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 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.