LY309887 is a novel and potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 6.5 nM, and has antitumor activity.

GNE-207 is a novel, potent, selective and orally bioavailable inhibitor of the bromodomain of CBP.  It has excellent CBP potency (CBP IC50 = 1 nM, MYC EC50 = 18 nM), a selectively index of >2500-fold against BRD4(1), and exhibits a good pharmacokinetic profile.

JNJ-47965567 is a novel, potent, centrally permeable, high affinity and selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), which is a ligand-gated ion channel. An increasing body of evidence suggests that the purinergic receptor P2X, ligand-gated ion channel, 7 (P2X7) in the CNS may play a key role in neuropsychiatry, neurodegeneration and chronic […]

GNE 5729 is a novel, potent, brain permeable positive allosteric modulator (PAM) and GluN2A subunit-selective of NMDAR with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively. The N-methyl-d-aspartate receptor (NMDAR) is an ionotropic glutamate receptor, gated by the endogenous coagonists glutamate and glycine, permeable to Ca2+ and […]

GSK1379725A (AU1) is the first small molecule selective for BPTF over Brd4, as an inhibitor of Brd4 and a selective BPTF ligand with Kd of 2.8 μM. AU1 is active in a cell-based reporter assay. No binding is detected with Brd4. Three new Brd4 inhibitors with submicromolar affinity were also discovered. Brd4 hits were validated […]

GNE 0723 is a novel, potent, brain permeable positive allosteric modulator (PAM) and GluN2A subunit-selective of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively. The N-methyl-d-aspartate receptor (NMDAR) is an ionotropic glutamate receptor, gated by the endogenous coagonists glutamate and glycine, permeable to Ca2+ and […]

LY285434 is a novel and potent angiotensin II receptor antagonist.

GNE684 is a novel and potent inhibitor of receptor interacting protein 1 (RIP1), it inhibits human RIP1 potently over than mouse and rat with IC50s of 21 nM, 189 nM and 691 nM, respectively. The kinase RIP1 acts in multiple signaling pathways to regulate inflammatory responses and it can trigger both apoptosis and necroptosis. Its […]

SCD1 Inhibitor is a novel, highly potent stearoyl-CoA desaturase1 (SCD1) inhibitor with the potential to be used for treating various diseases such as obesity, cancer, diabetes and acne. SCD1 is a rate-limiting enzyme in the conversion of saturated fatty acids to monounsaturated fatty acids.

Desciclovir is a prodrug of acyclovir, against viruses in the herpesvirus family.