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 GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.

A potent and selective group I PAK (pan-PAK1/2/3) inhibitor with Ki of 0.95/2 nM for PAK1/2, respectively.

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 HDAC8 inhibitor with IC50 of 0.5 uM..

A potent and selective HDAC8 inhibitor with IC50 of 70 nM.

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.

A potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM.

A potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM.

A potent and selective linear tachykinin NK2 receptor antagonist with pKb of 9.3.

A potent and selective MCH-R1 antagonist with IC50 of 22 nM, Ki of 14 nM.

A potent and selective melanocortin 4 receptor (MC4R) agonist with EC50 of 2.1 nM.

A potent and selective mTOR inhibitor with Ki of 1.5 nM.

A potent and selective NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 22 nM, >200-fold selectivity over Plk1, Mps1, Aurora A and CDK2.

A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor.

A potent and selective PDE10A inhibitor with binding affinity (Kd) of 0.15 nM, IC50 of 2.11 nM.

A potent and selective PDE10A inhibitor with IC50 of 7.28 nM.

A potent and selective RARγ receptor agonist with Ki of 150 nM.

A potent and selective ROCK inhibitor with Ki of 1.6 nM.

UNC-1679 (UNC1679) is a potent and selective small molecule chemical probe of a methyl-lysine reader protein L3MBTL3 with Ki of 0.35 uM.

A potent and selective small-molecule inhibitor of Lck with IC50 of 147 nM.

A potent and selective TAAR1 partial agonist with Ki of 0.5, 1.0, 6.8 and 2.6 nM for mouse, rat, human and monkey TAAR1, respectively.

A potent and selective tachykinin NK1 receptor antagonist with Ki of 2.9 nM.

A potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 34 nM, prevents tissue hyperplasia in the rat urethra or common iliac artery..

A potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 34 nM, prevents tissue hyperplasia in the rat urethra or common iliac artery..

NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells. IC50 value: 6.8 nMTarget: Cav3.1 T-type channelNNC 55-0396 can be an essential tool in preventing human ovarian cancer cell proliferation as a result of its ability to inhibit the function of T-type Ca2+ channels. It is believed that NNC 55-0396 may functions by dissolving in or passing through the plasma membrane of cells.

A potent and selective type III phosphatidylinositol 4-kinase (PI4KIIIβ) inhibitor with IC50 of 3.6 nM.

A potent and selective VEGFR2 (KDR) inhibitor with IC50 of 40 nM.

A potent and selective VEGFR2 (KDR) inhibitor with IC50 of 40 nM.

A potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM.

A potent and selective α4β2 nAChR agonist with Ki of 16 nM.

A potent and selective δ-opioid receptor agonist that has high affinity and selectivity for the δ1 subtype with Ki of 1.12 nM.

A potent and selective, brain penetrant FAAH inhibitor with IC50 of 11 nM.

A potent and selective, CNS penetrant mGlu2 negative allosteric modulator with IC50 of 78 nM.

A potent and selective, CNS penetrant mGlu3 negative allosteric modulator with IC50 of 245 nM.

A potent and selective, CNS-penetrant PDE1 inhibitor with IC50 of 2.4 nM for PDE1B..

A potent and selective, CNS-penetrant PDE1 inhibitor with IC50 of 35 nM for PDE1B..

A potent and selective, non-ATP competitive, allosteric MAPKAPK2/3 (MK2/3) inhibitor with IC50 of 8 nM for MK2, hTNFα EC50 of 0.31 uM.

A potent and selective, orally bioavailable aromatase inhibitor with IC50 of 1.7 nM, 180 times more potent than aminoglutethimide.

A potent and selective, orally bioavailable JAK2 inhibitor with IC50 of 2 nM.

A potent and selective, orally bioavailable, reversible BTK inhibitor with IC50 of 2.8 nM.

A potent and specific antagonist of platelet activating factor (PAF) receptor that inhibits PAF-induced human platelet and neutrophil aggregation in vitro with IC50 of 0.17 and 0.36 uM, respectively.

A potent and specific BET bromodomain inhibitor with Ki of 3.2-24.7 nM for BD1 and BD2 domains of BRD2, BRD3, and BRD4.

RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.

A potent and specific CCR6 antagonist.

OSU-T315 (ILK-IN-1) is a potent and specific integrin-linked kinase (ILK) inhibitor which inhibits PDK2 function in the AKT pathway activation

A potent and specific nuclear export inhibitor that binds to and inhibits CRM1 (XPO1).

A potent and specific, nonlipid agonist of LPA2 receptor with EC50 of 100 nM, without activating or inhibiting LPA1/3/4/5 receptors.

Proxalutamide (GT-0918) is a nonsteroidal antiandrogen (NSAA) – specifically, a selective high-affinity silent antagonist of the androgen receptor (AR) for the potential treatment of COVID-19, prostate cancer, and breast cancer.

A potent anthrax lethal toxin entry inhibitor with IC50 of 1.7 uM, inhibits endosomal trafficking pathways exploited by multiple toxins and viruses.

A potent anticancer agent that demonstrates potent antitumor activity in vitro against several cancer cell lines as well as in vivo against several tumor models, effectively inhibits in vitro tubulin polymerization. .

A potent aromatase inhibitor for the treatment of hypogonadism..

A potent bactericidal agent that inhibits the KinA autophosphorylation with IC50 of 1.6 uM.

A potent BCL6 protein-protein interaction inhibitor with Kd of 78 nM.

A potent benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity.

A potent BET bromodomian inhibitor with IC50 of 3-7 nM for BRD2/3/4 BD1 and BD2..

A potent blocker of high-conductance Ca2+-activated K+ (BKCa, KCa1.1) channels that binds to the α-subunit of BKCa with Ki of 1.9 nM.

A potent blocker of voltage-gated potassium channels Kv7 (KCNQ) that enhances ACh release from rat hippocampal slices in vitro with EC50 of 0.7 uM.

A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR.

A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR.

A potent Caspase-6 inhibitor with IC50 of 192 nM, also inhibits Caspase-4/8/9/10 with IC50 of 0.1-0.8 uM.

A potent CCR2 specific antagonist that blocks MCP-1 mediated response with an IC50 of 3.2 nM.

A potent CCR4 antagonist that blocked CCL22- and CCL17-mediated migration of human peripheral blood CD4+CD25+ Treg and Th2 cells ex-vivo and murine Tregs in-vivo.

A potent CCR4 antagonist that blocked CCL22- and CCL17-mediated migration of human peripheral blood CD4+CD25+ Treg and Th2 cells ex-vivo and murine Tregs in-vivo..

A potent CDK1 and CDK2 inhibitor with IC50 of 9.5 nM and 5.4 nM against CDK1/cyclinB and CDK2/cyclinA3 respectively.

A potent chelator of iron that arrests late stages of cytokinesis by blocking the physical process of constriction in dividing cells.

A potent CXCR7 (ACKR3) agonist..

A potent CYP26A1 inhibitor with IC50 of 10 nM, potently inhibits all-trans-retinoic acid metabolism in intact T47D cells with IC50 of 8.7 nM.

Beaucage reagent is a DNA cleavage reagent.

A potent dopamine D2 receptor antagonist with Ki of 28 nM.

A potent dopamine D2 receptor antagonist with Ki of 28 nM.

A potent dopamine stabilizer with Ki of 447 and 1305 nM for D2 and D3 receptors respectively.

A potent dual H3/H2 receptor antagonist with Ki of 0.07 and 7.8 uM, respectively.

A potent dual inhibitor of EGFR and ErbB2.

A potent G2 checkpoint inhibitor that specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint.

A potent GIRK2 inhibitor that inhibits GIRK2-mediated flux with an IC50 of 0.35 uM.

A potent glucagon receptor (GCGR) negative allosteric modulator..

A potent glutaminyl cyclase (QC) inhibitor with Ki of 60 nM.

A potent GSK3β inhibitor with IC50 of 22 nM.

A potent gucokinase (GK) activator with EC50 of 0.29 uM.

Daclatasvir is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) and is used in combination with other oral antiviral agents to treat chronic hepatitis C. Elevations in serum enzyme levels during daclatasvir therapy are uncommon, and it has yet to be convincingly implicated in cases of clinically apparent liver injury with jaundice. Nevertheless, and for unknown reasons, successful all-oral regimens of antiviral therapy in patients with chronic hepatitis C and cirrhosis is occasionally complicated by hepatic decompensation and may cause reactivation of hepatitis B in susceptible patients coinfected with the hepatitis B virus (HBV).

A potent HCV NS5B RNA polymerase inhibitor.

A potent HDAC inhibitor with IC50 of 172 nM.

A potent HDAC inhibitor with IC50 of 27 nM (HeLa cell extracts).

A potent heat shock protein coinducer.

A potent hERG channel activator that concentration-dependently increases the hERG current (2.1 and 3.4-fold at 3 and 10 uM, respectively) and markedly slows hERG channel deactivation and inactivation.

A potent HIF-2α inhibitor with IC50 of <500 nM in HIF-2α scintillation proximity assay. .

A potent histamine 1 receptor antagonist..

A potent HIV integrase strand transfer inhibitor (InSTIs) with IC50 of 8 nM in HIV replication assay.

A potent HIV-1 entry inhibitor that blocks the gp120-CD4 interaction.

A potent HIV-1 integrase strand transfer inhibitor with IC50 of 33 nM, 9.5 nM, 40 nM, 20 nM and 237 nM for wt IN, IN Y143R, IN N155H, G118R and IN G140S-Q148H, respectively.

A potent Hsp90α/p23 interaction inhibitor with IC50 of 0.15 uM, more effective than CP-9 in degrading pAkt/total Akt and Raf-1.

A potent Hsp90α/p23 interaction inhibitor with IC50 of 3.2 uM.

A potent human indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with Ki of 0.97 uM, also exhibits significant antitrypanosomal activities with EC50 of 0.82 uM..

A potent inhibitor of developmental angiogenesis in the zebrafish eye, and a cysteinyl leukotriene 1 and 2 receptor (CysLT1 and 2) antaognist with IC50 of 1.2 and 52 uM, respectively.

A potent inhibitor of drug-resistant S31N mutant of the M2 ion channel of influenza A virus with IC50 of 153 nM.

A potent inhibitor of HDAC1/3/6 with IC50s of 43-72 nM.

A potent inhibitor of HIV-1 integrase-LEDGF/p75 interaction.

A potent inhibitor of hTGase (Tissue transglutaminase) with IC50 of 0.8 uM.

ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC50 of 7 μM.

A potent inhibitor of MLL1/WDR5 protein-protein interaction with IC50 of 0.9 nM.

Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.IC50 value:Target: P-glycoprotein In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects.

A potent inhibitor of sEH (soluble epoxide hydrolase) with IC50 of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively.

A potent inhibitor of sEH (soluble epoxide hydrolase) with IC50 of 18 nM and 69 nM for mouse sEH and human sEH, respectively.

A potent inhibitor of the mRNA decapping scavenger enzyme (DcpS) with IC50 of 0.11 nM.

A potent inhibitor of TrkA with IC50 of 2.9 nM, also inhibits TrkB, TrkC.

A potent inhibitor of tumor promoting phorbol ester TPA/PMA and inhibitor of Ca2+/calmodulin dependent EF-2 phosphorylation

A potent inhibitors of Botulinum Neurotoxin A (BoNT) Light Chain with IC50 of 0.9 uM..

A potent integrin αvβ3 antagonist with IC50 of 18 nM.

A potent inwardly rectifying K+ channel Kir7.1 inhibitor with IC50 of 5.6 uM in T1+ flux assays.

BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM). BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively

A potent Kir7.1 inhibitor with IC50 of 2.0 uM, induces long-lasting uterine contractility similar to those observed with VU590..

A potent Kv11.1 (hERG) channel allosteric modulator that protects cardiac tissue from hERG-related drug-induced arrhythmias.

NS5806 is a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2[1].

A potent lipid peroxidation inhibitor that has antishock and endothelial protective actions.

Cevimeline HCl is a cholinergic agonist that binds to muscarinic receptors. Muscarinic agonists in sufficient dosage can increase secretion of exocrine glands, such as salivary and sweat glands, and increase tone of the smooth muscle in the GI and urinary tracts.

Cevimeline is a parasympathomimetic and muscarinic agonist that affects M1 and M3 receptors. It is used in the treatment of dry mouth and Sjögren's syndrome. Cevimeline has also been shown to reduce Xerostomia symptoms and increase salivary flow in head and neck cancer survivors after radiotherapy.

A potent matrix metalloproteinase (MMP) inhibitor..

A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.1 nM), cellular potency (SJSA-1 EdU IC50=16 nM), and favorable pharmacokinetic properties.

A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.4 nM), cellular potency (SJSA-1 EdU IC50=25 nM), and favorable pharmacokinetic properties.

A potent melanocortin MC3 and MC4 receptor antagonist with IC50 of 0.23 nM and 0.06 nM, respectively.

A potent microtubule inhibitor that not only inhibits the expression levels of HIF-1α protein but also destabilizes HIF-1α mRNA.

A potent monoamine oxidase B (MAO-B) inhibitor..

A potent mutant c-Src T338C kinase inhibitor with IC50 of 317 nM.

A potent mutant Src T338C inhibitor with IC50 of 111 nM.

A potent neutral endopeptidase EC 3.4.24.11 (atriopeptidase) inhibitor that increases endogenous ANF levels and produces natriuretic and diuretic responses intravenously in mice..

A potent non-nucleoside RSV L-protein polymerase inhibitor with EC50 of 0.01 uM and 1.3 uM for RSV A2 and RSV B-WST, respectively.

A potent non-nucleoside RSV L-protein polymerase inhibitor with IC50 of 89 nM.

A potent non-peptide antagonist of tachykinin NK2 receptor with pKi of 9.5 in CHO cells.

A potent Nrf2 activator that upregulates Nrf2 expression and resulted in translocation of Nrf2 into the nucleus..

A potent nuclear receptor TR3 (Nur77)-specific targeting compound that can induce melanoma autophagy through a mitochondrial signaling pathway.

A potent nucleoside analog reverse transcriptase inhibitor (nRTI). An analog of cytidine that can inhibit both types (1 and 2) of HIV reverse transcriptase as well as the reverse transcriptase of hepatitis B. Needs to be phosphorylated to its triphosphate

A potent pan HER/VEGFR inhibitor with IC50 of 5/20/60/50 nM for EGFR/HER2/ERBB4/VEGFR2 respectively.

A potent pan-HDAC inhibitor with IC50 of 16-30 nM, inhibits cell proliferation of P815, C2, and BR cells with IC50 of 0.65, 0.30, and 0.23 uM, respectively.

A potent PD-1/PD-L1 interaction inhibitor with IC50 of 2.25 nM in a homogenous time-resolved fluorescence binding assay..

A potent PD-1/PD-L1 interaction inhibitor with IC50 of 2.25 nM in a homogenous time-resolved fluorescence binding assay..

A potent PD-1/PD-L1 interaction inhibitor with IC50 of 6-100 nM in a homogenous time-resolved fluorescence binding assay..

A potent PD-1/PD-L1 interaction inhibitor with IC50 of 80 nM in a homogenous time-resolved fluorescence binding assay..

A potent PDE4 inhibitor with IC50 of 94.5 nM..

A potent PfDHODH inhibitor that exhibits low nanomolar in vitro potency against DHODH from P falciparum, P vivax, and P berghei.

A potent phosphodiesterase 12 (PDE12) with Ki of 17.5 nM, with no activity for related enzyme CNOT6 (Ki>10 uM).

A potent photoaffinity ligand for the peripheral-type benzodiazepine binding site with Ki of 4 nM.

A potent PI3K inhibitor with IC50 3 nM, does not inhibit PI4K activity.

A potent PIKfyve inhibitor that inhibits autophagy by impairing lysosomal maturation, potently and reversibly inhibits autophagosome-lysosome fusion by activating RAB5A.

A potent protein tyrosine kinase inhibitor that shows selectivity for PDGFR in vitro and in cells.

A potent psychopharmacologic agent that shows high affinity for 5-HT, dopamine, histamine and adrenoceptors.

A potent respiratory syncytial virus (RSV) fusion inhibitor..

A potent RIG-I-like receptor (RLR) agonist that triggers IRF3-dependent innate immune antiviral genes and IFN-β expression.

JNJ 2408068 is a potent RSV (respiratory syncytial virus) inhibitor. JNJ2408068 significantly inhibits replication of RSV A and B subtypes in the lungs of cotton rats without any evidence of toxicity. The minimum protective dose of JNJ 2408068 appears to be approximately 0.39 mg/kg[1].

A potent small molecule inhibitor of MELK kinase activity with IC50 of 42 nM.

A potent small molecule inhibitor that binds and disrupts the MDM2/MDMX-p53 interaction with IC50 of 0.19 uM and 19.7 uM, respectively..

A potent small-molecule inhibitor of the MIR155 host gene/miR-155 axis.

A potent SR-3 antagonist

A potent Src inhibitor extracted from patent WO/2012003544A1..

A potent STAT5 inhibitor with a dual mechanism of action, potently inhibits STAT5 through liberation of endogenous phosphatase activity following NADPH oxidase (NOX) inhibition at 200-300 nM.

A potent TLR7 agonist with EC50 of 59 nM..

A potent TLR7 agonist with EC50 of 8.6 nM. .

3M-011 is a potent TLR7/8 agonist and cytokine inducer; stimulates type I interferon (IFN) and other cytokines such as TNF-alpha, IL-12, and IFN-gamma from rat peripheral blood mononuclear cells; induces IL-12 and COX-2 expression in mDC from HIV+ and HIV- individuals, and inhibits H3N2 influenza viral replication in the nasal cavity; potentiates NK cytotoxicity, and shows antitumor effects in scid/B6 mice and scid/NOD mice.

A potent TLR7/8 agonist that induces robust production of the Th1-polarizing cytokines TNF-alpha and IL-12 from neonatal antigen-presenting cells (APCs)..

A potent TNFα/TNFRc1 interaction antagonist with IC50 of 50 nM, with no affinity for the related cytokine receptors TNFRc2 or CD40, and no cytotoxicity (>100 uM).

A potent tubulin inhibitor that is a toxin payload in antibody drug conjugates (ADCs)..

A potent type I interferon (IFN) inducer that directly binds to STING and triggers a strong antiviral response through the TBK1/IRF3 route.

A potent tyrosine kinase inhibitor targeting c-Kit and PDGFR with IC50 of 0.15 and 0.05 uM in cell based assays.

A potent tyrosine kinases inhibitor with IC50 of 13/9/3/26/2 nM for Lck/Btk/Lyn/Syk/Txk..

A potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction with IC50 of 5 nM.

A potent γ-secretase inhibitor that preferentially inhibits cleavage of the APP CTF cleavage with IC50 of 7.1 nM.

A potent, allosteric HIV integrase inhibitor (Kd=34 nM) that binds the LEDGF/p75 binding site on integrase.

A potent, allosteric inhibitor of CBFβ-RUNX1 interaction with IC50 of 3.2 uM in FRET assays.

A potent, allosteric, α1-selective small molecule activator of AMPK (EC50=20 nM).

A potent, and selective Bax agonist (Ki=43.3 nM) that induces conformational changes in Bax by blocking S184 phosphorylation.

A potent, and selective FAAH inhibitor with IC50 of 18 nM.

A potent, and selective GluR5-subunit containing kainate receptor antagonist with Kd of 402 nM.

A potent, ATP-competetive CDKs inhibitor with IC50 of 7, 7, 7, 3 uM for Cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk/p35 kinase.

A potent, ATP-competitive and highly selective Chk2 inhibitor with IC50 of 138 nM.

A potent, ATP-competitive and relative selective Nek2 inhibitor with IC50 of 0.27 uM.

A potent, biased allosteric agonist of CXCR3 (pEC50=5.22) that activates solely G proteins, induces chemotaxis, but fails to induce receptor internalization or β-arrestin 2 recruitment..

A potent, biased allosteric agonist of CXCR3 (pEC50=6.64), selectively induces chemotaxis and receptor internalization, and induces β-arrestin 2 recruitment without any stimulation of G proteins..

A potent, brain penetrant, dual MAO-A and AChE inhibitor that shows neuroprotective effects both in vitro and in vivo.

A potent, cell-permeable inhibitor of MK2 with IC50 of 8.5 nM.