A potent and selective HDAC3 inhibitor with IC50 of 0.26 uM, with no activity against HDAC1/4/6/8.

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.

A potent and selective inhibitor of LTA4 hydrolase (LTA4H) with IC50/Ki of 5 nM/23 nM.

A potent and selective inhibitor of mediator-associated kinase CDK8 (IC50=12 nM) and its paralogue CDK19.

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 MTH1 protein with IC50 of 5 nM.

A potent and selective inhibitor of neutral endopeptidase (NEP) with IC50 of 18.9 nM for hNEP.

A potent and selective inhibitor of PDGFR with IC50 of about 0.4 uM both in vitro and in cells.

A potent and selective inhibitor of sterol O-acyltransferase 2 (SOAT2, ACAT2) with IC50 of 11.8 nM, >6,000-fold selectivity over ACAT1.

A potent and selective inhibitor of the MDM2-p53 interaction with Kd of 38 pM, and IC50 of 1.6 nM.

A potent and selective inhibitors of leukotriene C4 synthase (LTC4S) with IC50 of 95 nM, Ki of 6 nM.

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.