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

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

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.

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

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

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

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.

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

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

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

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

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

A novel Non-competitive AMPA/kainate antagonist.

A novel Non-competitive AMPA/kainate antagonist.

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

A novel platelet inhibitor

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

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

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

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

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

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 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 Sirt2 inhibitor with IC50 of 3.745 uM.

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

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

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...

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

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.

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.

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

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

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 VPS34 inhibitor.

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

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, 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).

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

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.

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.

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 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.

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

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

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 JAK3 inhibitor with IC50 of 0.15 nM.

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

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 Akt inhibitor with Ki of 0.16 nM for Akt1.

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 CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.

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 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.

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.

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 PDGFR with IC50 of about 0.4 uM both in vitro and in cells.

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.

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

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 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.

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).

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 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.

Beaucage reagent is a DNA cleavage reagent.

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

A potent GSK3β inhibitor with IC50 of 22 nM.

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 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 18 nM and 69 nM for mouse sEH and human sEH, respectively.

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

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

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].

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

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 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 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.

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].

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

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

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, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively.

A potent, dual class I PI3K/mTOR inhibitor with IC50 of 2/3/3/15/ for p110α/β/δ/γ, respectively.

RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53.

A potent, full dopamine D1 agonist.

A potent, functionally selective TSH receptor (TSHR) positive allosteric modulator with EC50 of 11.6 uM (β-Arr 1 translocation).

A potent, highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 4 nM for CK1δ.

PF04802367 is a potent, highly selective GSK-3 inhibitor with IC50 of 2.1 nM for human GSK-3β in enzyme assays; shows equal effectivity against GSK-3α and GSK-3β with IC50 of 10.0 and 9.0 nM respectively in mobility shift assays, inhibits phosphorylation of tau with an IC50 of 466 nM in a stable inducible CHO cell line over-expressing GSK-3β and substrate tau; modulates tau phosphorylation in vitro and in vivo.

A potent, highly selective, ATP-competitive ROCK inhibitor with IC50 of 0.5/1.1 nM for ROCK1/ROCK2 respectively.

A potent, highly selective, peptide bombesin receptor subtype-3 (BRS-3) antagonist with IC50 of 2-8 nM for human and rodent BRS-3, displays 1000-fold selectivity over hNMBR and hGRPR, increases food intake and produces an obesity phenotype in mice..

A potent, long lasting 5-HT(1B/1D) receptor agonist as a antimigraine agent..

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.

A potent, noncovalent SARS-CoV papain-like protease (PLpro) inhibitor with IC50 of 2.6 uM.

A potent, non-prostanoid prostacyclin partial agonist that potently inhibits human (IC50=35 nM), rabbit (IC50=136 nM) and rat (IC50=1.3 uM) platelet aggregation.

A potent, orally active microsomal triglyceride transfer protein (MTP) inhibitor that inhibits both human and rodent MTP with IC50 of 2 nM.

A potent, orally active pan-inhibitor of HIF prolyl hydroxylase (HIF-PHD) with IC50 of 1.0,1.0, and 14 nM for HIF-PHD1, 2, and 3, respectively.

A potent, orally bioactive 20S proteasome inhibitor with IC50 of 1.3 nM (inhibition of proteasomal chymotrypsin-like proteolytic activity).

Cavosonstat is a potent, orally bioavailable inhibitor of S-nitrosoglutathione reductase (GSNOR) and CFTR modulator.

A potent, orally-active MEK1/2 inhibitor with IC50 of 10-100 nM.

RC-3095 is a gastrin-releasing peptide receptor antagonist, synergizes with gemcitabine to inhibit the growth of human pancreatic cancer CFPAC-1 in vitro and in vivo. RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. RC3095 inhibits tumor growth and decrease the levels and mRNA expression of epidermal growth factor receptors in H-69 small cell lung carcinoma.R,BRS-1) antagonist.

GNF-351 is a potent, pure aryl hydrocarbon receptor (AHR) antagonist (IC50=62 nM) devoid of partial agonist potential; antagonizes agonist and SAhRM-mediated suppression of SAA1, inhibit both DRE-dependent and -independent activity; decreases migration and invasion of HNSCC cells and prevents benzo[a]pyrene-mediated induction of the chemotherapy efflux protein ABCG2.

A potent, selective 5-HT2A receptor antagonist with Ki of 0.36 nM, > 80-fold selectivity for 5-HT2A over other serotonergic receptors.

A potent, selective 5-HT2B receptor agonist with pKi of 7.1, >10-fold selectivity over 5-HT2A, 5-HT2C, and other 5-HT subtypes.

A potent, selective agonist of 5-HT1A and 5-HT1B receptors, with preference for 5-HT1B.

A potent, selective and ATP-competitive CK2 inhibitor with Ki of 0.5-1 uM.

A potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist with Ki of 1.4 nM, 100-fold selectiivity over CRF1.

A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM.

A potent, selective and orally active blocker of voltage-gated potassium channels Kv7 (KCNQ) that blocks KCNQ1, KCNQ2 and KCNQ2+KCNQ3 with Kd of 0.78, 0.7 and 0.6 uM, respectively.

NI-42 is a potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs; weakly inhibits BRPF2 (BRD1), BRPF3, BRD9 and BRD4 (BD1) with IC50 of 48, 260, 310 and 4500 nM respectively, and no activity for ATAD2A/2B (IC50>100 uM); shows a modest (GI50=1-10 uM) and selective inhibition of proliferation of certain cancer lines, particularly those lines exhibiting monocytic lineage differentiation; a novel, structurally orthogonal chemical probe for the BRPFs suitable for cellular and in vivo studies.

A potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM.

A potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively.

A potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM.

A potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway.

A potent, selective cannabinoid receptor CB2 agonist with Ki of 7.1 nM, >80-fold selectivity over CB1 receptors in radioligand binding assay.

A potent, selective competitive and nonpeptide PAR-1 antagonist with IC50 of 70 nM.

A potent, selective dual mTORC1 and mTORC2 inhibitor with enzyme IC50 of 1.5 nM.

PU-H54 is potent, selective Grp94 inhibitor.

ML-T531 is a potent, selective hERG potassium channel (Kv11.1) activator with EC50 of 3.13 uM.

A potent, selective human Arginase inhibitor with Ki of 0.25 uM (pH=7.5), 8.5 nM (pH=9.5) for type II arginase.

Bay-8040 is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 28 nM; displays no significant inhibition toward 68 other pharmacologically relevant targets (>10 uM), and a panel of related serine proteases; shows in vivo efficacy with regard to decreasing cardiac remodeling and amelioration of cardiac function in monocrotaline-induced rat model for pulmonary arterial hypertension.

A potent, selective inhibitor of human LIMK1 with IC50 of 38 nM .

CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression.

A potent, selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.

CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM; displays selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, and a panel of 55 other receptors; restores impaired Cl(-) transport i

A potent, selective KDM5 sub-family(JARID1) inhibitor with biochemical IC50 of 71/19/69/69 nM for KDM5A/B/C/D, respectively.

A potent, selective ligand for the mitochondrial translocator protein 18kDa (TSPO/PBR).

EPPTB is a selective antagonist of the trace amine-associated receptor 1 (TAAR1).

A potent, selective N-methyl-D-aspartate (NMDA) antagonist with selectivity for the NR2B subunit.

A potent, selective OX1 receptor antagonist with Ki of 57 nM (whole cell assay), and 27 nM (cell membrane-based SPA assay).

A potent, selective small molecule inhibitor of transcription factor STAT5b with Ki of 44 nM, >50-fold selectivity over STAT5a..

PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. IC50 value: 2 nM (EC50) [1]in vitro: blocks Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 of 2 nM, by preferentially binding to the C-type inactivated state of the channel. PAP-1 is 23-fold selective over Kv1.5, 33- to 125-fold selective over other Kv1-family channels, and 500- to 7500-fold selective over Kv2.1, Kv3.1, Kv3.2, Kv4.2, HERG, calcium-activated K+ channels, Na+,Ca2+, and Cl- channels [1]. The blockade of Kv1.3 results in membrane depolarization and inhibition of TEM proliferation and function. In this study, the in vitro effects of PAP-1 on T cells and the in vivo toxicity and pharmacokinetics (PK) were examined in rhesus macaques (RM) with the ultimate aim of utilizing PAP-1 to define the role of TEMs in RM infected with simian immunodeficiency virus (SIV). Electrophysiologic studies on T cells in RM revealed a Kv1.3 expression pattern similar to that in human T cells. Thus, PAP-1 effectively suppressed TEM proliferation in RM [2].in vivo: PAP-1 does not exhibit cytotoxic or phototoxic effects, is negative in the Ames test, and affects cytochrome P450-dependent enzymes only at micromolar concentrations. PAP-1 potently inhibits the proliferation of human TEM cells and suppresses delayed type hypersensitivity, a TEM cell-mediated reaction, in rats [1]. When administered intravenously, PAP-1 showed a half-life of 6.4 hrs; the volume of distribution suggested extensive distribution into extravascular compartments. When orally administered, PAP-1 was efficiently absorbed. Plasma concentrations in RM undergoing a 30-day, chronic dosing study indicated that PAP-1 levels suppressive to TEMs in vitro can be achieved and maintained in vivo at a non-toxic dose [2].

A potent, selective sodium-coupled citrate transporter (NaCT or SLC13A5) with IC50 of 0.51 uM, >20-fold selectivity over NaDC1 and NaDC3.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.28 uM.

A potent, selective α2A-adrenoceptor antagonist with Ki of 1.7 nM, 80-fold selectivity over α2B-adrenergic receptors.

A potent, selective, allosteric and oral mGluR1 antaognist with IC50 of 2.6 and 2.3 nM for human and rat mGluR1, respectively.

A potent, selective, allosteric and orally acitve positive modulator of small-conductance calcium-activated K+ channel KCa2.2 and KCa2.3 with EC50 of 1.6 and 0.14 uM, respectively.

A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36.

A potent, selective, brain penetrant PDE10A inhibitor with Ki of 4 nM.

BAY-678 is a cell-permeable inhibitor of human neutrophil elastase (HNE).

A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 260 nM.

SW106 is a potent, selective, competitive PTH/PTH-related peptide receptor (PPR) antagonist with IC50 of 0.99 uM.

A potent, selective, noncompetitive inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) with IC50 of 7 uM.

A potent, selective, non-pseudosubstrate inhibitor of O(6) -alkylguanine DNA methyltransferase (MGMT) with low-nanomolar potency.

A potent, selective, non-RGD-mimetic αIIbβ3 integrin receptor antagonist with IC50 of 45 nM, with no activity on αVβ3 receptors. .

A potent, selective, orally active cannabinoid CB2 receptor inverse agonist with Ki of 35.9, 1.55 and 0.38 nM for human, mouse and rat CB2, respectively.

A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM.

PF-1355 is a potent, selective, orally active Myeloperoxidase (MPO) inhibitor with EC50 of 1.47 uM.