A potent, orally active p38 MAPK inhibitor with IC50 of 50 nM, significantly decreases incidence of arthritis in mouse collagen-induced arthritis..

A potent, orally active pan-inhibitor of HIF prolyl hydroxylase (HIF-PHD) with IC50 of 1.0,1.0, and 14 nM for HIF-PHD1, 2, and 3, respectively.

A potent, orally active PfDHODH inhibitor (IC50=0.3 uM) with antimalarial activity.

A potent, orally active sigma receptor antaognist with Ki of 27 and 7 nM for σ1 and σ2, respectively.

A potent, orally active γ-secretase inhibitor with cell IC50 of 0.3 nM.

A potent, orally active, and irreversible pan-Caspase protease inhibitor with IC50 of <0.08 to 7 nM for inhibition of activated caspase 3, 6 and 8.

A potent, orally available, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 12 and 63 nM, respectively.

A potent, orally bioactive 20S proteasome inhibitor with IC50 of 1.3 nM (inhibition of proteasomal chymotrypsin-like proteolytic activity).

A potent, orally bioavailable brain‐penetrant, NR2B-selective NMDA receptor (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM respectively, with no off-target activity.

A potent, orally bioavailable dual CXCR2/CXCR1 receptor antagonist with IC50 of 1.3 nM and 7.3 nM, respectively.

A potent, orally bioavailable P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury..

A potent, orally bioavailable, dual Src/Abl kinase inhibitor with IC50 of 0.5, 0.4, 0.5 and <1 nM for Src, Lck, Yes and Bcr-Abl, respectively.

A potent, orally bioavailable, small-molecule inhibitor of HDM2/p53 protein-protein interaction.

RC-3095 is a gastrin-releasing peptide receptor antagonist, synergizes with gemcitabine to inhibit the growth of human pancreatic cancer CFPAC-1 in vitro and in vivo. RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. RC3095 inhibits tumor growth and decrease the levels and mRNA expression of epidermal growth factor receptors in H-69 small cell lung carcinoma.R,BRS-1) antagonist.

A potent, peptide-inhibitor of human chymase with Ki of 1 nM.

A potent, picomolar, dual inhibitor of Aurora A and B with IC50 of 0.02 and 0.03 nM, respectively.

A potent, picomolar, dual inhibitor of Aurora A and B with IC50 of 0.02 and 0.03 nM, respectively.

A potent, reasonably selective agonist of peripheral cannabinoid receptor with Ki of 11 nM for CB2, 22-fold selectivity over the psychoactive CB1 receptors (Ki=245 nM)..

A potent, reasonably selective cannabinoid CB2 agonist with Ki of 0.4 nM, 25-fold selectivity over CB1 receptor..

A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 280 nM.

A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 66 nM.

A potent, reversible type III inhibitor of SAHH (S-adenosyl-L-homocysteine hydrolase) with Ki of 17.9 nM.