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.

A potent and selective linear tachykinin NK2 receptor antagonist with pKb of 9.3.

A potent and selective MCH-R1 antagonist with IC50 of 22 nM, Ki of 14 nM.

A potent and selective melanocortin 4 receptor (MC4R) agonist with EC50 of 2.1 nM.

A potent and selective mTOR inhibitor with Ki of 1.5 nM.

A potent and selective NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 22 nM, >200-fold selectivity over Plk1, Mps1, Aurora A and CDK2.

A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor.

A potent and selective PDE10A inhibitor with binding affinity (Kd) of 0.15 nM, IC50 of 2.11 nM.

A potent and selective PDE10A inhibitor with IC50 of 7.28 nM.

A potent and selective RARγ receptor agonist with Ki of 150 nM.

A potent and selective ROCK inhibitor with Ki of 1.6 nM.

A potent and selective small molecule chemical probe of a methyl-lysine reader protein L3MBTL3 with Ki of 0.35 uM.