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 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-1 entry inhibitor that blocks the gp120-CD4 interaction.

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.