A novel human RBC Cl-conductance blocker (IC50=210 nM) and HERG channel activitor (EC50=79.4 uM, HERG1 channel activation).

A novel hypoxia-sensitive fluorescent probe.

A novel isocitrate lyase (ICL) inhibitor that displays showed excellent anti-Mycobacterium tuberculosisl activities and low cytotoxicity.

A novel LTA4 hydrolase (LTA4H) inhibitor that inhibits LTB4 synthesis in human neutrophils with IC50 of 0.5 uM.

A novel lysosomotropic REV-ERB ligand that has a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy.

A novel melatonin melatonin receptor MT1/MT2 and serotonin 5-HT1A/5-HT1D receptor agonist.

A novel microtubule inhibitor, downregulates T315I mutant Bcr-Abl and induces apoptosis of imatinib-resistant chronic myeloid leukemia cells.

A novel microtubule targeting agent that induces apoptosis, upregulates death receptors, and potentiates TRAIL-mediated apoptosis in multiple cancer cells.

A novel mineralocorticoid receptor antagonist (IC50=0.26 uM) with carbonic anhydrase inhibitory activity (IC50=19 uM).

A novel mitochondrial and mTOR inhibitor with potent anti-cancer activity, inhibits leukemia cell lines with IC50 of 70-260 nM.

A novel MPT (mitochondrial permeability transition) inhibitor of that inhibits Ca2+-induced MPT in rat liver isolated mitochondria.

A novel negative allosteric modulator of dofetilide binding to the Kv11.1 (hERG) channel with the strongest effect at 10 uM (IC50=3.9 uM).

A novel Non-competitive AMPA/kainate antagonist.

A novel nonpeptidic inhibitor of 14-3-3 protein-protein interaction that promotes the apoptotic death of cells expressing either wt Bcr-Abl construct or T315I mutation.

A novel Notch inhibitor that reduces protein expression of NOTCH1, NICD and HES1 in HEK293 cells and downregulates Notch target genes.

A novel orally active, anti-inflammatory compound that inhibits leukocyte infiltration and changes in lung function in response to allergen challenge.

A novel orally available, synthetic retinoid with potential antineoplastic and chemopreventive activities.

A novel orally bioavailable fungal beta-1,3-D glucan synthetase inhibitor against Candida species C. glabrata (MIC 0.03 to 0.25 ug/ml), C. parapsilosis (MIC 0.06 to 0.25 ug/ml).

A novel peptidic, potent and highly selective CXCR4 antagonist with IC50 of 1.7 nM.

A novel platelet inhibitor

A novel potent "funny" If current channel (If channel) inhibitor that inhibits rOct1- and hOCT1-mediated [3H]MPP uptake with IC50 of 23.8 and 40.5 uM, respectively.

A novel potent (IC50=910 ng/mL), highly selective microsomal prostaglandin E synthase 1 inhibitor (mPGES-1) for treatment of undisclosed indications..

A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM.

A novel potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 4.83 nM, dispalys >300-fold selectivity over p38α.

A novel potent and selective, orally active URAT1 inhibitor with Ki of 57 nM, 130 and 42-fold selectivity over OAT1 and OAT3, respectively.

A novel potent Aurora kinase inhibitor that inhibits Aurora-A and Aurora-B with IC50 of 24 nM and 45 nM, respectively.

A novel potent bitter receptor (TAS2Rs) antagonist that inhibits activation of hTAS2R31 by saccharin and acesulfame K with IC50 of 6.4 and 7.9 uM respectively.

A novel potent cannabinoid receptor agonist..

A novel potent cdc2-like kinase (CLKs) and DYRKs inhibitor with IC50 of 40, 35 and 15 nM for DYRK1A, DYRK2 and CLK1, respectively.

A novel potent CDK inhibitor with IC50 of 79 nM, 63 nM and 20 nM for Cdk4/cyclin D1, Cdk1/cyclin B and Cdk9/cyclin T1, respectively.

A novel potent CFTR potentiator that blocks hCFTR with apparent Kd of 71.3 uM.

A novel potent CFTR potentiator with Kd of 31.7 nM.

ZINC 39395747 is a novel potent derivative of propylthiouracil that functions as a cell-active inhibitor of cytochrome b5 reductase 3 (CYB5R3) with IC50 of 9.14 uM.

A novel potent DNA-intercalating payload dimer (PBD dimer) payload for antibody-drug conjugates (ADCs).

A novel potent gonadotrophin releasing hormone (GnRH) antagonist..

A novel potent gonadotrophin releasing hormone (GnRH) antagonist..

A novel potent LIMK inhibitor with IC50 of 0.3 nM and 1 nM for LIMK1 and LIMK2, respectively.

A novel potent LIMK inhibitor with IC50 of 8 nM and 32 nM for LIMK1 and LIMK2, respectively.

A novel potent MAP3K14 kinase inhibitor with IC50 of 1.8 nM (NIK autophosphorylation).

A novel potent proton pump inhibitor that irreversibly inhibits H+,K+-ATPase activity with IC50 of 0.28 uM.

A novel potent small-molecule BET bromodomain (BRD) inhibitor that binds to BET proteins with Ki values of <1 nM.

A novel potent soluble guanylate cyclase (sGC) activator.

A novel potent specific histone acetyltransferaseTip60 inhibitor.

A novel potent specific histone acetyltransferaseTip60 inhibitor.

A novel potent TOPK inhibitor that effectively suppresses SUV-induced activation of MAPKs signal transduction resulting in reduced SUV-induced skin carcinogenesis.

A novel potent ULK1 inhibitor with IC50 of 11 nM..

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.

A novel potent, allosteric, simultaneously direct activator and inhibitor of AMPK complexes containing the β1 or β2 isoform, respectively.

A novel potent, and selective prostaglandin EP4 receptor antagonist with binding IC50 of 2.4 nM.

A novel potent, combined serotonin 5-HT1A and 5-HT1B receptor antagonist with Ki of 0.13 and 2.4 nM in brain homogenates, respectively.

A novel potent, competitive squalene synthase inhibitor that upregulate the LDLR in mouse and human liver cell lines with EC50 of 26 nM.

A novel potent, highly selective fatty acid amide hydrolase (FAAH) inhibitor with IC50 of 0.99, 1.65 and 57.3 nM for human FAAH-1, FAAH-1 (P129T) and FAAH-2, respectively.

A novel potent, highly selective, ATP-competitive IKK-2 inhibitor with IC50 of 40 nM, 350-fold selectivity over IKK-1.

A novel potent, in vivo-active BCL6 inhibitor with IC50 of 0.1 uM in ELISA assays.

A novel potent, irreversible and orally active inhibitor of steroid sulfatase (STS) with IC50 of 13 nM in ZR-75-1 cells.

A novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM.

A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 6.2, 3.4 and 4.2 nM for L858R-T790M, T790M and Del19-T790M, respectively.

A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 8.3, 4.2 and 4.3 nM for L858R-T790M, T790M and Del19-T790M, respectively.

A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively.

A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively.

A novel potent, non-agonist PPARγ ligand that blocks CDK5-mediated PPARγ phosphorylation, without the classical agonism.

SR-1664 is a novel potent, non-agonist PPARγ ligand that blocks the Cdk5-mediated phosphorylation in vitro (IC50=80 nM) and in vivo, without the classical agonism.

A novel potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 of 2 uM.

A novel potent, orally active CCK-2/gastrin receptor antagonist with Ki of 0.47 nM.

A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.

A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.

A novel potent, orally active proton pump inhibitor that irreversibly inhibits H+,K+-ATPase activity with IC50 of 0.28 uM.

A novel potent, orally active, dual-acting aromatase and steroid sulfatase (STS) inhibitor with ICI0 of 0.82 nM and 39 nM, respectively.

A novel potent, pan-AMPK activator with similar potency for all AMPK heterotrimers.

A novel potent, partial LXRβ-selective agonist (EC50=9 nM) with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays.

A novel potent, selective and orally active ASK1 (MAP3K5) inhibitor with pIC50 of 8.3.

A novel potent, selective and orally active enterocytic microsomal triglyceride transfer protein (MTP) inhibitor that inhibits only MTP localized to enterocytes with IC50 of 6 nM.

A novel potent, selective and reversible dual inhibitor of G9a/DNMTs with IC50 of 16 nM and 32 nM for G9a and DNMT1, respectively.

A novel potent, selective cannabinoid receptor 2 (CB2) agonist with Ki of 12 nM, >30-fold selectivity over CB1.

A novel potent, selective CDK8 inhibitor with IC50 of 0.5 uM against recombinant Cyclin C/CDK8 complex.

A novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2.

A novel potent, selective CXCR2 inhibitor with IC50 of 0.4 nM.

A novel potent, selective CXCR2 inhibitor with IC50 of 7.6 nM.

9-ING-41 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor[1]. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity[2].

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 hERG potassium channel (Kv11.1) activator that induces a leftward shift in the voltage dependence of activation..

A novel potent, selective HIV non-nucleoside reverse transcriptase inhibitor (NNRTI) with EC50 of 1, 1.3, 2.8 and 11 nM for WT, K103N, Y181C and K103N/Y181C, respectively.

A novel potent, selective inhibitor of phosphorylation and transcriptional activity of STAT5, but not STAT3, AKT, or Erk1/2 phosphorylation.

A novel potent, selective IRAK4 inhibitor with IC50 of 51 nM.

A novel potent, selective KCNQ2/Q3 (Kv7.2/Kv7.3) potassium channel opener/activator with EC50 of 0.38 uM..

A novel potent, selective Kv2 channel inhibitor that potently inhibits Kv2.1 and Kv2.2 with IC50 of 0.14 and 0.09 uM, respectively.

A novel potent, selective Kv2 channel inhibitor that potently inhibits Kv2.1 and Kv2.2 with IC50 of 0.14 and 0.09 uM, respectively.

A novel potent, selective Kv2 channel inhibitor that potently inhibits Kv2.1 and Kv2.2 with IC50 of 0.14 and 0.09 uM, respectively.

A novel potent, selective Mcl-1 inhibitor with IC50 of <3 nM in FRET assays.

A novel potent, selective mGluR2 positive allosteric modulator with EC50 of 199 and 206 nM for human and rat mGlu2, respectively, without exerting agonist activity.

A novel potent, selective monoamine oxidase B (MAO-B) inhibitor with IC50 of 29-56 nM.

A novel potent, selective mTOR inhibitor with biochemical IC50 of 21.7 nM for mTORC1, exhibits cellular potency against mTOR with IC50 of 5 nM.

A novel potent, selective Nrf2 activator with pEC50 of 7.7 (inducing of NQO1 specific enzyme activity).

A novel potent, selective orally bioavailable MET tyrosine kinase inhibitor with IC50 of <1 nM and 12 nM for unphosphorylated and phosphorylaed MET, respectively.

A novel potent, selective PDE1 inhibitor with IC50 of 13/45/1.4 nM for PDE1A/B/C, respectively.

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 Sirt2 inhibitor with IC50 of 0.118 uM.

A novel potent, selective TBK1 PROTAC with DC50 of 12 nM, selectively degrades TBK1 with excellent selectivity against a related kinase IKKε.

A novel potent, selective TRPM8 antagonist with IC50 of 15.6 nM (hTRPM8).

A novel potent, selective TRPM8 channel antagonist with IC50 of 10 and 21 nM in hTRPM8 HEK293 cells activated by Cooling Agent 10 or cold.

A novel potent, selective Y4R positive allosteric modulator (EC50=5.1 uM) that potentiates Y4R activation in G-protein signaling and arrestin3 recruitment experiments.

A novel potent, selective, allosteric and orally active dopamine D1 receptor potentiator with Kb of 26 nM.

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, cell permeable and ATP competitive LIMK inhibitor.

A novel potent, selective, competitive and orally active DPP4 inhibitor with potential for the treatment of type 2 diabetes.

A novel potent, selective, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1β, regulates cytokine production through PIKfyve-c-Rel pathway ( IL-12p40 IC50=2 nM).

A novel potent, selective, orally active aldosterone synthase inhibitor with IC50 of 2 nM, displays 150-fold selectivity over related cortisol synthase.

A novel potent, selective, orally active CBP/p300 bromodomain with IC50 of 1.0 nM.

A novel potent, selective, orally active nociceptin/orphanin FQ peptide (NOP, ORL1) receptor agonist with Ki of 4.6 nM, with high selectiivity over classical opioid receptors.

A novel potent, selective, orally active translocator protein 18 kDa (TSPO/PBR) antagonist with Ki of 0.33-9.3 nM for both rat and human TSPO.

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

A novel potent, selective, orally available PI3Kδ inhibitor with IC50 of 31 nM.

A novel potent, selective, orally bioavailable and brain-penetran α7nAChR positive allosteric modulator with EC50 of 60 nM.

A novel potent, selective, orally bioavailable inhibitor of voltage-gated potassium channel KCNH3 with IC50 of 9.0 nM.

LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.

A novel potent, selective, reversible cyclooxygenase-1 (COX-1) inhibitor with IC50 of 4.9 nM.

A novel potent, slow tight binding LPA1 receptor antagonist with IC50 of 86 nM, Kd of 0.34 nM.

A novel potent, specific TOPK inhibitor that has no effect on ERK1, JNK1, or p38 kinase activity.

A novel potent, specific, covalent USP7 inhibitor with Kd of 7.8 uM (USP7 catalytic domain).

A novel potent, specific, orally available GPR40 agonist that influences glucose-dependent insulin secretion both in vitro pancreas β-cell-derived cells and in vivo.

A novel potent, subtype-selective sigma 2 receptor/PGRMC1 ligand with Ki of 16.2 nM, 574-fold selectivity over sigma 1 receptors..

A novel potent, subtype-selective sigma 2 receptor/PGRMC1 ligand with Ki of 61 nM, 9-fold selectivity over sigma 1 receptors (Ki=556 nM).

A novel powdery mildew (Erysiphe necator) fungicide that shows protectant and post-infective activities. .

A novel prodrug S1P receptor modulator lacking S1P3 receptor agonism to avoid bradycardia associated with fingolimod and other S1P receptor modulators.

A novel protein kinase affinity probe...

A novel P-selectin inhibitor that directly binds to P-selectin.

SLMP53-1 is a novel reactivator of wild-type and mutant p53, shows a p53-dependent anti-proliferative activity in human wt and mut p53R280K-expressing tumor cells.

A novel SAM-competitive, highly selective, orally bioavailable EZH1/2 dual inhibitor with IC50 of 16/50 nM, respectively.

A novel selective small molecule inhibitor of PDE6δ/KRas interaction with Kd of 358 pM..

A novel selective small molecule Rac1 inhibitor that blocks Rac1-PAK1 complex formation with IC50 of 88±48 nM.

A novel selective small molecule Rac1 inhibitor that blocks Rac1-PAK1 complex formation with IC50 of 95±21 nM.

A novel selective STAT3 inhibitor that inhibits JAK2-STAT3 activation but has no effects on other transcription factors such as NF-κB, and kinases such as AKT, ERK, and c-Src.

A novel selective STAT3 inhibitor with IC50 of 4.2 uM, does not inhibit STAT1, STAT5, or NFkB signaling pathways (IC50>50 uM).

A novel selective, small molecule large-conductance Ca(2+)-activated K(+) channel (BKCa, KCa1.1, MaxiK) positive modulator with EC50 of 11 uM.

A novel selective, small-molecule inhibitor of sirtuin SITR2 with IC50 of 21.8 uM.

A novel SirReal-based PROTAC that induces isotype-selective Sirt2 degradation (IC50=0.25 uM)..

A novel small molecule activator of Kv 11.1 (hERG) channel (216% over control at 3 uM for hERG1a activation).

A novel small molecule ALDH inhibitor with IC50 of 600 nM, 800 nM and 1000 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively.

AKI-603 is a novel small molecule Aurora A kinase inhibitor with IC50 of 12.3 nM, also inhibits Aurora B kinase activity to a less extent; disrupts normal spindle structure, and induces cell-cycle arrest; t; suppresses stem cell properties in breast cancer cells, and also suppresses the expression of self-renewal genes (β-catenin, c-Myc, Sox2, and Oct4); reduces xenograft tumor growth after intragastric administration.

A novel small molecule disruptor of HuR-mRNA interaction with Ki of 350 nM.

A novel small molecule inducer of heme oxygenase-1 that protect human iPSC-derived cardiomyocytes from oxidative stress.

A novel small molecule inhibitor of PDE6δ/KRas interaction with Kd of 203 pM.

A novel small molecule inhibitor of the DNA repair protein Ku70/80, disrupts of Ku70/80-DNA interaction with IC50 of 3.5 uM in EMSA assay.

A novel small molecule inhibitor of transforming acidic coiled-coil-containing protein 3 (TACC3) that selectively inhibits the nucleation of centrosome microtubules in ovarian cancer cells.

A novel small molecule inhibitor of transforming acidic coiled-coil-containing protein 3 (TACC3) that selectively inhibits the nucleation of centrosome microtubules in ovarian cancer cells.

A novel small molecule inhibitor that inhibits PP2A and β-catenin interaction by selectively engaging PR55α binding site (Kd=45 pM).

A novel small molecule KLF5 inhibitor derived from ML264, demonstrates >10-fold enhanced efficacy in multiple cancer cell lines with IC50 of 1.5-10 uM.

A novel small molecule sirtuin-1 (SIRT1) activator that reduces acetylation of mutant 53 and exhibits anti-proliferative effects against TNBC cells carrying mutant p53.

A novel small molecule STAT3 inhibitor that inhibits STAT3 DNA binding activity with IC50 of 1.16 uM, binds to the STAT3 coiled-coil domain (CCD).

JP-153 (JP153) is a novel small molecule targets the Src-FAK-Paxillin signaling, inhibits Src-dependent phosphorylation of paxillin (Y118) and downstream activation of Akt (S473) in RECs; potently inhibits VEGF-induced proliferation and migration, inhibits retinal neovascularization in the murine oxygen-induced retinopathy model.

A novel small molecule that activates GATA4/NKX2-5 transcriptional synergy with EC50 of 7 uM in cell reporter assay. .

A novel small molecule that inhibits GATA4/NKX2-5 transcriptional synergy with IC50 of 3 uM, with no activity on the protein kinases involved in the regulation of GATA4 phosphorylation.

A novel small molecule that overcomes HdmX-mediated p53 repression, binds directly to HdmX (Kd=450 nM) to prevent p53-HdmX complex formation.

CB-002 is a novel small molecule that restores p53 function in mutant p53-expressing colorectal cancer cells without toxicity to normal human fibroblasts; increases expression of endogenous p53 target genes NOXA, DR5, and p21 and cell death; decreases the stability of mutant p53 in RXF393 cancer cells and an exogenously expressed R175H p53 mutant in HCT116 p53-null cells.

A novel small molecule Wnt signaling inhibitor that targets the cysteine-rich domain of Frizzled, specifically binds to the Wnt binding site on the Frizzled8 cysteine-rich domain with Kd of 2.9 uM, IC50 of 5.7 uM..

A novel small-molecule arenaviruse inhibitor that exhibits strong anti-LCMV activity (IC50<1 uM) without cell toxicity.

A novel small-molecule inhibitor of androgen receptor (AR) N-terminal domain inhibitor for the treatment of advanced prostate cancer.

A novel small-molecule inhibitor of androgen receptor (AR) N-terminal domain inhibitor for the treatment of advanced prostate cancer.

A novel small-molecule Wnt signaling inhibitor that inhibits TCF-dependent transcription with IC50 of 6.1 uM in 7dF3 reporter assay.

A novel sodium glucose transporter type 1 and type 2 (SGLT1/2) inhibitor for the oral treatment of type 2 diabetes..

A novel specific CRAC channel inhibitor that blocks function of effector but not regulatory T cells in vitro and attenuates the pogression and severity of EAE in vivo.

A novel specific glycomimetic E-Selectin antagonist with Kd of 0.46 uM, IC50 of 1.75 uM.

A novel specific p110β inhibitor with IC50 of 5.74 nM.

A novel specific ROCK1 kinase inhibitor with IC50 of 11.2 uM, without inhibitory activity against ROCK2.

A novel specific TRPM8 channel antagonist for treatment or prevention vasomotor symptoms..

A novel specific, cell permeant modulator of Kv3 channels with EC50 of 0.9 and 1.9 uM for Kv3.1b and Kv3.2a, respectively.

A novel synthetic, orally bioavailable TLR4/MD2 ligand, significantly reduces the IL-6 secretion by subsequent challenge with LPS at 0.63 uM.

Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1].

A novel tubulin inhibitor that inhibits the proliferation of cancer cell lines with IC50 of 0.2-1.0 uM.

A novel uridine nucleotide analog HCV NS5B polymerase inhibitor for treatment of HCV infection combined with Grazoprevir and Ruzasvir..

A novel, broadly acting non-nucleoside inhibitor of HCV NS5B polymerase with IC50 of 3 nM and 2 nM for GT1b and GT2a, respectively.

A novel, cell-permeable, potent and selective inhibitor of MELK kinase domain with IC50 of 37 nM.

A novel, dual-acting muscarinic receptor antagonist and β2-adrenoceptor agonist (MABA) with pKi of 9.21/9.53 for hM2/M3, pKi of 9.37 for β2-adrenoceptor.

A novel, high affinity and long-acting antagonist of human M3 muscarinic acetylcholine receptor with pKi of 9.03-9.21.

A novel, highly potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 0.026 nM.

A novel, highly potent inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli.

A novel, highly potent positive modulator of Kv7 channels with EC50 of 100 nM (Kv7.2-Kv7.5).

A novel, long-acting and orally active, selective mu-opioid agonist that displays higher binding affinity (Ki=237 nM) at the MOR than kappa and delta opioid receptors (>100-fold).

A novel, novobiocin-based, C-terminal inhibitor of Hsp90 and a potent inducer of Hsp70.

A novel, orally active quinoline compound that can reverse P-glycoprotein (P-gp)-mediated MDR.

A novel, orally active, non-steroidal selective androgen receptor modulator (SARM) with in vitro potency of 13 nM.

A novel, orally active, small molecule inhibitor of BMI-1 that accelerates BMI-1 degradation, inhibits AML cells growth with IC50 of <100 nM.

A novel, potent and selective ALDH1A1 inhibitor with Ki of 300 nM and IC50 of 4.6 uM.

A novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

A novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

A novel, potent inhibitor of most upstream tyrosine kinases in BCR signaling pathway, inhibits BCR kinases Lyn, Syk and Btk with IC50 of 0.15 uM, 1.6 uM and 2.1 uM, respectively.

A novel, potent inhibitor of most upstream tyrosine kinases in BCR signaling pathway, inhibits BCR kinases Lyn, Syk and Btk with IC50 of 0.15 uM, 1.6 uM and 2.1 uM, respectively.

A novel, potent nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with IC50 of 44 nM.

A novel, potent, and selective inhibitor of Late sodium current (late INa) for treatment of long QT-3 syndrome (LQT-3), hypertrophic cardiomyopathy (HCM), and ventricular tachycardia–ventricular fibrillation (VT–VF).

A novel, potent, and selective p110δ PI3K inhibitor with IC50 of 0.1 nM in cell-based assays.

A novel, potent, and selective spleen tyrosine kinase (SYK) inhibitor with enzyme IC50 of 30 nM, cell IC50 of 7 nM (FcεR1-mediated histamine release in human monocyte-derived mast cells, in the presence of 0.1% albumin).

A novel, potent, brain permeant PKC inhibitor with IC50 of 80 nM, without detectable binding to the estrogen receptor (Ki>10 uM).

LXRβ agonist 17 is a novel, potent, orally active liver X receptor β (LXRβ) agonist with Ki/EC50 of 3/21 nM, displays 27-fold selectivity over LXRα; also exhibits excellent selectivity against other nuclear hormone receptors (>3,000-fold); induces the expression of LXR target genes in vitro and in vivo.

A novel, potent, selective orally active CCK-2 receptor antagonist with pKi of 8.49 for hCCK2.

A novel, second-generation C-terminal Hsp90 inhibitor with Kd of 191 and 726 uM for Hsp90α and Hsp90β, respectively.

A novel, specific CD147 inhibitor that can specifically disrupt CD147 dimerization, inhibits the motility and invasion of HCC cells (IC50=7-10 uM).

A novel, spectfic c-Myc IRES (internal ribosome entry site) function inhibitor that prevents binding of hnRNP A1 to the Myc IRES and specifically inhibits Myc IRES activity in MM cells.

FN1-8 is a novel, synthetic small molecule that efficiently interferes with Gli/TAF9 interaction and downregulate Gli/TAF9-dependent transcriptional activity (at 15 uM); inhibits non-canonical Gli activation and acts downstream of the canonical Hh pathway; suppresses cancer cell proliferation in vitro and inhibits tumor growth in vivo.