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 Sirt2 inhibitor with IC50 of 3.745 uM.

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.

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, 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, orally available fungal CYP51 (lanosterol 14-α-demethylase) inhibitor.

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 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 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 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 VPS34 inhibitor.

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 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 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.

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 orally bioavailable small-molecule STAT3 inhibitor.

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 platinum-containing compound that disrupts STAT3 signaling, inhibits cell growth and induces apoptosis in STAT3-activated cancer cells.

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 selective Chk2 inhibitor with IC50 of 0.14 nM.

A potent and highly selective D4 dopamine receptor antagonist with Ki of 3.5 nM, >200-fold selectivity over D2 and D3 receptors.

A potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM.

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 orally active p53-MDM2 interaction inhibitor with IC50 of 2.4 nM.

A potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively.

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 Chk2 inhibitor with Ki/IC50 of 11 nM/120 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.