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

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

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

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

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, 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 enterocytic microsomal triglyceride transfer protein (MTP) inhibitor that inhibits only MTP localized to enterocytes with IC50 of 6 nM.

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

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

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 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 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 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, 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 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 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.

Balixafortide(POL 6326) is a novel potent, selective, peptidic CXCR4 antagonist that interferes with the tumor-protective microenvironment and sensitizes tumor cells to chemotherapy.

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

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.

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 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, small-molecule inhibitor of sirtuin SITR2 with IC50 of 21.8 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 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).

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 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 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 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 stearoyl-CoA desaturase1 (SCD1) inhibitor.The compound exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.

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

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, 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, 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 4 nM for CDK4/cyclin D1 and CDK6/cyclin D3, 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 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).

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, 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.

A novle PKM2 inhibitor inhibitor.

A nucleoside analogue that shows potent inhibition for replication of several mosquito-borne flaviviruses including DENV and ZIKV.

NM-107, also known as 2'-C-Methylcytidine; 2'-C-MeC; 2-CMC; mCyd ; 2'CMeC; 2CMC, is a a potent and selective anti-viral drug. NM-107 showed activity to inhibit the replication of foot-and-mouth disease virus. NM-107 exerts potent anti-DENV activity in DENV subgenomic RNA replicon and infectious systems, with an IC50 value of 11.2±0.3μM. NM-107 may be a promising compound for the development of direct-acting antivirals against DENV infection.

A nucleoside reverse transcriptase inhibitor (NRTI) that used to prevent and treat HIV/AIDS..

Tafluprost(AFP-168) is an anti-glaucoma prostaglandin (PG) analog.A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.1,2,3,4 Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency.

A orally active prodrug of LY3020371, which is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, respectively.

A pan-RAR inverse agonist that blocks RARα activity with IC50 of 114 nM.

A PAR1 peptide fragment (residues 42-47) that acts as a PAR1 agonist.

A partial/full agonist of dopamine receptor with Ki of 3.9/2.2/0.5/5.1 nM for D2S/D2L/D3/D4, respeectively.

Dexpramipexole 2Hcl(KNS-760704), also known as R-(+)-Pramipexole, is a neuroprotective agent and weak non-ergoline dopamine agonist. IC50 Value:Target: Dopamine ReceptorDexpramipexole has been found to have neuroprotective effects and is being investigated for treatment of amyotrophic lateral sclerosis (ALS). Dexpramipexole reduces mitochondrial reactive oxygen species (ROS) production, inhibits the activation of apoptotic pathways, and increase cell survival in response to a variety of neurotoxins and β-amyloid neurotoxicity. Compared to the S-(-) isomer, Dexpramipexole has much lower dopamine agonist activity.

A partially dueterated analog of Atazanavir, an oral HIV protease inhibitor; A deuterium-containing medicine with improved ADME properties; Compound 120 showed an approximately 50% increase in half life compared with Atazanavir.

A peptide antibiotic, commonly grouped with the aminoglycosides, which is given in combination with other antibiotics for MDR-tuberculosis. .

A peptide mimetic of the C-terminal Cys-Val-Ile-Met of K-Ras4B that potently inhibits FTase (Farnesyltransferase) with IC50 of 0.5 nM.

A peptidic glucagon like peptide 2 (GLP-2) analogue for treatment of type2 diabetes..

A pesticide agent..

A pH-dependent, GluN2B-selective inhibitor of NMDA receptor with IC50 of 0.19 uM at pH6.9, 10-fold selecivity over brain tissue pH 7.6 (IC50=1.8 uM).

A phenolic antioxidant and a selective inducer and activator of Nrf2 that ameliorates doxorubicin-induced cardiotoxicity in vivo.

A phosphate ester prodrug of the HIV-1 protease inhibitor amprenavir with improved solubility..

A picornavirus replication inhibitor by binding to the hydrophobic pocket within the VP1 coat protein, thus stabilizing the virion and blocking its uncoating..

A plant activator of systemic acquired resistance, boosts the production of herbivore-induced plant volatiles.

A plant flavonoid that has been found to inhibit cell proliferation by arresting the cell cycle at the G2/M phase.

A plant metabolite possessing anti-leukemic activity; inhibits the non-receptor kinases, Syk and Lck.

A polyamine oxidase (PAO) inhibitor that inhibits spermine oxidase and N1-acetylpolyamine oxidase with IC50 of 6.1 and 0.02 uM, respectively.

A polyene antifungal antibiotic that works by disrupting the cell membrane of the fungal cells..

A poorly reversible TRAAK inhibitor, shows no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2)..

A poten and selective, ATP-competitive DNA-PK inhibitor with IC50 of 0.19 uM, Ki of 24 nM.

A potent 20S proteasome inhibitor with IC50 of 49 nM (inhibition of proteasomal chymotrypsin-like proteolytic activity)..

A potent acetylcholinesterase (AChE) inhibitor with IC50 of 1.3 nM.

A potent acetylcholinesterase (AChE) inhibitor with IC50 of 1.3 nM.

A potent adenosine transport activity of ENT-1 with IC50 of 26.9 nM.

A potent AHR (aryl hydrocarbon receptor) agonist that induces degradation of AhR by the ubiquitin-proteasome pathway.

A potent and balanced dual PPARα/γ agonist (EC50= 50/21 nM).

A potent and biologically-active PDE4/7 inhibitor with IC50 of 50-100 nM for PDE4A/B/D, and 140 nM for both PDE7A/B.

A potent and effective calcium-sensitive opener of maxi-K potassium channels (maxi-K) with EC50 of 392 nM at -48.4 mV in HEK293 isolated outside-out membrane patches.

A potent and efficacious hERG channel activator steeply potentiates current amplitudes more than 10-fold with EC50 of 0.5 uM.

A potent and highly specific inhibitor of Aurora B and Aurora C with IC50 of 7 and 12 nM respectively, with less activity against Aurora A (IC50>2 uM).

A potent and highly specific MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM.

A potent and orally active non-peptide C5a receptor (CD88.

A potent and selective (up to 263-fold) inhibitor of breast cancer cells with GI50 of 0.5 uM (MCF-7), via activation the aryl hydrocarbon receptor (AhR) pathway.

A potent and selective 5-HT1A receptor antagonist.

A potent and selective 5-HT2C receptor agonist with EC50 of 190 nM, with excellent selectivity for 5-HT2C over 5-HT2A.

A potent and selective 5-HT3 receptor antagonist has been shown to be beneficial in the treatment of irritable bowel syndrome..

GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.

A potent and selective agonist for the cannabinoid receptor CB1 with Ki of 0.28 nM, 180-fold selectivity over CB2..

A potent and selective Akt inhibitor with Ki of 0.16 nM for Akt1.

A potent and selective ALK5 inhibitor with IC50 of 5.5 nM, displays 300-fold selecitvity over ALK3.

A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.

A potent and selective antagonist of H3 receptor with Ki/EC50 of 0.16/1.5 nM.

A potent and selective antagonist of H3 receptor with Ki/EC50 of 0.16/1.5 nM.

A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM.

A potent and selective dopamine D3 receptor antagonist with pKi of 8.0.

A potent and selective full β3 adrenergic receptor agonist with EC50 of 1.1 nM.

A potent and selective GC-C agonist (Ki=1.23-1.64 nM) that elicits pharmacological effects locally in the gastrointestinal tract.

A potent and selective GlyT1 inhibitor with EC50 of 54 nM.

A potent and selective GlyT1 inhibitor with IC50 of 15.8 nM, displays no activity for GlyT2 (IC50>30 uM).

A potent and selective HDAC3 inhibitor with IC50 of 0.24 uM, >75-fold selectivity over HDAC1 and no activity against HDAC4/6/8.

A potent and selective HDAC3 inhibitor with IC50 of 0.26 uM, with no activity against HDAC1/4/6/8.

A potent and selective Histamine H3 receptor antagonist with Ki of 0.1-5.8 nM (human, rat H3).

A potent and selective human PPARα agonist with EC50 of 4 nM, >1,000-fold selectivity over human PPARγ (EC50=4.5 uM) and PPARδ (EC50 >100 uM) in PPAR-GAL4 transactivation assays.

A potent and selective human α1D adrenoceptor (α1D-AR) antagonist with Ki of 1.1 nM.

A potent and selective human α1D adrenoceptor (α1D-AR) antagonist with Ki of 1.1 nM.

A potent and selective IKK-2 inhibitor with IC50 of 0.3 uM.

A potent and selective inhibitor of breast cancer cells via activation the aryl hydrocarbon receptor (AhR) pathway.

A potent and selective inhibitor of FAK phosphorylation with biochemical IC50 of 1.2 pM (pFAK Y397), cellular IC50 of 1 nM.

A potent and selective inhibitor of HIV-1 protease with IC90 of 4-40 nM.

A potent and selective inhibitor of IRE1 endoribonuclease with IC50 of 0.41 uM.

AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties.

A potent and selective inhibitor of LTA4 hydrolase (LTA4H) with IC50/Ki of 5 nM/23 nM.

A potent and selective inhibitor of mediator-associated kinase CDK8 (IC50=12 nM) and its paralogue CDK19.

TH287 hydrochloride is a potent and selective inhibitor of MTH1, with an IC50 of 0.8 nM. TH287 hydrochloride is highly selective towards MTH1, with no relevant inhibition of MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase and ITPA at 100 μM. TH287 hydrochloride could act as a chemotherapeutic agent for cancer research.

A potent and selective inhibitor of MTH1 protein with IC50 of 5 nM.

A potent and selective inhibitor of neutral endopeptidase (NEP) with IC50 of 18.9 nM for hNEP.

A potent and selective inhibitor of PDGFR with IC50 of about 0.4 uM both in vitro and in cells.

A potent and selective inhibitor of sterol O-acyltransferase 2 (SOAT2, ACAT2) with IC50 of 11.8 nM, >6,000-fold selectivity over ACAT1.

A potent and selective inhibitor of the MDM2-p53 interaction with Kd of 38 pM, and IC50 of 1.6 nM.

A potent and selective inhibitors of leukotriene C4 synthase (LTC4S) with IC50 of 95 nM, Ki of 6 nM.