GSK1059865 is a potent orexin 1 receptor antagonist.

Potent hSirt3 Inhibitor

A potent and selective Adenosine receptor A2A agonist

HDAC-IN-4 is a selective HDAC6 and HDAC10 inhibitor with pIC50s of 7.2 and 6.8 in BRET assay, respectively. Antitumoral activity.

GalR2-positive allosteric modulator

Potent mGluR5 PAM modulator

VMAT2 ligand, stimulating dopamine release, inhibiting the reuptake of dopamine and serotonin, acting as a mixed agonist-antagonist at nicotinic acetylcholine receptors and antagonist at µ-opioid receptors

ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively.

Novel Orally Available Polymerase Inhibitor, Showing Efficacy Against a Lethal Morbillivirus Infection in a Large Animal Model

Novel glucocerebrosidase activator; Non-inhibitory chaperones of glucocerebrosidase

Novel Inhibitor of Monoubiquitinated Proliferating Cell Nuclear Antigen (PCNA), inhibiting Repair of Interstrand DNA Crosslink, enhancing DNA Double-strand Break, and sensitizing Cancer Cells to Cisplatin.

Novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe

9-Hydroxycanthin-6-one is an alkaloid compound. 9,10-Dimethoxycanthin-6-one exhibits NF-κB inhibitory effects with an IC50 of 3.8 μM.

RY785 is a potent and selective voltage-gated potassium (KV2) channel inhibitor with an IC50 of 0.05 μM for KV2.2. RY785 has analgesic activity[1].

Potent, allosteric GPR55 antagonist

First reported nonpeptidomimetic agonist on the G protein-coupled chemokine receptor CXCR-3

Novel Multitarget Modulator of Alzheimer's Disease

Antagonist for G-protein Coupled Receptor 7 (GPR7)

Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction

Competitive inhibitor of secretory phospholipase A2 (sPLA2)

Novel allosteric agonist of Sphingosine 1-phosphate receptor 2 (S1PR2)

First-in-class Haspin inhibitor with a wide spectrum of anticancer effects