A highly potent, selective inhibitor of checkpoint kinase TTK/Mps1 with IC50 of 0.6 nM.

A highly potent, selective mutant p53 (R175H, R249S, R273H, R273C) reactivator.

A highly potent, selective P2Y1 receptor agonist with EC50 of 1.2 nM.

A highly potent, selective platelet activating factor (PAF) inhibitor with IC50 of 75 and 170 nM for aggregation inhibition of rabbit and human platelets induced by PAF.

A highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator with Ki of 0.9 nM, IC50 of 2.5 nM.

A highly potent, selective, and orally bioavailable 11β-HSD1 inhibitor with IC50 of 2.9 and 1.6 nM for hHSD1 and mHSD1, respectively.

A highly potent, selective, and orally bioavailable factor Xa (FXa) inhibitor with Ki of o.19 nM, >5,000-fold selectivity over a series of related serine proteases.

A highly potent, selective, and orally bioavailable factor Xa (FXa) inhibitor with Ki of o.19 nM, >5,000-fold selectivity over a series of related serine proteases.

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

A highly potent, selective, orally active mGluR5 negative allosteric modulator with Ki of 5.4 nM, IC50 of 3.1 nM.

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

A highly potent, selective, orally available Src family kinase inhibitor with IC50 of <0.5 nM, <0.5 nM and for Src, Yes and Fyn kinases respectively, >950-fold selectivity for Src over ABL.

A highly potent, selective, orally bioavailable HCV NS5B polymerase inhibitor with IC50 of 9, 4, and 18 nM for GT1a, GT1b, and GT1b-C316N mutant in HCV replicon assay, respectively.

A highly potent, selective, second generation prostaglandin E2 subtype 4 receptor (EP4) antagonist with Ki of 0.56 nM.

A highly potent, specific and cell permeant inhibitor of human proline endopeptidase (PE) with Ki of 1 nM.

A highly potent, subtype-selective agonist of 5-HT2C receptor with Ki of 10.5 nM, >20-fold selectivity over 5-HT2A and 5-HT2B receptor subtypes (IC50=212 and 485 nM, respectively).

A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM.

A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM.

A highly selective and potent GRK2 (G protein-coupled receptor kinase 2) inhibitor with IC50 of 130 nM.

A highly selective CYP17A1 (17,20-lyase) inhibitor with IC50 of 17 nM for human 17,20-lyase.

A highly selective inhibitor of the FMN riboswitch that controls expression of de novo riboflavin (Vitamin B2) biosynthesis in Escherichia coli.

A highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor.

A highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor.

A highly selective, non-peptide agonist of the δ-opioid receptor (δ-OR) with IC50/Ki of 2.73/0.18 nM.

A highly selective, potent, BBB penetrant and orally bioavailable 5-HT6R antagonist for the treatment of neurological disorders such as AD and schizophrenia.

A highly selective, potent, BBB penetrant and orally bioavailable 5-HT6R antagonist for the treatment of neurological disorders such as AD and schizophrenia.

A highly selective, small molecule inhibitor of the miRNA regulatory complex RISC subunit SND1.

A highly specific myosin II ATPase inhibitor.

A higly potent, orally bioavailable, BBB permeable 5-HT7 receptor antagonist with Ki of 153 pM, with slightly lesser potency toward 5-HT6, 5-HT2A and 5HT-2C (Ki = 1.2-2.0  nM).

A hit compound that inhibits the proliferation of human peripheral blood T cells stimulated with anti-CD3 with IC50 of <10 nM, inhibits TCR-Nck interaction..

A HIV-1 surface-membrane inhibitor, also is a Fap1-blocking small molecule that replicates SLV peptied functions.

A homogenous mixture of compound that is used to stain amyloid plaques, binds to amyloid fibrils but not monomers and gives a distinct increase in fluorescence emission..

A homoisoflavanone found in Caesalpinia sappan, a potent, selective IMPDH2 inhibitor that covalently binds to Cys140 with Kd of 3.944 nM, almost 10 times lower than the Kd of binding to IMPDH1.

CM-11 is a homo-PROTAC, bivalent small-molecule dimerizer of the VHL E3 ubiquitin ligase to induce self-degradation.

A hormonally active metabolite of vitamin D that binds to vitamin D receptor (VDR).

A hyperpolarization-activated cyclic nucleotide-gated (HCN) channel.

A imidazoline compound that stimulate insulin release by inhibition of ATP-dependent K+ channels and inducing of Ca2+ mobilization in mouse pancreatic beta-cells.

A linear sulfated polysaccharide extracted from red edible seaweeds, shows topical microbicide activity targeting HIV viruses.

A local anesthetic.

A locally-acting nonsteroidal anti-inflammatory drug (NSAID) with local anaesthetic and analgesic properties for pain relief and anti-inflammatory treatment of inflammatory conditions.

A long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma.

A loop diuretic used to treat high blood pressure and the swelling, a novel ligand and inhibitor of MAP2K6 kinase that inhibits MAP2K6 in part through alkylation of a nonconserved cysteine residue.

A low micromolar (EC50=9.7 uM, K2P2.1), selective activator of temperature- and mechano-sensitive K2P potassium channels.

A macrolide antibiotic that effectively inhibits tumor angiogenesis by suppressing VEGFR2-mediated signaling pathways in lung cancer.

A Mannich base compound, selective and orally active JAK3 inhibitor that blocks IL-2-induced activation of JAK3 and downstream substrates STAT5a/b.

A marine sponge alkaloid that inhibits Chk1 and Chk2 with IC50 of 3 and 3.5 uM, respectively.

A melanoma-selective anticancer agent (IC50=30 nM, Malme-3M cell line), induces cell death by autophagocytosis, targeting the cancer-protective protein dermcidin.

A melatonin receptor agonist of MT1 (Ki=0.1nM) and MT2 (Ki=0.12nM), and a 5-HT2C (Ki=631nM) receptor antagonist.

A melatonin receptor agonist of MT1 (Ki=0.1nM) and MT2 (Ki=0.12nM), and a 5-HT2C (Ki=631nM) receptor antagonist.

A membrane permeable IP3 receptor antagonist and broad TRP channels (TRPC5, TRPM2) blcoker.

A membrane-impermeable sodium channel blocker, blocks sodium current in voltage-clamped nociceptive DRG neurons.

A metabolite of Gefitinib, which is a potent inhibitor of tyrosine phosporylation in EGFR..

A metabolite of ST1535, which is potent, selective A2A adenosine receptor antagonist with Ki of 6.6 nM..

A metabolite of tamoxifen, orally active non-steroidal selective estrogen receptor modulator (SERM) for the treatment of estrogen receptor-positive breast cancer..

A mitochondriotoxic small molecule that selectively inhibits proliferation of mammary epithelial, neu-overexpressing cells, as well as a variety of mouse mammary tumor and human breast cancer cell lines.

A moderately potent, but highly selective α2-adrenoceptor antagonist, the only reported selective antagonist at the α2B-adrenoceptor not having potent α1-adrenoceptor antagonist activity.

A multichannel blocker agent that has antiarrhythmic activity.

A mycotoxin produced from F. moniliforme, and an inhibitor of ceramide synthase (sphingosine N-acyltransferase/CerS).

A nanomolar potent, selective, and orally bioavailable glycine transporter type-1 (GlyT1) inhibitor for the treatment of negative symptoms associated with schizophrenia.

Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.

Dip G is a natural compound, novel chemical probe reciprocally stabilizes ERβ and destabilizes ERα in breast cancer cells; targets CHIP ubiquitin E3 ligase to modulate ER protein stability, enhances the transcription and anti-proliferative activities of ERβ, while attenuating the transcription and proliferative effects of ERα; the first small molecule that can restore the balance of ERα and ERβ.

A natural furanocoumarin that is found to be a potent inhibitor of debenzylation activity of CYP3A4 enzyme with IC50 of 24.92 uM.

A natural poduct that functions as a splicing inhibitor with IC50 of 35 uM, blocks a late stage of spliceosome assembly..

A natural tetranortriterpenoid compound that inhibits Hsp90 and induce the degradation of Hsp90-dependent client proteins.

A naturally occurring nucleoside analog that possesses antitumor activity, also is a potent and efficacious readthrough agent.

A naturally occurring tetranortriterpenoid that has been found to act as a potent, selective, small-molecule agonist of TrkB with Kd of 1.4 uM.

A negative allosteric modulator of the Frizzled4 (Fzd4) receptor and a Wnt/β-catenin pathway inhibitor with pEC50 value of 5.74 for inhibition of Wnt antagonism.

A negative control of VU-WS113, which is a potent inhibitor of Wnt signaling with EC50 of 80 nM that selectively potentiates CK1α kinase activity..

A neuropeptide derived from the same precursor polypeptide as neurotensin, and with similar but subtly distinct expression and effects..

A new broad spectrum industrial microbicide with applications in material and coating preservation. .

A new compound which is similar with +JQ-1，BET bromodomain inhibitor

A new-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infections, the prodrug of the active compound VM-1500A..

A newly identified, small molecule HuR inhibitor that disrupts HuR multimerization modules and reduces tumor cell survival and proliferation..

A noncovalent small molecule binder to Keap1 (Kd=6 uM) and selective activator of Nrf2 signaling.

A non-immunosuppressive FTY720 analogue, PKCδ activator with higher antiproliferative potency with IC50 of 2.4, 2.4, and 3.5 uM in Huh7, Hep3B, and PLC5 cells, respectively.

A non-ionic emulsifying agent that can modulate multidrug resistance and enhances antitumor activity of vinblastine sulfate by modulating substrate-stimulated P-gp ATPase activity.

A nonnucleoside, competitive, small-molecule inhibitor of human ribonucleotide reductase (hRR) that binds to the large subunit hRRM1 at the catalytic site (C-site) with Kd of 37.4 uM, IC50 of 32 uM.

A nonpeptide endothelin ETA receptor antagonist. Antihypertensive.

A non-peptide small molecule agonist of the PTH1 receptor, activates both the cAMP and calcium signaling pathways..

A nonpeptide, cell-permeable STAT3 inhibitor that binds directly to the pTyr705 binding site of the STAT3 monomer.

A non-peptide, centrally-penetrant and selective agonist of GHSR with appetite-enhancing and anabolic effects.

A non-peptide, centrally-penetrant and selective agonist of GHSR with appetite-enhancing and anabolic effects.

A non-peptide, selective RGS4 inhibitor that inhibits RGS4/Gα(o) binding with 3 to 5 uM potency.

A nonpeptidic, selective, brain-penetrant agonist of nociceptin/orphanin FQ receptor (NOP receptor/ORL1) with pKi of 9.41.

A nonpeptidyl small molecule agonist of GDNF family receptor α1 (GFRα-1).

A non-planar analogue of fascaplysin that selectively inhibits CDK4/cyclin D1 with IC50 of 5.5 uM.

A non-selective agonist of Adenosine A3 receptor.

A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM).

A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM).

A non-selective beta blocker used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent..

A non-selective group I/group II metabotropic glutamate receptor (mGluR) antagonist..

A nonselective inhibitor of UBL protein-activating E1 enzymes that forms covalent adducts with UBL proteins SUMO1, ubiquitin, Nedd8, ISG15, and GABARAP in the presence of ATP and E1 enzymes in vitro.

A non-steroidal anti-inflammatory drug (NSAID).

A nonsteroidal selective estrogen receptor modulator (SERM) that shows 10- to 60-fold increased affinity for the estrogen receptor compared with Tamoxifen.

A non-steroidal sulphamate analogue of 2-methoxyoestradiol (2ME2) and microtubule disruptor, shows anti-proliferative activity against NCI 60 cell lines with mean GI50 of 50 nM.

A nontoxic heat shock protein (HSP) coinducer and potentiator of the heat shock response.

A nontoxic, orally active heat shock protein (HSP) coinducer and potentiator of the heat shock response.

A nootropic agent that enhances high-affinity choline uptake.

A nove potent, dual FGFR and PIK3C3 inhibitor with Kd of 0.53 nM for PIK3C3.

A nove potent, selective and reversible SHP2 inhibitor with Ki of 0.51 uM.

A novel 5-HT receptor antagonist for the treatment of Parkinson's disease..

A novel a potent, selective inhibitor of BRD4 with Kd of 550 nM, cellular IC50 of 724 nM.

A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM.

A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM.

A novel and highly selective 5-HT6 receptor small molecule antagonist with Ki of 2.34 nM.

A novel and irreversible inhibitor of mutant K-ras G12C..

A novel and irreversible inhibitor of mutant K-ras G12C..

A novel and irreversible inhibitor of mutant K-ras G12C..

FT011 is an anti-fibrotic agent, reduces mRNA expression of collagens I and III and inhibits collagen synthesis.

A novel antifolate modulator compound..

Olorofim (F901318) selectively inhibits fungal dihydroorotate dehydrogenase (DHODH), a key enzyme in the pyrimidine biosynthesis pathway. Olorofim (F901318). Olorofim exhibits excellent activity against A. fumigatus and other Aspergillus spp.

A novel antiprion compound with EC50 of 68 nM, significantly increases monoglycosylated/diglycosylated PrPSc..

A novel anti-TB agent that has an MIC range of 0.06-0.5 ug/mL..

A novel anti-TB agent that has an MIC range of 0.06-0.5 ug/mL..

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

A novel brain penetrant antiprion compound with EC50 of 57 nM, prevents both PrP(Sc) accumulation and astrocytic gliosis in the cerebrum.

A novel bromodomain BRD4 inhibitor that significantly induces HIV-1 reactivation.

A novel cardiotonic agent that acts as a calcium sensitizer with no chronotropic activity in mammalian cardiac muscle, elicits positive inotropic effect in dog and rabbit ventricular muscles (EC50=9.2 uM).

A novel cell membrane impermeable smoothened antagonist with IC50 of 7.6 nM in Hh-dependent Gli transcriptional activity assay.

A novel cell permeable smoothened antagonist with IC50 of 3.1 nM in Hh-dependent Gli transcriptional activity assay.

A novel chemical probe that enable selective 2’-hydroxyl acylation for accurate RNA structural analysis in living cells..

A novel compound that disrupts the HIV-1 integrase LEDGF interaction.

Dotinurad is a novel compound that exhibits a remarkable uric acid excretion-promoting action.

A novel conformational modulator of α-synuclein with EC50 of 105 uM, potentially outcompetes spermine in binding to α-synuclein.

A novel CTLA-4 inhibitor.

GB111-NH2 (Z-Phe-Lys-AOMK) is a novel cysteine cathepsin inhibitor that blocks the activity of cathepsins B, L and S. GB111-NH2 (Z-Phe-Lys-AOMK) inhibits autophagy and increases oxidative stress, specifically trigger macrophage cell death.

A novel dansylated analog of purvalanol B, and a CDK inhibitor that inhibits cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B.

A novel diaryldiamine that inhibits bacterial methionyl-tRNA synthetases in Gram-positive bacteria as a novel agent to treat Clostridium difficile infection (CDI).

A novel dual inhibitor of mTOR and DNA-PK with IC50 of 21 nM and 13 nM, respectively.

A novel dual-acting steroid sulfatase inhibitor (IC50=0.1 uM) and selective ERα modulator (SERM).

A novel Ehp inhibitor

A novel Ehp inhibitor

Benzenepentacarboxylic acid is a fluorescent dye that detects and scavenge HO radicals.

A novel FTY720 analog that acts as PP2A activator, disrupts the SET/PP2A interaction devoid of immunosuppressive effects leads to the reactivation of PP2A.

A novel highly potent, selective, long acting muscarinic receptor M3 antagonist with pIC50 of 9.8, 10-fold selectivity over M2 (pIC50=9.0).

A novel histamine H3 receptor inverse agonist for the treatment of sleep apnoea syndrome.

A novel HIV-1 non-catalytic-site integrase inhibitor (NCINI).

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 Non-competitive AMPA/kainate antagonist.

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 P2X3 and P2X2/3 receptor antagonist useful for the treatment of urinary tract diseases, pain, respiratory diseases and cardiovascular diseases.

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.