A potent and selective antagonist of H3 receptor with Ki/EC50 of 0.16/1.5 nM.

A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM.

A potent and selective Chk2 inhibitor with Ki/IC50 of 11 nM/120 nM.

A potent and selective dopamine D3 receptor antagonist with pKi of 8.0.

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.