GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.

NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.

Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α’s RNase.

WAY-647802 is a CDK inhibitor.

JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM.

Potent mGluR5 PAM modulator

CP-24879 hydrochloride is a D5D/D6D dual-inhibitor, showing beneficial effects against increased intracellular lipid accumulation and inflammatory injury in hepatocytes.

FGIN-1-27 is an anxiolytic compound that acts as a selective agonist at the peripheral benzodiazepine receptor (TSPO).FGIN-1-27 inhibited Th17 cell differentiation, significantly downregulated the expression of RORγt target genes, notably Il17a, Il17f, Il23r, Ltb4r1,Ccr6.FGIN-1-27 protected mice against EAE, induced amino acid starvation response (AAR), FGIN-1-27 produced anti-anxiety and anti-panic effects in non-mammalian models.

SR2640 (hydrochloride) is a potent and selective competitive leukotriene D4/leukotriene E4 antagonist. SR2640 can be used for researching the role of leukotrienes in human asthma.

A novel LTA4 hydrolase (LTA4H) inhibitor that inhibits LTB4 synthesis in human neutrophils with IC50 of 0.5 uM.

A novel FTY720 analog that acts as PP2A activator, disrupts the SET/PP2A interaction devoid of immunosuppressive effects leads to the reactivation of PP2A.

FEN1-IN-SC13 is a potent DNA fragmentation endonuclease 1 (FEN1) inhibitor (CN106692155A, SC13).

Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA).

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

AM-2232 is a drug that acts as a potent but unselective agonist for the cannabinoid receptors.

Tocainide hydrochloride is an orally activesodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus.

SB02024 is a novel highly potent, selective, ATP competitive, orally active inhibitor of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times selective towards other PI3K isoenzymes; SB02024 is also highly selective at 1 uM in the DiscoveRx ScanMax panel of 468 kinases; reduces the number of GFP-2xFYVE puncta with IC50 of 14 nM, induces a dose-dependent increase in levels of NCOA4 and p62; blocks autophagy in vitro and reduces xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7; also significantly potentiates cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro.

Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor.

MRS 1845 is a potent calcium channel protein inhibitor and inhibits capacitative Ca2+ influx in HL-60 cells (IC50 = 1.7 mM).

Guanabenz (WY 8678) is an α2 adrenergic receptor agonist that is used as an antihypertensive agent, also has been proposed to exert protective effects against misfolding by interfering with eIF2α-P dephosphorylation through selective disruption of a PP1-P

PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.

J14 is a reversible sulfiredoxin inhibitor with an IC50 of 8.1 μM. J14 induces oxidative stress (intracellular ROS accumulation) by inhibiting sulfiredoxin, leading to cytotoxicity and cancer cell death.

The product is discontinued. DDD107498, also known as DDD 498, is a multiple-stage antimalarial agent that inhibits protein synthesis. DDD107498 demonstrates potential to address a variety of clinical needs, including single-dose treatment, transmission blocking and chemoprotection. DDD107498 was developed from a screening programme against blood-stage malaria parasites; its molecular target has been identified as translation elongation factor 2 (eEF2), which is responsible for the GTP-dependent translocation of the ribosome along messenger RNA, and is essential for protein synthesis. This discovery of eEF2 as a viable antimalarial drug target opens up new possibilities for drug discovery.

ML 204 isa blocker of TRPC4 channels (IC50 values are 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively).

ML 792 is a potent, seletive SUMO-activating enzyme (SAE) inhibitor with IC50 of 3 nM and 11 nM for SAE/SUMO1 and SAE/SUMO2, respectively.

ML092 is a covalent and reversible Cruzain inhibitor, with an IC50 of 10 nM.