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

A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 260 nM.

SW106 is a potent, selective, competitive PTH/PTH-related peptide receptor (PPR) antagonist with IC50 of 0.99 uM.

A potent, selective, noncompetitive inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) with IC50 of 7 uM.

A potent, selective, non-pseudosubstrate inhibitor of O(6) -alkylguanine DNA methyltransferase (MGMT) with low-nanomolar potency.

A potent, selective, non-RGD-mimetic αIIbβ3 integrin receptor antagonist with IC50 of 45 nM, with no activity on αVβ3 receptors. .

A potent, selective, orally active cannabinoid CB2 receptor inverse agonist with Ki of 35.9, 1.55 and 0.38 nM for human, mouse and rat CB2, respectively.

A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM.

PF-1355 is a potent, selective, orally active Myeloperoxidase (MPO) inhibitor with EC50 of 1.47 uM.

A potent, selective, orally active neurokinin 3 (NK3R) antagonist for the treatment of schizophrenia.

Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

A potent, selective, orally active S1P1 antagonist with IC50 of 2.5 nM Ca2+ mobilization assays, without activity on S1P2, S1P3 and S1P4 (IC50>10 uM).

A potent, selective, orally active TRPA1 channel antagonist with IC50 of 71 and 131 nM for rTRPA1 and hTRPA1 in Ca2+ flux assays respectively, without agonist activity (EC50>40 uM).

PF-0346275 is a potent, selective, orally available GlyT1 inhibitor with Ki of 11.6 nM, without activity against GlyT2 (IC50>10 uM).

A potent, selective, orally available inhibitor of both native and mutant Bcr-Abl with IC50 of 20-80 nM.

Avacopan is a potent, selective, orally availale C5aR (CD88) inhibitor with IC50 of 0.1 nM.

JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.

A potent, selective, orally bioavailable inhibitor of class I PI3K isoforms with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/β/δ/γ, respectively.

A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1.

SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.

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

SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist.

A potent, specific acyl protein thioesterase 2 (APT-2, LYPLA2) inhibitor with IC50 of 144 nM and Ki of 120 nM, >20-fold selectivity over APT-1 and serine hydrolase enzyme family.

A potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM).

A potent, specific and orally active 5-Lipoxygenase-activating protein (FLAP) inhibitor with IC50 of 1.6 nM in FLAP binding assay.

VU 0465350 is a potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 92.3 nM; shows no activity for ALK2/4/5, also shows affinity for TGFBR2, VEGFR2 and AMPK; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.

A potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays.

A potent, specific inhibitor of HCV NS5B polymerase and HCV replication (IC50=1.28 uM, replicon assay).

MMV019313 (MMV 019313, MMV-019313) is a potent, specific malaria bifunctional farnesyl/geranylgeranyl diphosphate synthase (FPPS/GGPPS) inhibitor with IC50 of 330 nM; shows no activity against human FPPS or GGPPS (>200 uM); exhibits distinct modes of inhibition compared with bisphosphonates, inhibits P. falciparum growth with EC50 of 268 nM, overexpression and an S228T variant of PfFPPS/GGPPS confer resistance to MMV 019313.

A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM.

A potent, specific, allosteric inhibitor of KSP motor domain ATPase with Ki of 12 nM.

A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM

A potent, specific, orally active melanin concentrating hormone receptor 1 (MCHR1) inhibitor with kI of 3.8 nM, >100-fold selectivity over a battery of GPCRs, ion channels and enzymes.

A potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.

Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity. At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Pasireotide acetate) usually boasts enhanced water solubility and stability.

NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.

A proton pump inhibitor that reduces stomach acid secretion by inhibition of the H+/K+-ATPase in the parietal cells.

IPAG is a prototypic selective inhibitor of sigma1 receptor that engages the unfolded protein response and induces autophagy in cancer cells.

A PSMA (prostate-​specific membrane antigen) ligand-​tubulysin compound..

A pyrimidine analog reverse transcriptase inhibitor (NRTI) for the treatment of HIV/AIDS.

A retinoic acid analog and selective RARα agonist

A selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2).

K-7174 dihydrochloride is a selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2).

Capadenoson is a selective agonist of adenosine-A1 receptor.

MG624 is a potent and selective neuronal α7 nAChR antagonist with a Ki of 106 nM.

A selective GPR68 positive allosteric modulator (pEC50=6.83) with minimal PAM activity at the related proton-sensing GPCRs GPR4 and GPR65.

SR-11237 is a selective pan retinoid X receptor (RXR) agonist with no retinoid A receptor (RAR) activity. .

A selective prostaglandin E receptor subtype 4 (EP4) antagonist with pKi of 8.5.

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

A selective TRPM8 channel blocker with pEC50 of 6.91 in Ca(2+) influx assay, with no activity for TRPV4 (pEC50<4.6).

A selective Δ6 desaturase inhibitor that displays selectivity over Δ5 and Δ9 desaturases

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

A serine protease inhibitor that inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM).

A small molecule binds to the EXO70 (exocyst component of 70 kDa) subunit of the exocyst complex (Kd=253 uM), resulting in inhibition of exocytosis and endosomal recycling in both plant and human cells and enhancement of plant vacuolar trafficking..

A small molecule compound of prostaglandin D2（PGD2) inhibitor.

A small molecule corrector of ΔF508-CFTR with IC50 of 6.0 uM..

A small molecule inhibitor (IC50=0.3 uM) of DEAD-box polypeptide 3 (DDX3), a human host factor required for the replication of several DNA and RNA viruses.

A small molecule inhibitor of clathrin terminal domain and inhibits clathrin-mediated endocytosis.

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 0.01-10 uM in isolated platelet membranes and in intact platelets.

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM, inhibits the phosphorylation of OAG to OAPA with IC50 of 3.8 uM in intact platelets.

A small molecule inhibitor of PP2C that activates extensive 3' cleavage at a concentration 50-fold below that required by fluoride or CP..

A small molecule inhibitor of PSD-95/nNOS interaction with IC50 of 31 uM, without inhibiting nNOS catalytic activity.

A small molecule inhibitor of the NF-κB family member c-Rel with IC50 of 3 uM in EMSA assays.

A small molecule inhibitor of trans-translation that has broad-spectrum antibiotic activity.

Filastatin is a long-lasting inhibitor of Candida albicans filamentation. Filastatin inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 μM in the GFP-based adhesion assay. Filastatin inhibits fungal adhesion to polystyrene and human cells, the yeast-to-hyphal morphological transition, induction of the hyphal-specific HWP1 promoter. Filastatin has potent antifungal effect.

Navoximod (GDC-0919; NLG-​919) is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM.

PDI inhibitor 16F16 is a protein disulfide isomerase (PDI) inhibitor, first identified in a screen for compounds that prevent apoptosis induced by mutant huntingtin protein. 16F16 not only suppressed apoptosis induced by the misfolded protein mutant hungtingtin, it also protected rat neurons from cell death triggered by Aβ peptide. The actions of this inhibitor helped to identify a new mechanism in which a cell death pathway is regulated by protein misfolding via PDI upregulation.

A small molecule Skp2 E3 ligase inhibitor that prevents Skp2-Skp1 interaction and Skp2 SCF E3 ligase activity in vitro.

A small molecule TAAR1 agonist and β adrenoreceptor agonist that stimulates β1 and β2 adrenergic receptors.

A small molecule that inhibits NFATc1 and NF-κB activity, inhibits RANKL-induced osteoclastogenesis in vivo.

NSC243928(NSC-243928 ) is a small molecule that potently inhibit ovarian cancer stem-like cells (CSC) growth with GI50 of 0.83 uM, which os consistent with cell death/apoptosis..

A small molecule that promotes differentiation of iPS-derived hepatocytes.

A small-molecule compound that disrupts the Golgi apparatus by inhibiting the activation of ADP-ribosylation factor 1 (ARF1).

OB-1 is a small-molecule inhibitor of STOML3 oligomerization that reverses pathological mechanical hypersensitivity in vivo; effectively inhibits the self-association of stomatin, STOML1 and STOML2 at 2 uM, but not podocin; reversibly reduces the sensitiv

A small-molecule probe that selectively kills cells induced to express mutant RAS.

A small-molecule probe that selectively kills cells induced to express mutant RAS.

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.

A sodium channel inhibitor..

PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]

A specific inhibitor of MDA-9/Syntenin activity that inhibits MDA-9/Syntenin binding to EGFRvIII.

A specific inhibitor of mitochondrial Na(+)-Ca(2+) exchanger (mNCE) with IC50 of 1.5 uM in INS-1 cells.

A stable, orally active, non-prostanoid prostacyclin I2 (PGI2) mimetic and prostacyclin agonist with inhibitory activity against thromboxane A2 synthase.

A synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities.

A synthetic benzylamine antifungal that inhibits the synthesis of ergosterol by inhibiting squalene epoxidase.

A synthetic curcuminoid that selectively inhibits STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs.

A thienopyridine-class antiplatelet agent that works by irreversibly inhibiting P2Y12 receptor on platelets.

A thiosemicarbazone that is used in association with other antimycobacterial agents in the initial and continuation phases of antituberculosis regimens. Thiacetazone containing regimens are less effective than the short-course regimen recommended by the I

A toxic byproduct, iminoquinone metabolite of acetaminophen that covalently binds to the active site of MIF.

A triazole antifungal agent that blocks the synthesis of ergosterol by inhibiting of the enzyme lanosterol 14α-demethylase and accumulation of methylated sterol precursors, more potent at inhibiting 14α-demethylase than itraconazole..

A Tyrosine kinase inhibitor.

A VHL ligand for PROTAC..

A xanthone derivative that fuctions as an EP and DP receptor antagonist.

A-1155463 is a highly potent and selective BCL-XL inhibitor.

A-1210477 is a potent and selective MCL-1 inhibitor.

A-1331852 is a high affinity BH3 mimetic Ligand of BCL protein BCL-XL.

A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells).

A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines.

A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.

A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM).

A-381393 is a potent and selective agonist of the dopamine D4 receptor.

A-395 potently inhibited the formation of H3K27me3 (via antagonizing EED in the trimeric PRC2 complex (EZH2:EED:SUZ12)) with IC50 = 34 ± 2 nM (Hill Slope = 0.7)

A-420983 is a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.

A4250 (A-4250, Odevixibat) is a small molecule ileal bile acid transporter (IBAT) inhibitor for the treatment of cholestatic liver diseases including progressive familial intrahepatic cholestasis and NASH..

A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.

A-674563 is a potent, orally available Akt1 inhibitor with an IC50 value of 11nM. Also displays activity against PKA and CDK2 with IC50 values of 16nM and 46nM respectively.

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM, little effect on GPPase/FBPase activity.

A-779 is a peptide antagonist of the Mas receptor, also known as the angiotensin (1-7) (Ang (1-7)) receptor (IC50 = 0.3 nM in a radioligand binding assay).

A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM.

A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.

A83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively).

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

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.

AA 41612 is a potent, synthetic melanopsin antagonist with IC50 of 15.8 nM, attenuates melanopsin photocurrent in a dose-dependent manner.

AA-115 (APG 115) is a potent and orally active MDM2 inhibitor with Ki <1 nM, potently inhibits SJSA-1 cell growth with IC50 of 60 nM.

ATF6 agonist compound A147 is a specific, small molecule agonist of transcription factor ATF6, activates ATF6 and influences differentiation of stem cells.147 has broad antiviral activity against multiple DENV strains and serotypes and that the compound i

AA26-9 is a potent and broad spectrum serine hydrolase inhibitor.

AAI-101 is a novel extended-spectrum β-lactamase inhibitor with activity against many β-lactamases, including some class A and class D carbapenemases.

AAL993 (ZK260253) is a potent, orally active VEGFR inhibitor with IC50 of 130, 23 and 18 nM for VEGFR-1, 2 and 3, respectively.

AB-423 is the first-generation Hepatitis B Virus Capsid Assembly inhibitor, which was generally safe and well tolerated in Phase 1 healthy volunteer studies.

AB680 (AB-680) is a highly potent, selective, reversible inhibitor of CD73 with Ki/IC50 of 4.9/70 pM (hCD73), displays > 10,000-fold selectivity against related ecto-nucleotidases (CD39, NTPDases 2/3/8) and a large panel of unrelated enzymes, receptors, a

Abametapir is the active ingredient of Xeglyze Lotion.

ABBV-744 is a BDII-selective BET bromodomain inhibitor that is being investigated to treat AML and metastic castration-resistant prostate cancer.BBV-744, a highly potent and selective inhibitor of the BD2 domain of BET family proteins with drug-like properties. In contrast to the broad range of cell growth inhibition induced by DbBi, the antiproliferative activity of ABBV-744 was largely, but not exclusively, restricted to cell lines of acute myeloid leukaemia and prostate cancer that expressed the full-length androgen receptor (AR). ABBV-744 retained robust activity in prostate cancer xenografts, and showed fewer platelet and gastrointestinal toxicities than the DbBi ABBV-07514.Analyses of RNA expression and chromatin immunoprecipitation followed by sequencing revealed that ABBV-744 displaced BRD4 from AR-containing super-enhancers and inhibited AR-dependent transcription, with less impact on global transcription compared with ABBV-075. These results underscore the potential value of selectively targeting the BD2 domain of BET family proteins for cancer therapy.

ABC1183 is a potent, selective, orally active GSK3α/β and CDK9 inhibitor with IC50 of 327/657 nM and 321 nM (CDK9/cyclin T1), shows growth inhibitory activity against a broad panel of cancer cell lines; decreases cell survival through G2/M arrest and modu

ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity.

Abiraterone (D4A) is an active metabolite of the CYP17A1 inhibitor abiraterone.

ABL127 (ML174) is a potent, selective, covalent inhibitor of protein methylesterase 1 (PME-1) with IC50 of 10 nM.

AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.

ABT-199 is a Bcl-2-selective inhibitor with Ki < 0.010 nM.

ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤ 1 nM, respectively.

ABT-333 is an NS5B non-nucleoside polymerase inhibitor.

ABT-594 represents a novel class of broad-spectrum analgesics whose primary mechanism of action is activation of the neuronal nicotinic acetylcholine receptors.

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker. ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50 = 2 μM) and attenuates LVA currents in rat DRG neurons (IC50 = 8 μM).

ABT-702 is a potent non-nucleoside adenosine kinase inhibitor (IC50 = 1.7 nM), selective over other sites of adenosine interaction (A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase).

ABT-719 is a potent bacterial DNA gyrase inhibitor.

ABT-719 is a potent bacterial DNA gyrase inhibitor.

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM, respectively.

ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.

ABT-869 is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (VEGF) and platelet derived growth factor (PDGF) receptor families.

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).

ABX464 (ABX-464, ABX 464) is a novel class of anti-HIV small molecule targeting Rev-mediated viral RNA biogenesis, shows dose dependent inhibition of HIV-1 replication in stimulated PBMCs with IC50 of 0.1-0.5 uM.

AC 55541 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 6.7) that displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation.

AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.

AC-263093 (AC263093) is a potent, functionally selective neuropeptide FF receptor type 2 (NPFFR2) agonist with pKi of 6.9.

AC264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). Displays no activity at other PAR subtypes and exhibits no significant activity at over 30 other receptors implicated in nociception and inflammation.

AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.

AC710, is a potent Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases.

ACA is a cell permeable inhibitor of PLA2,reported to inhibit α-ketoisocaproic acid and glyceraldehyde-induced insulin secretion, as well as glucose-induced insulin secretion.

Acacetin is an O-methylated flavone found in Robinia pseudoacacia (black locust), Turnera diffusa (damiana),Betula pendula (silver birch),and in the fern Asplenium normale.

Acadesine results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3.

Acalabrutinib (ACP-196) is a second-generation, selective, irreversible inhibitor of BTK.

Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM.

Acarbose is the first identified α-glucosidase inhibitor.

Ac-DEVD-pNA is a colorimetric substrate for caspase-3 (CPP32) (Km=9.7μM) and related cysteine proteases.

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.

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

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

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

Acotiamide acts as an acetylcholinesterase inhibitor

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

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-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.

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.

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

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.

Adipamidoxime(NSC 70868) is a new bioactive compoud.

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

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

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

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

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.