SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC50s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis.

LR-90 is an advanced glycation end product (AGE) inhibitor, inhibits inflammatory responses in human monocytes. LR-90 is also used in the research of diabetic animal model.

RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).

A potent inhibitor of MLL1/WDR5 protein-protein interaction with IC50 of 0.9 nM.

Velneperit, also known as S-2367, is potent and selective neuropeptide Y Y5-receptor antagonist under evaluating for treatment of obesity.

FOY 251 is a metabolite of Camostat and a pollen protease inhibitor for prevention and control of allergy.

Gemcitabine elaidate is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity.

BIA is a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca2+, further suppressing tumor formation and progression in cancer xenograft models.It is a potential anticancer agent that prevents the binding between mTORC2 and TMBIM6.

N-Methyl-N,N-bis(2-pyridylethyl)amine is used as a reagent in the preparation of copper pyridylmethylethylenediamine dicyanamido polymeric complexes.

TGR-1202 is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.

ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 of 20.04 nM measured as percentage of NRAS phosphorylation; shows similar IC50 of 23.96 and 27.94 nM for STK19WTWT STK19D89N respectively; displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 uM; efficiently inhibits phosphorylation of NRAS in a dose- and time-dependent manner, inhibits NRAS activity in a dose-dependent manner but does not affect the levels of H3K9 methylation; effectively inhibits NRAS signaling, including the MEK-ERK and PI3K pathways in SK-MEL-2 and WM2032 cells (with NRASQ61R), but the inhibition was much less effective in A375 or UACC62 cells (with NRASWT), effectively inhibits cell growth and induces apoptosis of SK-MEL-2 and WM2032 melanoma cells.

ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.

STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.

Asciminib (ABL-001) is a potent and selective allosteric ABL1 inhibitor with IC50 of 0.25 nM in BCR–ABL1-transformed BaF3 cells.

Maytansinol inhibits microtubule assembly and induces microtubule disassembly in vitro. Target: Microtubule/Tubulin in vitro: Maytansinol disrupts the mitotic spindle and prevents mitotic exit in Drosophila. Maytansinol reduces the growth and/or survival of HCT116 cells in a dose-dependent manner and that the effect was more severe for p53+/+ than for p53-/- cells at both low and high doses. Maytansinol inhibits the growth of HCT116 human colon cancer cells. Maytansinol induces apoptosis in imaginal discs of wild-type larvae but not p53 mutant larvae. This parallels the finding in human HCT116 cells, in which Maytansinol was more effective when p53 was present, at least at some doses. Maytansinol induces apoptosis in imaginal discs of wild-type larvae but not p53 mutant larvae at 24 hours after exposure to drug.

RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.

A small molecule inhibitor of trans-translation that has broad-spectrum antibiotic activity.

CX546 is an AMPA receptor potentiator and GluR activator, binds specifically to the agonist bound non-desensitized receptor.

TH-257 (TH257) is a potent, selective, allosteric inhibitor of LIMK1 and LIMK2 with IC50 of 84 nM for LIMK1 and 39 nM for LIMK2 in a RapidFire MS assay.

AZD-7325 is a potent, α2/3 functionally selective, partial GABAA receptor modulator with pKi of 9.51.

BTZ043 racemate is a decaprenylphosphoryl-β-D-ribose 2-epimerase (DprE1) inhibitor acting as a new antimycobacterial agent that kill Mycobacterium tuberculosis.

CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM.

WHI-P97 is a rationally designed potent inhibitor of JAK-3.

A highly potent sigma receptor agonist with Ki of 1.7 nM and 25.2 nM for σ1 and σ2, respectively.

CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.

AKOS B018304 is an arylalkylidene derivative, with polar substitution at para-position.

URB937 is a potent fatty acid amide hydrolase (FAAH) inhibitor (IC50 = 26.8 nM, in vitro) that does not penetrate the blood-brain barrier, thus preventing arachidonoyl ethanolamidedeactivation only in peripheral tissues.

GNE-8324 is a potent and selective NMDA receptor PAM.

VU 0465350 is a potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 92.3 nM; shows no activity for ALK2/4/5, also shows affinity for TGFBR2, VEGFR2 and AMPK; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.

MI-2-2 is a potent inhibitor of the menin-MLL interaction that binds to menin with low nanomolar affinity (Kd=22 nM); inhibits the interaction of menin with MLL-AF9 in HEK293 cells in a dose-dependent manner with 4-fold potentcy improvement over MI-2; suppresses growth of MLL-AF9–transformed BMCs; causes MV4:11 cells growth inhibition of with GI50 of 3 uM.