ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.

HSD-016 (HSD016) is a potent, selective, and efficacious 11β-HSD1 inhibitor with IC50 of 149 and 530 nM for mouse and human 11β-HSD1, respectively.

INCB13739 (INCB-13739) is a potent, selective, oral 11βHSD1 inhibitor (IC50=1.1 nM) with high seelctivity over other dehydrogenases, glucocorticoid and mineralocorticoid receptors..

INU-101 (INU101) is a highly potent, selective, orally acitve 11β-HSD1 inhibitor with IC50 of 26.2 nM, 37 nM and 0.6 nM for mice, rats, and human 11β-HSD1, respectively.

(R)-(-)-Rolipram is a potent and cAMP-specific PDE4 inhibitor with IC50 of 0.22 uM; 2.5-fold more potent than (+)-rolipram (IC50= 2.58 uM) in inhibiting membrane-bound PDE 4.

(S)-(+)-Rolipram is a PDE4-inhibitor and an anti-inflammatory agent, less potent than its R enantiomer.

>98%,Standard References

2-PMPA is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) with an IC50 of 300 pM.

A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor with IC50 values of 7 nM and 24 nM for human and mouse DGAT-1 respectively.

A donepezil analog that can moderately inhibit acetylcholinesterase and metal-induced Aβ aggregation in vitro and shows disassembly of Aβ aggregates.

A donepezil analog that can moderately inhibit acetylcholinesterase and metal-induced Aβ aggregation in vitro and shows disassembly of Aβ aggregates.

A donepezil analog that can moderately inhibit acetylcholinesterase and metal-induced Aβ aggregation in vitro and shows disassembly of Aβ aggregates.

A highly potent, selective, brain-penetrating and orally active phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 0.61 nM.

A highly potent, selective, orally active renin inhibitor with IC50 of 2.1 nM in hPRA assay.

A novel bifunctional PDE4 inhibitor (IC50=5 nM) and long acting β2-adrenoceptor agonist (EC50=8 nM).

A novel potent soluble guanylate cyclase (sGC) activator.

A novel potent, allosteric, orally available muscle glycogen synthase 1 (GYS1) activator with EC50 of 5.2 uM.

A novel potent, allosteric, orally available muscle glycogen synthase 1 (GYS1) activator with EC50 of 5.2 uM.

Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay.

A novel potent, selective PDE5 inhibitor with IC50 of 0.056 nM for PDE5A1.

A novel potent, selective PDE9A inhibitor with IC50 of 11 nM, >45-fold selectivity over other PDE isoforms.

A novel potent, selective, brain-penetrable and orally active PDE2A inhibitor with IC50 of 1.5 and 4.2 nM for human and rat PDE2A, respectively.

A novel potent, selective, orally available DPP-4 inhibitor with IC50 of 9 nM.

A potent and selective, brain penetrant FAAH inhibitor with IC50 of 11 nM.

A potent aromatase inhibitor for the treatment of hypogonadism..

A potent monoamine oxidase B (MAO-B) inhibitor..

A potent, brain penetrant, dual MAO-A and AChE inhibitor that shows neuroprotective effects both in vitro and in vivo.

A potent, covalent, orally active ALDH1A2 inhibitor with IC50 of 0.3 uM.

A potent, orally active, centrally acting aminopeptidase inhibitor, the prodrug of the specific and selective aminopeptidase A inhibitor EC33.

A potent, orally available hydrophobic aminopeptidase inhibitor that structurally mimics the aminopeptidase inhibitor Tostedostat..

Cavosonstat is a potent, orally bioavailable inhibitor of S-nitrosoglutathione reductase (GSNOR) and CFTR modulator.

A potent, relatively selective and orally active adenylyl cyclase 1 (AC1) inhibitor with IC50 of 10 uM (cAMP production inhibition).

A potent, selective adenylyl cyclase AC5/6 inhibitor with IC50 of 7.7/17 uM, respectively.

A potent, selective and orally active human neutrophil elastase (HNE) inhibitor with Ki of 12 nM.

A potent, selective dipeptidyl peptidase-4 (DPP-4) inhibitor for treatment for type 2 diabetes..

Bay-8040 is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 28 nM; displays no significant inhibition toward 68 other pharmacologically relevant targets (>10 uM), and a panel of related serine proteases; shows in vivo efficacy with regard to decreasing cardiac remodeling and amelioration of cardiac function in monocrotaline-induced rat model for pulmonary arterial hypertension.

A potent, selective MMP-2 inhibitor with Ki of 230 nM.

A potent, selective, brain penetrant PDE9A inhibitor with IC50 of 1.8 nM.

BAY-678 is a cell-permeable inhibitor of human neutrophil elastase (HNE).

A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.

A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.

A potent, selective, reversible Cdc25 dual specificity phosphatase inhibitor with Ki of 32/96/40 nM for Cdc25A/B/C, respectively.

A selective protein phosphatase PHLPP inhibitor with IC50 of 4 uM for PP2C domain of PHLPP2.

A selective protein phosphatase PHLPP inhibitor with IC50 of 4 uM for PP2C domain of PHLPP2.

A selective, competitive inhibitor of HMG-CoA reductase, that is also antilipemic.

A selective, reversible inhibitor of MAO-A and serotonin reuptake inhibitor as an antidepressant..

A selective, reversible inhibitor of MAO-A and serotonin reuptake inhibitor as an antidepressant..

BCI is A small-molecule, allosteric inhibitor of DUSP6 (dual-specificity phosphatase 6) with IC50 of 12.3 uM; also inhibits human DUSP1 with IC50 of 11.5 uM; suppresses the ERK-induced activation of Dusp6 and regulates heart size in zebrafish.

A939572 is a potent, and orally bioavailable SCD1 inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.

Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM.

ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).

ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).

Acotiamide acts as an acetylcholinesterase inhibitor

AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.

AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein.

AG-881 is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1) in the cytoplasm and type 2 (IDH2).

AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.

AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM).

Alda-1 is an ALDH2 agonist, cell-permeable activator of both the wild-type ALDH2*1 and the asian E487K mutant ALDH2*2 forms of mitochondrial aldehyde dehydrogenase 2 (mtALDH2).

ALDH3A1 inhibitor EN40 is a potent and selective, covalent, in vivo-active inhibitor of ALDH3A1 with IC50 of 2 uM, demonstrates no activity against ALDH1A3 and ALDH6A1 at 30 uM.

Aliskiren hemifumarate(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.

ALLM (Calpain Inhibitor) is cell-permeable, peptide aldehyde inhibitor of calpains and cathepsins.

AM-2394 is a potent and selective Glucokinase agonist (GKA), which catalyzes the phosphorylation of glucose to glucose-6-phosphate.

AMG 580 (AMG580) is a novel potent, selective phosphodiesterase 10A (PDE10A) inhibitor with IC50 of 0.13 nM.

AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC 50 of 4 nM.

AMG-579 is a potent, selective, CNS penetrant, orally bioavailable PDE10A inhibitor with IC50 of 0.1 nM.

AN-2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines.

Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.

APO866 effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM.

Apremilast(CC10004) is a novel small molecule inhibitor of PDE4 with an IC50 value of 74 nM.

APX-115 (Ewha 18278) is a first-in-class, orally active, pan-NADPH oxidase (Nox) inhibitor with Ki of 1.08, 0.57, 0.63 nM for Nox1, Nox2, and Nox4, respectively.

Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.

Atabecestat (JNJ-54861911, JNJ54861911) is a novel potent, oral beta-secretase (BACE) inhibitor for treatment of Alzheimer's Disease.

Atorvastatin Calcium

Avanafil(TA-1790) is a potent and highly selective phosphodiesterase-5(PDE-5) inhibitor(IC50=5.2 nM) for erectile dysfunction; lower selectivity against PDE1, PDE6, and PDE11.

AZD2716(AZD-2716) is a novel potent, selective, orally bioavailable sPLA2 inhibitor with excellent plasma sPLA2 inhibition (IC50=0.1 nM).

AZD3293 is a potent and selective orally active, brain-permeable BACE1 inhibitor,currently in development as a potential treatment for early Alzheimer’s disease.

AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.

AZD-3988 is a potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50 = 0.6 nM).

AZD-7986(Brensocatib) is a highly potent, reversible, and selective DPP1 inhibitor with enzyme and cell pIC50 of 8.4.

Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100-fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.

Batimastat was used to study the role of MMP in proteolytic release of EGF in human follicular thyroid carcinoma cell line FTC-133.

Activator of soluble guanylyl cyclase (sGC); acts at a nitric oxide (NO)-independent regulatory site in the sGC α1 subunit. Inhibits platelet aggregation (IC50 = 36 nM) and phenylephrine-induced contractions of rabbit aorta (IC50 = 0.30 μM). Also reduces vascular smooth muscle growth through cAMP- and cGMP-dependent PKA and PKG pathways.. For the detailed information of BAY 41-2272, the solubility of BAY 41-2272 in water, the solubility of BAY 41-2272 in DMSO, the solubility of BAY 41-2272 in PBS buffer, the animal experiment (test) of BAY 41-2272, the cell expriment (test) of BAY 41-2272, the in vivo, in vitro and clinical trial test of BAY 41-2272, the EC50, IC50,and affinity,of BAY 41-2272, Please contact DC Chemicals.

Bay 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human); 50-fold more selective for PDE2 compared to PDE1 and greater than 100-fold selective compared to PDE5, PDE3B, PDE4B, PDE7B, PDE8A, PDE9A, PDE10A, and PDE11A.

BAY 85-8501 (BAY85-8501) is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 65 pM.

BAY-1436032 (BAY1436032) is a potent, selective, orally available inhibitor of pan-mutant IDH1 with IC50 of 15 nM for both IDH1 R132H and R132C, respectively.

BEC is a boronic acid-based arginine analog that acts as a slow-binding, competitive transition state inhibitor of arginase I and II (Ki = 310 nM for human recombinant type II arginase, pH 7.5).

Beloranib is being studied as a first-in-class obesity therapy that demonstrates a unique mechanism of action through methionine aminopeptidase 2 (MetAP2 ) inhibition.

Benazepril hydrochloride, an angiotensin converting enzyme inhibitor, which is a medication used to treat high blood pressure.

Benzbromarone is a highly effective and well tolerated non-competitive inhibitor of xanthine oxidase, used as an uricosuric agent, used in the treatment of gout.

beta-secretase inhibitor.

Betrixaban (PRT-054021) is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a).

BI 409306 is an inhibitor of phosphodisterase 9A（PDE9A）.

BI 135585 (BI-135585, BI135585) is a potent, selective, orally active 11β-HSD1 inhibitor with IC50 of 4.3 nM and 53 nM in human adipocytes and primary human adipose tissue, respectively.

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.

BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate.

BIBR-1048 (Dabigatran) is an anticoagulant from the class of the direct thrombin inhibitors.

A novel potent, selective, orally active human 11β-HSD1 inhibitor with IC50 of 3.0 nM.

BMS-986205 is an optimized indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor, is well tolerated with potent pharmacodynamic activity, alone and in combination with nivolumab in advanced cancers in a phase 1/2a trial

BRD7116 competitively binds to bacterial DNA gyrase, exhibits an EC50 of 200 nM for LSCe cells, with cell-non-autonomous anti-leukemia activity.

BVT 2733 is a selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor,protecting osteoblasts against endogenous glucocorticoid induced dysfunction.

BVT 14225 is a new selective 11b-HSD1 inhibitor, it belongs to a class of arylsulfonamidothiazoles with in vitro and in vivo antidiabetic effects

BW-A 78U is a PDE4 inhibitor with an IC50 of 3 μM.

C75 trans is the trans form of C75; C75 is a potent fatty-acid synthase(FASN) inhibitor with IC50 of 35.4 μM(LNCaP cell Proliferation inhibition).

CA-074 Me is a selective and cell-permeable inhibitor of cathepsin B.

Captopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE).

Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.

Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents.

Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.

CB-1158 (INCB-01158) is a potent, selective, oral available Arginase inhibitor with IC50 of 98 nM.

CDC25 Phosphatase Inhibitor I, BN82002, is a cell-permeable ortho-hydroxybenzylamino compound that has been reported to display antitumor properties.

CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

CHR-2797 is an aminopeptidase inhibitor, with IC50 values of 100 nM for LAP3 (LAP), 150 nM for PSAP (PuSA) and 220 nM for CD13 (Aminopeptidase N).

CHS-828 is a pyridyl cyanoguanidine anti-tumor agent that has been identified as a competitive inhibitor of Nampt as well as an inhibitor of NF-κB pathway activity.

Cilastazol is a 2-oxo-quinoline with vasodilator, antimitogenic, antithrombotic, and cardiotonic properties. This compound has been shown to cause inhibition of adenosine uptake, eventually resulting in changes to cAMP levels. Studies have shown Cilostazo

Cilazapril Monohydrate is a angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.

Cilomilast(SB 207499; Ariflo) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity.

Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

CPA inhibitor is a potent inhibitor for carboxypeptidase A (CPA).

CTS-1027 is a potent small molecule inhibitor of MMPs(IC50=0.4 nM/0.6 nM for MMP2/MMP13); >1,000 fold selectivity over MMP1.

CVT-10216 is a potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) (IC50 values are 29 and 1300 nM for ALDH2 and ALDH1, respectively).

D609 is a selective competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor (Ki = 6.4 μM); antiviral and antitumor agent.

Dabigatran etexilate mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.

Darapladib is a selective and orally active inhibitor of Lp-PLA2 (IC50= 270 pM)

DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9. IC50 value: 15 Nm.

Deltarasin is a novel and small molecule inhibitor which can inhibit the KRAS-PDEδ interaction(Kd= 41 nM. binding to PDEδ) and impairs oncogenic KRAS signalling.

DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.

Diacylglycerol acyltransferase inhibitor-1 is a diacylglycerol acyltransferase (DGAT1) inhibitor.

Dipivefrin is a prodrug of epinephrine that is hydrolyzed by cholinesterase and other esterases in the cornea to epinephrine.

DKM 3-42 is a selective, covalent, in vivo-active ALDH3A1 inhibitor with IC50 of 50 uM against purified human ALDH3A1, targets ALDH3A1 catalytic cysteine, impairs both in situ and in vivo lung cancer pathogenicity.

DMP 777(L-694458) is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.

DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10, 742 nM for CYP1B1 and CYP1A1, respectively.

DMU-2105(CYP1B1 inhibitor 7k) is a potent and specific CYP1B1 inhibitor.

Dnp-GPLG is a peptide for use as a negative control for activity of matrix metalloproteinases (MMPs) that cleave peptides containing the sequence Dnp-GPLG.

Dnp-P-Cha-Abu-Cys(Me)-HA-K(Nma)-NH2 is a fluorogenic substrate for matrix metalloproteinase-1 (MMP-1) and MMP-9.

Dnp-P-Cha-G-Cys(Me)-HA-K(Nma)-NH2 is a fluorogenic substrate for matrix metalloproteinase-1 (MMP-1) and MMP-9

Dnp-PLALWAR is a fluorogenic substrate for matrix metalloproteinase-1 (MMP-1) and MMP-8.

Dnp-PLAYWAR is a fluorogenic substrate for matrix metalloproteinase-8 (MMP-8) and MMP-26.The activity of MMP-8 and MMP-26 can be quantified by measuring tryptophan fluorescence that is unquenched upon peptide hydrolysis that removes the N-terminal dinitro

Dnp-PLG-Cys(Me)-HA-DArg-NH2 is a peptide substrate for matrix metalloproteinase-1 (MMP-1).It has an improved kcat/Km ratio compared with the MMP-1 flurogenic substrate Dnp-PLGLWA-DArg-NH2.

Dnp-PLGMWSR is a fluorogenic substrate for matrix metalloproteinase-2 (MMP-2) and MMP-9.The activity of MMP-2 and MMP-9 can be quantified by measuring tryptophan fluorescence that is unquenched upon peptide hydrolysis that removes the N-terminal dinitroph

Dnp-RPLALWRS is a fluorogenic substrate for matrix metalloproteinase-7 (MMP-7).The activity of MMP-7 can be quantified by measuring tryptophan fluorescence that is unquenched upon peptide hydrolysis that removes the N-terminal dinitrophenol (Dnp) group.

DO264 is an inhibitor of α/β-hydrolase domain-containing protein 12 (ABHD12; IC50 = 11 nM).It inhibits ABHD12-dependent hydrolysis of lysophosphatidylserine (lyso-PS) in mouse brain membrane lysates (IC50 = 2.8 nM) and human THP-1 cells.

Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.

Donepezil(E 2020) is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM, respectively.

E6005 potently and selectively inhibited human PDE4 activity with an IC50 of 2.8 nM and suppressed the production of various cytokines from human lymphocytes and monocytes with IC50 values ranging from 0.49 to 3.1 nM.

E-64D is an inhibitor of cathepsins B and L; also thought to inhibit calpain,showed a potent activity for COVID-19(SARS-COV-2)with EC50: MERS-COV(1.275),SARS-COV(0.760)

Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention

Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention

Elenbecestat (E2609) is a novel potent, oral BACE1 inhibitor for treatment of Alzheimer's disease..

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. Phase 2.

Epalrestat is an orally active aldose reductase inhibitor that acts on diabetic neuropathy.

Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively).

FTI 277 HCl is the methyl ester of FTI 277, which is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I.

Galantamine(Narwedin) is a competitive and reversible cholinesterase(AChE) inhibitor.

Galanthamine hydrobromide is a long-acting, centrally active acetylcholinesterase(AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors.

GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.

GKT137831 is a novel and specific dual Nox1/Nox4 inhibitor with Ki of 140±40 nM and 110±30 nM; a potent inhibitor of fibrosis and hepatocyte apoptosis.

GLX351322 is an inhibitor of NADPH oxidase 4, and inhibits hydrogen peroxide production from NOX4-overexpressing cells with an IC50 of 5 μ M.

GM6001 (galardin, ilomastat) is a broad spectrum MMPs inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4-27 nM.

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.

GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme.

HET0016 (HET-0016) is a potent, selective inhibitor of CYP4A, potently inhibits the formation of 20-HETE with IC50 of 8.9 nM in human renal microsomes.

Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).

H-Val-Pro-Pro-OH (TFA), a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM.

IBMX(NSC165960; SC2964) is a competitive nonselective PDEs inhibitor with IC50 of 2-50 uM but does not inhibit PDE8 or PDE9; nonselective adenosine receptor antagonist.

IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity.

IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM.

IDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50 of 59 nM, shows activity in Hela cell (IC50=12 nM).

IDO-IN-2 is an IDO inhibitor extracted from patent WO/2015031295 A1, compound example 1, has IC50 values of 0.068 μM in HeLa cell and 0.16 μM in HEK293 cell.

INCB024360 is a potent IDO1 inhibitor(IC50=10 nM) with desirable pharmaceutical properties, which is poised to start clinical trials in cancer patients.

Irosustat（STX64） is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.

Irsogladine maleate is a selective PDE4 inhibitor that facilitates gap junction intercellular communication through muscarinic acetylcholine receptor binding. It is a potent inhibitor of angiogenesis in wild-type and plasminogen activator-deficient mice.

JNJ0966 is a highly selective compound that inhibited activation of MMP-9 zymogen and subsequent generation of catalytically active enzyme.

JNJ-42165279 is a potent and selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC50 of 70nM.

JTT-551 (JTT551, JTT 551) is a novel potent, selective inhibitor of protein tyrosine phosphatase 1B (PTP1B) with Ki of 0.22 uM, displays >45-fold and >136-fold selectivity over TCPTP, CD45 and LAR.

JTT-551 sodium (JTT551, JTT 551) is a novel potent, selective inhibitor of protein tyrosine phosphatase 1B (PTP1B) with Ki of 0.22 uM, displays >45-fold and >136-fold selectivity over TCPTP, CD45 and LAR.

KML29 is an O-hexafluoroisopropyl carbamate analog of JZL 184 that potently and selectively inhibits MAGL (IC50s = 15, 43, and 5.9 nM in mouse, rat, and human brain proteomes, respectively) over FAAH (IC50s >50 μM).

KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and 5050s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MM

L 006235 is a reversible and potent cathepsin K inhibitor that displays more than a 4000 fold selectivity over cathepsins B, L and S.

LB-100 is a small-molecular protein phosphatase 2A(PP2A)inhibitor with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.

LCZ696 is a first-in-class dual inhibitor of the angiotensin II receptor(AT II receptor) and neprilysin; a novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio).

Leupeptin hemisulfate is a reversible, competitive serine/cysteine protease inhibitor, which has been shown to inhibit cathepsins B, H, L, and S, calpain, and trypsin. Leupeptin hemisulfate is an orally active, antioxidant and anti-inflammatory agent.

Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.

Lisinopril Dihydrate is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.

LMPTP inhibitor 1 is a potent molecule for diabetes which can increase liver IR phosphorylation in vivo and reverses high-fat diet-induced diabetes by inhibiting the IR phosphatase LMPTP.

LSN3154567 is a novel inhibitor of NAMPT with IC50 of 18 nM (NCI-H1155 cell), 49 nM (Calu-6 cell), 333 nM (HCC1937 cell), and 389 nM (MCF-7 cell), respectively.

Luteolin 7-O-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 17.63, 7.99, 11.42, 12.85, 0.03 μM for MMP-1, MMP-3, MMP-8, MMP-9, MMP-13, respectively.

Luteolin-3-O-beta-D-glucuronide is a luteolin glucosiduronic acid consisting of luteolin having a beta-D-glucosiduronic acid residue attached at the 3'-position.

LX1606 is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.

LY2183240 is a novel and highly potent blocker of anandamide uptake (IC50 = 270 pM).

LY2811376 is the first orally available non-peptidicβ-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM.

LY2886721 is an BACE inhibitor used for the treatment of Alzheimer's Disease.

LY315920 (Varespladib) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM,. Phase 3.

Marimastat is a broad spectrum MMP inhibitor and selective TACE inhibitor

Mca-PL is a fluorogenic peptide that has been used as a building block in the synthesis of Mca-PLGL-Dpa-AR-NH2, a fluorogenic substrate for matrix metalloproteinase-2 (MMP-2) and MMP-7.

Merimepodib(VX-497) is a novel noncompetitive inhibitor of IMPDH (Inosine monophosphate dehydrogenase).

Methoxsalen (Oxsoralen)

Mevastatin (Compactin; ML236B) inhibits HMGCR (HMG-CoA reductase) (Ki for acid form is 1 nM) which in turn inhibits isoprenoid biosynthesis and therefore blocks protein isoprenylation and reduces plasma cholesterol levels in humans.

Milrinone(Primacor) is a a potent and selective phosphodiesterase 3 inhibitor with an IC50 of 0.42 μM for the inhibition of FIII PDE