AG 1406 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 .

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

AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides.

AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM.

AG-1557 is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK).

AG-17 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431.

AG-18(RG-50810; Tyrphostin A23) inhibits EGFR with IC50 of 40 μM.

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

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.

AG-490 (Tyrphostin B42) is an inhibitor of EGFR, ErbB2 and JAK2 with IC50 of 0.1 μM, 13.5 μM, and ~10 μM, respectively.

AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 µM in HT-22 cells.

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).

AG-99 is an inhibitor of EGF receptor kinase with an IC50 value of 10 µM in the human epidermoid carcinoma cell line A431.

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).

AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM.

AHAS inhibitor is a novel acetohydroxyacid synthase(AHAS) inhibitor, a promising drug target against Mycobacterium tuberculosis (MTB).

AHU-377 is an inhibitor of neprilysin with IC50 value of 5 nM.

AI-10-104 is a small molecule inhibitor that interferes with CBFβ binding to RUNX proteins with IC50 of 1.25 uM in FRET assays.

AIC246 is a novel anti-CMV compound which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

AICAR phosphate (Acadesine, AICA Riboside, NSC 105823) is a selective AMPK activator in both hepatocytes and adipocytes.

AIM-100 is a small molecule inhibitor of Ack1 with an IC50 of 24 nM IC50 value: 24 nM [3] Target: Ack1 Ack1 inhibitor AIM-100 not only inhibited Ack1 activation but also suppressed AKT tyrosine phosphorylation, leading to cell cycle arrest in the G1 ph

AK-7 is a cell- and brain-permeable inhibitor of SIRT2 (IC50 = 15.5 μM).

AK778 (Col001) is a small-molecule compound that inhibits the interaction of Hsp47 with collagen, competitively inhibits the interaction and causes the inhibition of collagen secretion by destabilizing the collagen triple helix. .

AKB-9778 is a potent, selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP) with IC50 of 17 pM.

AKOS B018304 is an arylalkylidene derivative, with polar substitution at para-position.

Akt Inhibitor VIII is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity (IC50 = 58 nM, 210 nM, and 2.12 μM; respectively).

AL 082D06(D-06) is the first selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM, exhibits excellent selectivity against AR, PR, MR and ER(Ki > 10 uM).

AL-335 is a potent inhibitor of hepatitis C virus (HCV) NS5B polymerase with IE50 values as low as 70 nM. AL-335 is potentially useful for the Treatment of Hepatitis C Infection. AL-335 demonstrated high levels of the nucleoside triphosphate in vitro in primary human hepatocytes and Huh-7 cells as well as in dog liver following a single oral dose. AL-335 was selected for the clinical development where it showed promising results in phase 1 and 2 trials.

ALB-127158A, also known as ALB-127158(a), is a MCH1 antagonist for the treatment of obesity.

Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).

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).

ALE-0540 is a nerve growth factor (NGF) antagonist that inhibits the binding of NGF to TrkA or both p75 and TrkA with IC50 of 5.88 and 3.72 uM, respectively.

Alexamorelin is a synthetic growth hormone (GH) secretagogue.

Alflutinib (AST-2818, ASK120067) is a third generation EGFR mutation selective tyrosine kinase inhibitor, inhibits EGFR active mutations as well as T790M acquired resistant mutation.The Alflutinib free base form is not stable, so we make it the mesylate s

Alflutinib (AST-2818, ASK120067) is a third generation EGFR mutation selective tyrosine kinase inhibitor, inhibits EGFR active mutations as well as T790M acquired resistant mutation..

ALG1001 (Risuteganib, ALG-1001) is a first-in-class, RGD class oligopeptide that inhibits integrin receptors (αvβ3, αvβ5, and α5β1) associated with angiogenesis; ALG1001 inhibits an integrin-mediated pathway of the vitreoretinal interface, connecting the posterior aspect of the vitreous with the internal limiting membrane of the retina. In blocking this pathway, ALG-1001 helps to achieve vitreous breakdown and separation from the retina.

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

ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.

ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.

ALKS-8700 also known as diroximel fumarate, is a prodrug of monomethyl fumarate in a controlled-release formulation that rapidly and efficiently converts to MMF in the body.

Allitinib (AST-1306, ALS1306)) is a novel potent, selective irreversible EGFR and HER2 inhibitor with IC50 of 0.5 and 3 nM in cell-free assays.

ALLO-1 is a SMO antagonist that inhibits both wild-type (IC50 = 50 nM) and mutant SMO, including the D473H SMO mutant (IC50s = 300-1000 nM).

ALLO-2 is a potent small molecule Smoothened (Smo) antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.

Allopregnanolone is a progesterone metabolite. Allopregnanolone is an allosteric modulator of the GABA receptor.

Allopurinol sodium is a potent xanthine oxidase inhibitor (IC50 values of 0.2 to 50 μM). Allopurinol sodium can be used for the research of hyperuricemia and gout. Antileishmanial effect[1][2].

Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.

Alobresib is a novel BET bromodomain inhibitor with antineoplastic activity..

Alofanib ((RPT-835) is a potent, selective, allosteric FGFR2 inhibitor that significantly inhibits bFGF-induced proliferation of HUVEC cells with IC50 of 11 nM

Alogliptin is an orally administered, anti-diabetic drug in the DPP-4 inhibitor class. A randomized clinical trial reporting in 2011 aimed to determine the efficacy and safety of alogliptin versus placebo and voglibose among newly diagnosed Type 2 diabete

Alovudine is a DNA polymerase subunit gamma-1 (POLG) inhibitor, shows promise for treating AML.

alpha-hederin is a water-soluble pentacyclic triterpenoid saponin, possessing several biological properties such as antispasmodic, moliscicidic, anthelmithic and inhibiting cell proliferation.

Alpha-Mangostin has neuroprotective, anti-cancer, antifungal, neuroprotective, renoprotective, antioxidant and anti-inflammatory activities.

Alprenolol is a non-selective beta blocker as well as 5-HT1A receptor antagonist.

Alprostadil(Caverject) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases.

Alrestatin is an AKR (aldose reductase) inhibitor, which attaches molecules to the active site of the NADP+/enzyme complex in a stacked formation.

ALS-22335 is an anti-virus compound.

Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, that is reported to be the most active Paullone.

Altiratinib is a MET/TIE2/VEGFR2/TRK (A,B,C) kinase inhibitor in Phase 1 clinical development for the treatment of invasive solid tumors including glioblastoma.

Alvelestat (AZD9668) is a novel, oral inhibitor of neutrophil elastase (NE) with the pIC50 of 7.9 for Human NE.

ALW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor, used for cancer treatment.

ALX-5407 is a potent, selective, orally active inhibitor of GlyT1 glycine transporter with IC50 of 3 nM.

ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.

AM-0466 is a potent and selective NaV1.7 Inhibitor (Nav 1.7 IC50 = 21 nM; Nav 1.5 IC50 =>30.0 uM. PXR = 22% @10 uM; CYP 2C9 IC50 = 4.6 uM; CYP3A4 TDI IC50 =>50.0 uM.).

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

AM-2099 is a potent and selective NaV1.7 Inhibitor.

AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist

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

AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also potent GPR55 agonist (EC50 = 39 nM).

AM630 is a selective CB2 receptor antagonist that binds to CB1 and CB2 receptors with Ki values of 5.2 µM and 31.2 nM, respectively.

AM966 is a high affinity, selective, oral LPA1 (lysophosphatidic acid receptor, IC50=17 nM) antagonist, with selectivity for this receptor over the other LPA receptors.

Amcasertib(BBI503) is an orally administered investigational agent designed to inhibit cancer stem cell pathways, including Nanog, by targeting stemness kinases.

AMD3465 is a Potent, selective CXCR4 antagonist; exhibits 8-fold higher affinity than AMD 3100 (Cat.No. 3299). Inhibits SDF-1α-ligand binding (Ki = 41.7 nM).

Amenamevir, also known as ASP2151, is a herpes virus helicase-primase inhibitor.

Ametantrone is a new anthracenedione antineoplastic agents, produced a concentration-dependent inhibition of hepatic microsomal lipid peroxidation.

AMG 319 is an investigational, highly selective, small molecule inhibitor of PI3Kδ that blocks B cell proliferation following BCR stimulation both in vitro and in vivo, inhibits basal AKT phosphorylation, and inhibits proliferation in lymphoid tumor cells

AMG 333 is a potent and highly selective TRPM8 antagonist with an IC50 of 13 nM.

AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM.

AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM; >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2.

AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell.

AMG-073 HCl (Cinacalcet HCl) represents a new class of compounds for the treatment of hyperparathyroidism.

AMG-1 is a potent inhibitor of human c-Met and RON with IC50 values of 4 and 9 nmol/L respectively.

AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.

AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.

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

AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.

AMG-548 is a potent and selective inhibitor of p38α with Ki of 0.5 nM, dispalys weak inhibition for p38β (Ki=3.6 nM), and >5,000-fold selectivity over p38γ and p38δ; shows >1,000-fold selectivity over other 36 kinases, and is efficacious in acute and chro

AMG9810 is a potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC50 = 17 nM).

AMG-Tie2-1 is a highly potent, non-selective inhibitor of Tie-2 (IC50 <1 nM).

AMI-1 is a PRMT and HIV-1 RT polymerase inhibitor.

Aminocaproic acid (Amicar)is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders.

Ammonium pyrrolidine dithiocarbamate (PDTC) is a potent nuclear factor-κB (NF-κB) inhibitor that inhibits IκB phosphorylation, blocks NF-κB translocation to the nucleus and reduces the expression of downstream cytokines.

Amorolfine hydrochloride is a antifungal reagent.

Amoscanate(nithiocyamine) is an experimental anthelmintic agent of the arylisothiocyanate class which was found to be highly effective in animals against the four major species of schistosomes which infect humans,and is also highly active against hookworm

Ampalex (Ampakine CX516) is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator as a treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).

AMPPD, 1,2-dioxo-cyclohexane derivatives, is a new biochemistry ultrasensitive alkaline phosphatase substrate.

Amprenavir (Agenerase) is a HIV protease inhibitor(Ki=0.6 nM) used to treat HIV infection.

Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively.

An acetylcholinesterase (AChE) inhibitor that inhibits both butyrylcholinesterase and acetylcholinesterase.

HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction[1].

An adenosine A1 receptor agonist (EC50= 8.2 nM)..

Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).

An aminoglycoside antibiotic similar in structure to gentamicin B1.

An analog of thymoquinone that blocks pSer/pThr recognition by Plk1 Polo-box domain as a phosphate mimic..

An angiotensin II analog that is an agonist of AT1 angiotensin receptor..

An antibiotic that inhibits eukaryotic protein synthesis by inhibiting peptidyl transferase or the 80S ribosome system.

Naphthoquine phosphate is a potent and orally active antimalarial agent. Naphthoquine phosphate has thorough killing function for various schizonts of plasmodia, including resistance of P. falciparum to Chloroquine.

An antimicrobial agent used as a substitute for chlorophenols

MMAF-Ome belongs to ADC, and inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4-) cell lines, respectively.

An E3 ligase ligand-linker conjugate for PROTAC.

An E3 ligase ligand-linker conjugate for PROTAC..

An E3 ligase ligand-linker conjugate for PROTAC..

An E3 ligase ligand-linker conjugate for PROTAC..

An E3 ligase ligand-linker conjugate for PROTAC.

LE135 is a retinoid acid receptor antagonist, produces pain through direct activation of TRP channels.

An enantiomer of Ibuprofen that is generally not considered a COX inhibitor and is instead thought to be involved in pathways of lipid metabolism as it is incorporated into triglycerides along with fatty acids.

An immunoactive peptide that has been shown to inhibit cell proliferation and induce apoptosis in human leukemia, non-small cell lung cancer, melanoma, and other human cancers.

Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.

IRES-J007 ia an improved IRES inhibitor that blocks IRES-hnRNP A1 binding; binds to a small pocket structure within the RRM-containing fragment of hnRNP A1 (UP1 fragment), inhibits cyclin D1 and c-MYC IRES activity to a greater extent compared with C11 (IRES-C11); significantly reduces tumor growth of GBM xenografts in mice, and markedly reduces the mRNA translational state of cyclin D1 and c-MYC transcripts combined with PP242.

An inhibitor of LPS-induced TNFαrelease.Pomalidomide is thalidomide derivative that displays inhibition of LPS-induced TNFα release. Shows immunomodulator and anticancer effects.

An insulin secretion stimulator by closing the ATP-sensitive potassium KATP channels in pancreatic β cells.

An irreversible, dual EGFR/HER2 inhibitor with IC50 of 0.5/0.4/10/14 nM for wt EGFR/EGFR L858R/EGFR L858R+T790M/HER2 respectively.

PK 11195 is a ligand of translocator protein. It targets Leishmania chemotherapy (IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively).

Rovazolac is a liver x receptor (LXR) modulator extracted from patent WO2013130892A1.

An orally active adenosine receptor agonist that can induce acute cardiovascular toxicity and coronary vascular injury in vivo..

An orally active, irreversible inhibitor of protein disulfide isomerase (PDI), forming a covalent bond with the active site cysteines of PDI.

An orally available, brain penetrant p75NTR ligand that blocks p75-mediated cell death, also increases proliferation and survival of hippocampal neural progenitors.

An oxazolidinone antibiotic that possesses potent antimicrobial activity in vitro and in vivo..

An STAT3 inhibitor that selectively targets the DNA-binding domain of STAT3, without affecting the activation and dimerization of STAT3.

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.

AN3365 is a first-in-class antibiotic that demonstrates potent activity across a wide spectrum of Gram-negative bacteria, including those resistant to many other antibiotics.

ANA-12 is a potent and selective TrkB antagonist with anxiolytic and antidepressant activity in mice.

Anacardic acid inhibits the histone acetyltransferase (HAT) activity of the transcription co-activators p300 and p300/CREB-binding protein-associated factor (pCAF) with IC50 values of 8.5 and 5 µM, respectively.

Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3.

Anamorelin(RC1291; ONO-7643) is a synthetic orally active ghrelin receptor agonist which is under development for the management of non-small lung cancer associated cachexia/anorexia.

Anastrozole is known to inhibit the CYP19 enzyme (aromatase, IC50 = 15 nM) that converts androgens to estrogens. Anastrozole has been seen to reversibly bind to the CYP19 enzyme through competitive inhibition.

AnCoA4 (AnCoA-4, AnCoA 4) is a potent Orai1 channel inhibitor that inhibits store-operated calcium (SOC) with EC50 of 0.88 uM.

GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity.

Anidulafungin

Anle138b is a novel oligomer modulator.

Maytansinol inhibits microtubule assembly and induces microtubule disassembly in vitro. Target: Microtubule/Tubulin in vitro: Maytansinol disrupts the mitotic spindle and prevents mitotic exit in Drosophila. Maytansinol reduces the growth and/or survival of HCT116 cells in a dose-dependent manner and that the effect was more severe for p53+/+ than for p53-/- cells at both low and high doses. Maytansinol inhibits the growth of HCT116 human colon cancer cells. Maytansinol induces apoptosis in imaginal discs of wild-type larvae but not p53 mutant larvae. This parallels the finding in human HCT116 cells, in which Maytansinol was more effective when p53 was present, at least at some doses. Maytansinol induces apoptosis in imaginal discs of wild-type larvae but not p53 mutant larvae at 24 hours after exposure to drug.

Ansamitocin P-3, a potent anti-tumor maytansinoid found in Actinosynnema pretiosum, is a maytansine analog which displays potent cytotoxicity against the human solid tumor cell lines A-549 and HT-29.

ANT431 is a novel potent metallo-β-lactamase (MBL) inhibitor with IC50 of 290 nM and 195 nM for NDM-1 and VIM-2, shows a comparatively weak inhibitor of VIM-1 and IMP-1 (Ki of 14.6 and 4.15 uM, respectively).

AP1867 is a synthetic FKBP12F36V-directed ligand.

AP1903 (Rimiducid, AP-1903) is a potent, specific synthetic ligand of FKBP Phe36Val mutant (F36V-FKBP) with binding IC50 of 1.8 nM.

AP24534 is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.

ALK-IN-1 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.

Apararenone (MT-3995) is a novel potent, selective non-steroidal mineralocorticoid receptor antagonist for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis..

Apatinib (YN968D1) is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.

Apatinib is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities.

Apcin is a cell-permeable, small molecule anaphase-promoting complex/cyclosome (APC/C) inhibitor, which binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.

APD597(JNJ-38431055) is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.

Apicidin (OSI 2040) is a fungal metabolite that exhibits potent, broad spectrum antiprotozoal activity in vitro, potently inhibits HDAC with IC50 of 0.7 nM in an enzyme activity assay.

Apilimod(STA 5326) is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-r/LPS–stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.

Apilimod(STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-r/LPS–stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.

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.

Aplaviroc, also known as AK-602; GW-873140; GW873140A; ONO-4128, is a CCR5 entry inhibitor for the potential treatment of HIV infection. Aplaviroc (GW873140) binds specifically to human cellular CC chemokine receptor 5 (CCR5) and demonstrates potent anti-human immunodeficiency virus activity in vitro in the subnanomolar range. In vitro studies show that aplaviroc selectively inhibits the binding of a particular monoclonal antibody, 45531, to CCR5.

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

Apomorphine hydrochloride hemihydrate is a non-selective dopamine agonist which activates both D1-likeand D2-like receptors, with some preference for the latter subtypes..

Apoptosis Activator 2 activates caspases in a cytochrome c-dependent manner and induces apoptosis in tumor cells.

Apoptozole is an inhibitor of heat shock protein 70 (Hsp70; 65% inhibition at 200 μM) that acts by blocking its ATPase activity.

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

Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.

APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM

APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM

APS-3-77 is the negative binder of KSR2.

APX001 (APX 001A;E1210) is a novel broad-spectrum antifungal agent that inhibits the fungal protein Gwt1, demonstrates significantly acitive MIC50 and MIC90 values of 0.004 and 0.031 ug/ml (16 strains of C. auris).

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.

APY0201 is a potent, highly selective PIKfyve kinase inhibitor.

APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.

AR231453 is a potent and selective small molecule agonist of GPR119 that enhances glucose-dependent insulin secretion and glucagon-like peptide 1 (GLP-1) release; Antidiabetic agent.

AR7 is a retinoic acid receptor α (RARα) antagonist.

ARA-290 (Cibinetide) is a non-erythropoietic erythropoietin (EPO) derivative.

Ara-G (9-β-D-Arabinofuranosyl guanine) is an inducer of apoptosis, inhibitor of DNA synthesis, an antimetabolite, and antineoplastic.

Umifenovir is currently being investigated as a potential treatment and prophylactic agent for COVID-19 caused by SARS-CoV2 infections in combination with both currently available and investigational HIV therapies. Arbidol hydrochloride (Umifenovir hydroc

Arctigenin is an extract from A. lappa, a burdock plant traditionally used in Japanese Kampo medicine for its antioxidant, anti-inflammatory,

Arctiin, a plant lignan that can be extracted from the Arctium lappa (burdock) seeds, is a possible environmental endocrine disruptor compounds and have been shown to influence sex hormone metabolism as well as protein synthesis, steroid biosynthesis.

Argatroban

Argatroban monohydrate is a direct, selective thrombin inhibitor.

Arg-Gly-Asp-Ser(RGDS peptide) is an integrin binding sequence that inhibits integrin receptor function; decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS

Arglabin is a sesquiterpene gamma-lactone is isolated from Artemisia glabella; anticancer natural compound.

ARM390 is a non-peptidic, low-internalizing δ-selective opioid receptor agonist.

ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ.

ARN-3236 is potent, orally active and selective SIK2 inhibitor. ARN-3236 inhibited the growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μmol/L.

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment.

ARQ 092 is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3).

ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.

ARQ-531 is a potent, reversible, orally available inhibitor of both wild type and C481S-mutant BTK kinase with IC50 of 0.85 and 0.39 nM,

ARRY-520 is a synthetic, small molecule kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM.

ARS-1323 is a novel inhibitor of mutant K-ras G12C.

ARS-1620 is a covalent compound with high potency and selectivity for KRAS-G12C.

ARS-1630 is the R-conformational atropisomer of ARS-1620, 1,000-fold less potent than ARS-1620 (1.2 ± 0.6 M-1s-1) and thus acts as a unique inactive control compound..

ARS-853 is a selective, covalent inhibitor of KRAS-G12C that inhibits mutant KRAS driven signaling by binding to the GDP bound oncoprotein and preventing activation.

ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader with Kd values of 4.7, 7.6, 7.6 nM against bromodomain 2, 3 and 4, respectively.

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.

AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.

AS 8351 induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes, in combination with CHIR 99021, A83-01, BIX 01294, SC1, Y-27632, OAC2, SU 16f and JNJ 10198409.