Prostaglandin D 2 (PGD 2 ) is one of a family of biologically active lipids derived from arachidonic
acid via the action of COX-1 and COX-2. PGD 2 is released from mast cells and binds …

NKG2D (natural-killer group 2, member D) is a homodimeric transmembrane receptor that
plays an important role in NK, γδ + , and CD8 + T cell-mediated immune responses to …

GPR139 is an orphan G-protein–coupled receptor expressed in the central nervous system.
To identify its physiologic ligand, we measured GPR139 receptor activity from recombinant …

A series of novel, potent quinolinyl-derived imidazo[1,5-a]pyrazine IGF-IR (IGF-1R) inhibitors—most
notably, cis-3-(3-azetidin-1-ylmethylcyclobutyl)-1-(2-phenylquinolin-7-yl)imidazo[1,5-…

Transient receptor potential melastatin type 2 (TRPM2) is a cation channel activated by free
intracellular ADP-ribose and reactive oxygen species. TRPM2 signaling has been linked to …

A highly effective one-pot Friedländer quinoline synthesis from o-nitroarylcarbaldehydes
and ketones or aldehydes was developed and the scope and limitations of the method were …

A focused high throughput screening for GPR139 was completed for a select 100K
compounds, and new agonist leads were identified. Subsequent analysis and structure–activity …

The synthesis of a series of tricyclic antagonists for the prostaglandin D 2 receptor DP2 (CRTH2)
is disclosed. The activities of the compounds were evaluated in a human DP2 binding …

A series of amino analogs of 1,3-dihydro-1-phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-2H-indol-2-one
(1) were synthesized to improve aqueous solubility, while retaining high affinity for …

The discovery and optimization of a series of imidazo[1,5-a]pyrazine inhibitors of mTOR is
described. HTS hits were optimized for potency, selectivity and metabolic stability to provide …