TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes.

Apoptozole is an inhibitor of heat shock protein 70 (Hsp70; 65% inhibition at 200 μM) that acts by blocking its ATPase activity.

FAPI-34 is a fibroblast-activating protein (FAP) inhibitor with favorable pharmacokinetic and biochemical properties. (patent WO2019154886A1).

A293 (AVE1231) is a potent and antiarrhythmic compound and selective inhibitor of two-pore-domain potassium channel TASK-1 (KCNK3, hK2P3.1).A293 (AVE1231) is an inhibitor of hKv1.5 currents with predominant action on channels in their open state.A293 (1 uM) prominently depolarized arterial smooth muscle and increased basal tone level and contractile responses to methoxamine of arteries from young rats but had almost no effect in adult rats.Pharmacological inhibition of atrial TASK-1 currents via A293 (AVE1231) exerts antiarrhythmic effects in vivo as well as in silico, resulting in acute cardioversion of paroxysmal trial fibrillation (AF).

TBA-7371 (TBA7371, AZ 7371) is a potent, non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) with IC50 of 10 nM, an enzyme involved in mycobacterial cell wall biogenesis.TBA-7371 also inhibits PDE6 with an IC50 value of 4 uM.TBA-7371 is active against M. tuberculosis with an MIC range of 0.78-3.12 µM and demonstrates efficacy in a rodent model of tuberculosis.

BDM44768 (BDM 44768) is a potent, selective catalytic site inhibitor of insulin-degrading enzyme (IDE) with IC50 of 60 nM (hIDE). BDM44768 displays excellent selectivity over a panel of metalloproteases (>45-fold selectivity over hNEP and hECE, no significant acitivity against hACE and hMMP-1). BDM44768 significantly increased concentrations of Aβ1-40 in culture supernatants of human SY5Y neuroblastoma cells. Acute treatment of mice with BDM44768 (50 mg/kg, i.p.) increases insulin signalling and surprisingly impairs glucose tolerance in an IDE-dependent manner in C57BL/6J mice.

GLPG2451 (GLPG 2451) is a potent potentiator of cystic fibrosis transmembrane conductance regulator (CFTR) with EC50 of 11 nM for F508del CFTR in the YHA assay and EC50 of 18 nM in TECC assay using HBE cells from patients carrying the F508del mutation. GLPG2451 improves the gating function of the CFTR channel.

MR120 (CCR6 antagonist 1b) is a potent, selective CCR6 antagonist, disrupts the CCL20-induced chemotaxis of CCR6+CD4+ T cells.

SB699551 is a potent, selective 5-HT5A receptor antagonist with pKi of 8.3, >100-fold selectivity over 5-HT1B/D, 5-HT2A, 5-HT2C, 5-HT1A and 5-HT7 receptors. SB699551 also is a novel PSMD4/Rpn10 inhibitor, decreases cell viability in MM cell lines.

Vidofludimus (IMU-838) is a selective and potent second-generation dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 160 nM, shows anti-SARS-CoV-2 activity with EC50 of 7.6 uM in Vero cells. Vidofludimus inhibits T cell proliferation with EC50 of 11.8 uM, with a similar effect on CpG ODN 2006-PTO dependent B cell proliferation. Vidofludimus is specific for human DHODH and does not have off-target effect on kinases, is about 7.5-fold and about 64.4-fold more active on human DHODH as compared to rat DHODH and mouse DHODH, respectively. Vidofludimus inhibits specifically IL–17F, IL–17A and IFN-g expression in PBMCs. Vidofludimus is 2.6 times more potent in inhibiting DHO oxidation by human DHODH compared to teriflunomide (IC50=420 nM). Vidofludimus shows inhibition of rat EAE motor signs in a rat experimental autoimmune encephalomyelitis (EAE) model. Vidofludimus exerts a broad-spectrum activity against a selection of major human pathogenic viruses.

BDM88951 (BDM 88951) is a highly potent, selective inhibitor of endoplasmic reticulum aminopeptidase 2 (ERAP2) with IC50 of 19 nM. BDM88951 displays selectivity index (>150) towards closely related ERAP1 and IRAP enzymes, as well as MMPs, TACE and LAP3. BDM88951 is a potent inhibitor of ERAP2-mediated hydrolysis of two nonapeptides precursors of SIINFEKL, an ovalbumine-derived antigen, in a dose dependent manner. BDM88951 engage ERAP2 in cells and inhibits antigen presentation in a cellular context, also displays favorable in vitro ADME properties and in vivo exposure.

FT709 is a potent and selective USP9X inhibitor, an IC50 of 82 nM. USP9X has been linked with centrosome function, chromosome alignment during mitosis, EGF receptor degradation, chemo-sensitization, and circadian rhythms.

Zastaprazan is a proton pump inhibitor (WO2018008929). Zastaprazan can be used for the research of gastrointestinal inflammatory diseases or gastric acid-related diseases.

O4I4 (compound 23) is a OCT4-inducing compound with metabolical stability.

AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

MO-I-1182 is a small molecule inhibitor of aspartate beta-hydroxylase (ASPH), suppresses cholangiocarcinoma metastasis.

BMS-708163 is a potent, selective γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, respectively.

IKAM-1 (Compound 39-100) is an orally bioavailable, small-molecule IKKβ activation modulator (IKAM) that selectively targets MAP3K1, inhibits TNF-α-induced IKKβ-mediated NF-κB activation in A549 cells with IC50 of 4.7 uM.

Vafidemstat (ORY-2001) is an oral, brain penetrant drug that inhibits LSD1 and MAOB by reducing cognitive impairment, including memory loss and neuroinflammation. It also has neuroprotective effects.

Mafodotin, also known as mc-MMAF and SGD-1269 or Maleimidocaproyl monomethylauristatin F, is a MMAF derivative having a Maleimidocaproyl linker (MC linker), which is ready to conjugate to antibody or other proteins or biopolymers. Mafodotin is a useful a

RBF197 (RBF-197) is a novel highly potent and selective eIF4A inhibitor, inhibits human eIF4A helicase activity with IC50 of 55.2 pM.

HLQ2H (Msi3 inhibitor 2H) is a first-in-class, specific inhibitor of fungal Hsp110 molecular chaperone Msi3, inhibits the holdase activity of Msi3 (IC50=5.02 uM) as well as the growth and viability of C. albicans.

PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.

SSR125543 (Crinecerfont, SSR-125543) is a potent, nonpeptide, orally active corticotropin-releasing factor (CRF) receptor CRF1 antagonist, shows anxiolytic- and antidepressant-like activities in vivo. .

GLP-1(7-36), amide is a physiological incretin hormone that stimulates insulin secretion.

​​X-376​​ is a highly selective and potent inhibitor of ​​ALK (anaplastic lymphoma kinase) tyrosine kinase​​, demonstrating strong activity with an ​​IC50 of 0.61 nM​​. While it primarily targets ALK, it also exhibits inhibitory effects on ​​MET kinase​​, though with slightly reduced potency (IC50 = 0.69 nM). Due to its robust kinase-blocking properties, X-376 shows significant ​​anti-tumor efficacy​​, making it a promising candidate for cancer research and therapeutic development.

Ensartinib, also known as X-396, is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, X-396 binds to and inhibits ALK kinase, ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development.

J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA is used for the relief of mechanical allodynia and mechanical hyperalg

Devazepide is a potent, and orally active CCK1 (CCK-A) receptor antagonist that displays appetite-stimulant effects. It blocks the anorectic response to CCK-8 and increases food intake in rats following systemic and i.c.v administration.