29 μM, respectively.

TAK-715 is a p38 MAPK inhibitor for p38α.

Clarithromycin (A-56268) is a Macrolide Antimicrobial. The mechanism of action of clarithromycin is as a Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 3A Inhibitor, and P-Glycoprotein Inhibitor. The chemical classification of clarithromycin is Macrolides.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.

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)

Alflutinib (ASK120067) is an inhibitor of EGFR, and its targets including EGFR activating mutations and T790M, thus leading to tumor growth inhibition.

Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.

Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.

Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.

HIV-IN-9 (Compound 2b) is an HIV inhibitor with an IC50 value of 6.65 μg/mL, demonstrating high binding affinity for HIV-RT. Additionally, it inhibits the cytochrome P450 isoenzymes CYP3A4, CYP1A2, CYP2C1, and CYP2D6 [1].

Dihydrocubebin, isolated from Piper cubeba, serves as a potent and selective inhibitor of cytochrome P450 3A4 (CYP3A4) [1].

6β-hydroxy Dexamethasone is a metabolite of dexamethasone that is more hydrophilic than the parent compound. Dexamethasone is metabolized by CYP3A4; therefore, quantification of the dexamethasone metabolites, 6α- and 6β-hydroxy dexamethasone, can be used to determine CYP3A4 enzyme activity in humans., The formation of 6-hydroxy dexamethasone metabolites is species-specific, with hamsters producing the highest amount. In rats, dexamethasone hydroxylation is sex-specific, with male rats producing metabolites in similar ratios to humans and female rats producing fewer hydroxylated metabolites than male rats.

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 oxidation in a concentration-dependent manner.

Ginsenoside F1 (20(S)-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 CYP2D6.

Mirtazapine N-oxide is a metabolite of mirtazapine.1It is formed from mirtazapine by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4 in human liver microsomes.

Faldaprevir is an effective NS3/NS4A protease inhibitor potentially for the treatment of HCV infection. Faldaprevir is known to inhibit P-glycoprotein, CYP3A4, and UDP-glucuronosyltransferase 1A1.

N-desmethyl Eletriptan is a metabolite of eletriptan .1It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes. 1.Evans, D.C., O’Connor, D., Lake, B.G., et al.Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoproteinDrug Metab. Dispos.31(7)861-869(2003)

Desmethyl mirtazapine is a metabolite of the antidepressant mirtazapine.1It is formed from mirtazapine by the cytochrome P450 (CYP) isoform CYP3A4.

Nampt-IN-5 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) .

BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM).

TAK-700 salt is a potent and highly selective inhibitor of human 17,20-lyase with an IC50 of 38 nM and is over 1000-fold more selective than other CYPs such as 11-hydroxylase and CYP3A4.

Erythromycin is a macrolide antibiotic that inhibits bacterial protein synthesis by targeting the 50S ribosomal subunit, blocking the progression of nascent polypeptide chains.[1] It is effective against a host of bacterial genera, including Streptococcus, Staphylococcus, and Haemophilus (MIC90s range from 0.015-2.0 mg/l).[2] Erythromycin is known to potently inhibit the cytochrome P450 isoform CYP3A4, which can affect the metabolism of numerous clinically relevant medications.[3],[4] Erythromycin lactobionate is a soluble salt of erythromycin that is typically used for intraperitoneal or intravenous injections.[5],[6]

Resveratroloside has cardioprotective effect, it exhibits α±-glucosidase inhibitory activity, it also can inhibit hydroxylation of testosterone by CYP3A4.

BI 653048 is a selective and orally active agonist of nonsteroidal glucocorticoid (IC50: 55 nM). BI 653048 is also an HCV NS3 protease inhibitor.

AWZ1066S is a highly specific anti-Wolbachia drug candidate for the short-course treatment of filariasis (EC50: 2.5 nM in cell assay).

4-hydroxy Atorvastatin is a metabolite of atorvastatin , an HMG-CoA reductase inhibitor present in formulations that have been used to treat hypercholesterolemia and certain dyslipidemias. Atorvastatin is metabolized by the cytochrome P450 (CYP) isoform CYP3A4 to form 4-hydroxy atorvastatin.

Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (Ki = 15 μM in human liver microsomes).

AP-24567 is a CYP3A4-mediated metabolite.

Voriconazole N-oxide is a major metabolite of the triazole antifungal voriconazole . It is formed via oxidation of voriconazole by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19.

(R)-3-Hydroxy Midostaurin is a potent inhibitor of kinases,is a major metabolite of midostaurin undergoing by the hepatic CYP3A4 enzyme,has the potential for acute myeloid leukemia (AML).

YS-370 is an orally active inhibitor of P-gp and shows moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance to paclitaxel and colchicine and exhibits stronger antitumor activity in combination with paclitaxel.

16α-hydroxy Dehydroepiandrosterone is a metabolite of the endogenous steroid hormone dehydroepiandrosterone .116α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosteronevia16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol .2 1.Miller, K.K.M., Cai, J., Ripp, S.L., et al.Stereo- and regioselectivity account for the diversity of dehydroepiandrosterone (DHEA) metabolites produced by liver microsomal cytochromes P450Drug. Metab. Dispos.32(3)305-313(2004) 2.Hampl, R., and Starka, L.Minireview: 16α-Hydroxylated metabolites of dehydroepiandrosterone and their biological significanceEndocr. Regul.34(3)161-163(2000)

Clindamycin sulfoxide is an active metabolite of the antibiotic clindamycin . It is formed via S-oxidation of clindamycin primarily by the cytochrome P450 (CYP) isoform CYP3A4. Clindamycin sulfoxide inhibits the growth of P. prevotti, B. fragilis, and C. sordelli in vitro with MIC values of 2, 2, and 1 mg/L, respectively.

Kushenol K is a potent and Selective Inhibitor of cGMP Phosphodiesterase 5, it also has inhibitory effects on diacylglycerol acyltransferase (DGAT). Kushenol K shows weak antiviral activity against Herpes simplex virus types I and II.