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.