Acebilustat(ZK322) is a potent and selective leukotriene A4 hydrolase inhibitor.

Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide.

Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.

Acemetacin is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.

Acetaminophen is a COX inhibitor for COX-1 and COX-2 with IC50 of 113.7 μM and 25.8 μM, respectively.

Acetanilide (Antifebrin)

Acetazolamide is a potent carbonic anhydrase (CA) inhibitor; best-studied agent for the amelioration of acute mountain sickness (AMS).

Acetoacetic acid sodium salt is a metabolite of non-esterified fatty acids, involved in the development of human diabetes. Acetoacetic acid sodium salt induces oxidative stress to inhibit the assembly of very low density lipoprotein in bovine hepatocytes.

Acetohydroxamic acid is an Urease Inhibitor. In the urine, it acts as an antagonist of the bacterial enzyme urease.

Acetosyringone is a phenolic compound from wounded plant cells, enables virA gene which encodes a membrane-bound kinase to phosphorylate itself and activate the virG gene product, which stimulates the transcription of other vir genes and itself. Acetosyri

Acetyl Perisesaccharide C is an oligosaccharide, which is isolated from the root barks of Periploca sepium.

Acetylcholine iodide is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.

Acetylspiramycin (ASPM) is a macrolide antimicrobial agent.

Ac-IEPD-CHO is a potent, reversible inhibitor of serine protease Granzyme B (GzmB) with Ki of 80 nM, also inhibits caspase-7 (Ki=550 nM) and induces apoptosis..

Ac-IETD-pNA is a substrate for caspase-8.

Acipimox

Acitazanolast is an active metabolite of tazanolast and anti-allergic drug.

Acitretin

Ack1 inhibitor (R)-9b is a potent and selective ACK1 (TNK2) inhibitor with IC50 of 48 nM.

Ack1 inhibitor 37 is a potent and selective Ack1 (TNK2) inhibitor with Ki of 0.3 nM, displays high selectivity over related kinases LCK, JAK3, KDR and TIE2 (Ki= 138, 6.5, 380 and 200 nM).

Ac-LEHD-pNA is a substrate for caspase-9.1 Caspase-9 preferentially binds to and cleaves the Leu-Glu-His-Asp (LEHD) peptide sequence to release p-nitroalinide, which can be quantified by colorimetric detection at 405 nm as a measure of enzyme activity.

Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD).

ACO1 is a potent, selective Grp94 inhibitor with IC50 of 0.44 uM, displays >200-fold selectivity against other Hsp90 isoforms.

acolbifene, also known as EM-652, or SCH-57068, is a selective estrogen receptor modulator (SERM). Acolbifene is currently being studied in the prevention of breast cancer in women at high risk of breast cancer. EM-652 (SCH 57068) and the prodrug EM-800 (

Acotiamide acts as an acetylcholinesterase inhibitor

ACP-105 is a novel non-steroidal SARM (Selective Androgen Receptor Modulator).

Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.

Acrizanib（LHA510） is a potent and selective angiogenesis inhibitor and VEGFR‑2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.

ACSS2 inhibitor is a novel ACSS2 inhibitor.

ACT 709478 is a potent, selective, orally-bioavailable, brain penetrant T-type calcium channel blocker with IC50 of 6.4, 18, and 7.5 nM for Cav3.1, Cav3.2, and Cav3.3 channels respectively.

ACT-246475 (ACT246475) is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.

ACT-281959 (ACT281959) is the prodrug of ACT-246475, which is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.

ACT-541468 is a dual orexin receptor antagonist.

ACTB-1003 is a potent inhibitor of FGFR1 with IC50 <10 nM in FGFR-1 biochemical assay; more information can be find in Patent WO/2007/064883A2, Example 12.

Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].

Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.

Ac-WEAD-pNA is a colorimetric substrate for caspase-1 and caspase-4.

ACY-738 demonstrates inhibitory activity against recombinant HDAC6 with IC50 values of 1.7 nM, with respective average selectivity over class I HDACs being 100-fold.

ACY-775 (ACY775) is a potent and specific HDAC6 inhibitor (IC50=7.5 nM) with improved brain bioavailability.

ACY-957 (ACY957) is a potent, selective inhibitor of HDAC1 and HDAC2 with IC50 of 7 and 18 nM, shows limited activity against HDAC3 (IC50=1,300 nM) and no activity against HDAC4/5/6/7/8/9 (IC50>20 nM).

Acyclovir (Aciclovir)

AD 2900 (AD2900, AD-2900) is a novel potent, broad S1P receptor antagonist with IC50 of 3.8, 3.2, 6.2, 5.9 and 0.405 uM for S1P1, 2, 3, 4 and 5 respectively.

AD80, a multikinase inhibitor, shows strong activity against human RET, BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.

ADAMTS-5 inhibitor 15f is a highly potent and selective inhibitor of metalloprotease ADAMTS-5 with IC50 of 30 nM, >50-fold selectivity against ADAMTS-4 and >1000-fold selectivity against ADAMTS-1/13, MMP-13 and TACE.

ADAMTS-5 inhibitor 8 is a highly potent and selective inhibitor of metalloprotease ADAMTS-5 with IC50 of 30 nM, >50-fold selectivity against ADAMTS-4 and >1000-fold selectivity against ADAMTS-1/13, MMP-13 and TACE.

Adapalene

Adarotene (ST1926) is an effective apoptosis inducer and surprisingly produced DNA damage.ST1926 exhibites a potent antiproliferative activity on a large panel of human tumor cells. IC50 value: 0.12 uM (LNCaP cell) [1] Target: Apoptosis inducer; Antican

Adavivint (SM-04690, SM 04690, SM04690) is a novel small molecule Wnt pathway inhibitor with EC50 of 3 nM in vitro

ADC-3680 (PTR-36, ADC-3680B) is a potent, selective prostaglandin D2 receptor (DP2, CRTH2) antagonist for the treatment of asthma..

ADC-3680 is a potent, selective prostaglandin D2 receptor (DP2, CRTH2) antagonist for the treatment of asthma..

Adefovir Dipivoxil(Preveon, Hepsera) works by blocking reverse transcriptase, an enzyme that is crucial for the hepatitis B virus (HBV) to reproduce in the body.

Adelmidrol is an anti-inflammatory ethanolamide derivative of azelaic acid.

Ademetionine Disulfate Tosylate is the disulfate-tosylate mixed salt of a mixture of diastereoisomers of the ademetionine ions. Ademetionine possesses anti-inflammatory activity and has been used in treatment of chronic liver disease.

Adenosine (Adenocard)

Adenosine 5'-monophosphate monohydrate (5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK).

Adhesamine is a diaryldispirotripiperazine derivative that selectively targets cell-surface glycosaminoglycans, especially heparan sulfate, for increasing cell adhesion and growth.

Adipamidoxime(NSC 70868) is a new bioactive compoud.

Adiphenine HCl

AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with Kds of 1.8 and 3.1 μM, respectively.

AdipoRon is a novel small-molecule AdipoR agonist; binds to both AdipoR1(Kd= 1.8 uM) and AdipoR2(Kd=3.1 uM).

ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than µ- or κ-opioid receptor with Ki of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid

ADM 12 (ADM_12.

Adoprazine, a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.

Adrenomedullin (AM) (1-52), human (TFA) affects cell proliferation and angiogenesis in cancer.

ADT-094 (ADT094) is a novel, non-COX inhibitory sulindac derivative that potently and selectivity inhibits colon tumor cell growth by inhibiting PDE5 and PDE10 with IC50 of 2.4 uM and 0.5 uM, respectively.

ADT-OH is a derivative of anethole dithiolethione (ADT) and synthetic hydrogen sulfide (H2S) donor.

ADU-S100 (MIW815) is a synthetic cyclic dinucleotide agonist of STING, elicits potent and durable anti-tumor immunity when administered IT in pre-clinical syngeneic tumor models..

ADX-102 (Reproxalap, NS-2) is a novel small molecule immunomodulator that covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal, which have been shown to mediate inflammatory pain; DX-102 is a promising agent for the treatment of dry eye disease.

ADX-47273 is a novel, potent and selective metabotropic glutamate receptor 5 allosteric modulator with an EC50 of 170 nM.

ADX-88178 is a novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4 receptor.

AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.

AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.

AER-271 (AER271) is a selective, small molecule inhibitor of aquaporin-4 (AQP4), the prodrug of AER-270 with enhanced solubility.

AES-135 (AES135) is a novel HDAC inhibitor that biochemically inhibits HDACs 3, 6, 8 and 11 with IC50 values of 190-1100 nM.

AF-2364, an analogue of Lonidamine (LND), had a contraceptive effect when orally administered to adult Sprague–Dawley rats.

AF-353 is a novel, orally bioavailable, highly potent and selective P2X3/P2X2/3 receptor antagonist.

AF38469 is a potent, selective, orally bioavailable Sortilin inhibitor with IC50 of 330 nM, shows no activity against the NTR1 receptor as well as a panel of targets known to bind acidic molecules (δ-Opioid, GPR40, PPARδ, EP1, Angiotensin AT1, Endothelin

AF40431 (AF-40431) is the first reported small-molecule ligand of the VPS10P family sorting receptor Sortilin with IC50 of 4.4 uM, binds in the neurotensin-binding site of sortilin..

AF64394 is a potent, selective GPR3 inverse agonist with pIC50 of 7.3, displays >100-fold selectivity over GPR6 and GPR12.

AF-792 (RO-5) is a novel selective P2X3 and P2X2/3 antagonist with pIC50 of 8.2 and 7.9 respectively, with no inhibition at other P2X receptors.

Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2.

Afegostat D-Tartrate is a pharmacological chaperone, which specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum (ER) with high affinity.

Afloqualone is a agonist of GABA receptor .

AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ≤0.12 μg/ml.

Afoxolaner is an isoxazoline that inhibits insect and acarine ligand-gated chloride channels, in particular those gated by the neurotransmitter gamma-aminobutyric acid (GABA), blocking pre and post synaptic transfer of chloride ions across cell membranes.

Aftin-4, an amyloid forty-two inducer, activates γ-secretase, promoting the generation of amyloid-β-1-42 (Aβ1-42) from amyloid-β protein precursor.

Afuresertib (GSK2110183) is a potent pan-AKT inhibitor that demonstrated synergy with bortezomib in preclinical models of multiple myeloma (MM).

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

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.

AG13958 is a VEGF inhibitor that was clinical development by Pfizer in 2006-07 for treatment of age-related macular degeneration (AMD).

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-24322 is a second generation CDK inhibitor. AG-024322 is a potent inhibitor of CDK1, CDK2, and CDK4 that produces cell-cycle arrest and antitumor activity in preclinical models. The no-adverse-effect dose of AG-024322 was 2 mg/kg and associated with ov

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.

Aganepag is a potent Prostanoid EP2 receptor agonist, with an EC50 of 0.19 nM, and shows no activity at EP4 receptor. Aganepag can be used in the research of wound healing, scar reduction, scar prevention and wrinkle treatment and prevention.

AGI-14100 (AGI14100) is a novel potent and selective, orally available IDH1 mutant inhibitor.

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.

AGL-2263 is an insulin receptor (IR) blocker.

AGN 194310(VTP-194310) is a potent and selective pan-RARs agonist with Kd values of 3/2/5 nM for RARα/β/γ respectively.

AGN 210676 is a selective prostaglandin EP2 agonist extracted from patent US20070203222A1, Compound example 23, has an EC50 of 5 nM.

AGN192836 (AGN 192836) is a potent, selective α2 adrenergic (alpha 2-adrenoceptor) agonist with EC50 of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.

Agomelatine is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.

AGPS-IN-1a is a potent inhibitor of the ether lipid-generating enzyme alkyl-glycerone phosphate synthase (AGPS), selectively lowers ether lipid levels in several types of human cancer cells and impairs their cellular survival and migration..

AgrA inhibitor F19 is a small-molecule AgrA inhibitor that act as antivirulence agent against Gram-positive pathogens, blocks staphylococcal transcription factor AgrA from binding to its promoter and inhibits toxin and virulence factor transcription.

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.

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

AJM300 (AJM 300, AJM-300) is a novel potent, selective, oraaly available alpha 4 integrin antagonist fortreatment of active ulcerative colitis..

AK106-001616 (AK 106-001616) is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2) with IC50 of 3.8 nM (human cPLA2 enzyme).

AK306 is a small molecule clathrin heavy chain (CLTC/CHC) binding compound that induces arrest and apoptosis of the HCT116 colon cancer cell line with EC50 of 50 nM.

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.

AKR1C3 inhibitor KV-37 is a potent, isoform selective and metabolically stable inhibitor of Aldo-keto reductase 1C3 (AKR1C3) with IC50 of 66 nM, displays 109-fold selectivity over AKR1C2.

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).

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50 = 3.5 nM) and Akt2 (IC50 = 42 nM), with potent and balanced activity.

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.

AL-9 is a small molecule HCV replication inhibitor with EC50 of 0.29 and 0.75 uM for genotype 1b and 2a, inhibits purified PI4KIIIα with IC50 of 0.57 uM.

ALB-127158 is a potent (IC50=7 nM), selective, non-peptide antagonist of MCHR1 (Melanin-concentrating hormone receptor 1) for treatment of obesity..

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

Albendazole(Albenza)

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

Alcaftadine

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).

ALDH1A inhibitor 673A (ALDH1Ai 673A) is a potent, selective, pan-ALDH1A inhibitor with IC50 of 246, 230 and 348 nM for ALDH1A1, ALDH1A2 and ALDH1A3, respectively.

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.

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.

Alendronate (Fosamax)

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..

Alfuzosin is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).

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.

Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD).

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

Alizapride (MS 5080) is a dopamine D2 antagonist with prokinetic and antiemetic effects used in the treatment of nausea and vomiting..

Alizapride (MS 5080) is a dopamine D2 antagonist with prokinetic and antiemetic effects used in the treatment of nausea and vomiting..

Alizarin has a selective and effective inhibitory activity towards cancerous cells, it acts through the inhibition of ERK phosphorylation and cell cycle arrest in the S-phase.

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.

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

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.

Alloepipregnanolone, a pregnane with anesthetic, hypnotic, and sedative properties, interferes with the development of rapid tolerance to the anxiolytic effect of ethanol.

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

Allopurinol (Zyloprim) is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 μM.

Allopurinol riboside, a metabolite of allopurinol, shows potent activities against parasites.

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].

Alloxazine is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor.

all-trans-4-Oxoretinoic acid, an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).

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

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

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

Alosetron Hydrochloride is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.

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.

Alprazolam (D-65MT, U 31889) is a triazolobenzodiazepine agent with anxiolytic, sedative-hypnotic and anticonvulsant 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.

ALS-8112 is a potent, selective RSV polymerase inhibitor, the 5'-triphosphate of ALS-8112 (ALS-8112-TP) inhibits RSV polymerase(IC50=20 nM) without appreciable inhibition of human DNA and RNA polymerases.

ALS-8176 (Lumicitabine) is the 3',5'-di-O-isobutyryl prodrug of ALS-8112 5'-triphosphate (ALS-8112-TP), which is a potent, selective RSV polymerase inhibitor with IC50 of 20 nM.

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.

Altretamine (Hexalen)

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

Alverine citrate is a drug used for functional gastrointestinal disorders.

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

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

ALW-II-49-7 (DDR2-IN-1) is a potent, selective DDR2 inhibitor with IC50 of 18.6 nM, also shows ability to inhibit DDR1 and Ephrin-family kinases (IC50=40 nM for EphB2).

ALX-1393 (ALX 1393, ALX1393) is a potent, specific GlyT2 inhibitor with Ki of <1 uM.

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 432 is potent, selective, orally active prostaglandin D2 receptor (DP2/CRTH2) antagonist with binding IC50 of 6 nM for hDP2.