THK-5470(THK 5470), a monoamine oxidase-B (MAO-B) imaging probe, could be used for neurological diseases study. THK-5470 shows remarkably high binding affinity against MAO-B with an IC50 value of 4.2 nM, low binding affinity against tau with an IC50 value of 4462 nM. THK-5470 has high selective binding property and high affinity (from patent EP2019-846498).

DI-87 ((R)-DI-87) is a highly potent, specific, orally bioavailable deoxycytidine kinase (dCK) inhibitor with IC50 of 3.15 nM.

FT234 (FT-234) is a selective HDAC11 inhibitor.FT234 demonstrated significant reduction in self-renewal stem-like SP cells with 2 uM FT234 or FT895, as well as the formation of vascular networks by SP cells at 5 uM compound treatment.FT234 significantly decreased the mRNA of Sox2 as well as its target genes like HK2 and PDK2 in SPAdh cells.FT234 compound inhibited the growth and viability by 60–80% in both A549 and H1650 cells at 5-10 uM, inhibited the viability of cancer cell lines A549 and H1650 ranged from 4.663–6.594 uM, reduced the viability of chemo-resistant cancer cells as well as chemo-insensitive CSCs.FT234 selectively prevent growth of cancer cells in presence of cancer associated fibroblasts (CAFs).

LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.

DBCO-PEG4-acid is a PEG Linker. PEG Linkers may be useful in the development of antibody drug conjugates.

(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM.

cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.

3’3’-cGAMP Fluorinated (c-[2'FdGMP]-[2'FdAMP]) is a synthetic analog of cyclic guanosine monophosphate- adenosine monophosphate (cyclic GMP-AMP, cGAMP) with a fluorine atom at 2’ position of the nucleosides. 3’3’-cGAMP is a cyclic di-nucleotide produced by bacteria. It is also referred to as "canonical" cGAMP due the presence of the classical 3’-5’ phosphodiester linkages between the guanosine and the adenosine. It has been reported that cGAMP binds STING (stimulator of IFN genes) and subsequently induces TBK1-IRF3-dependent production of IFN-β [1]. The incorporation of fluorine into biologically active molecules is commonly used in medicinal chemistry to improve their metabolic stability or to modulate physicochemical properties such as lipophilicity [2, 3]. Moreover, the introduction of a fluorine atom can change the biological activities of a molecule. Interestingly, when used at low concentrations in various cellular assays, 3’3’-cGAMP Fluorinated induces higher levels of type I IFNs than does cGAMP. STING ligands such as cGAMP induce type I IFNs and activate interferon stimulated genes (ISG) through IRFs. To facilitate their study, InvivoGen has developed stable reporter cells in two well established immune cell models: THP-1 human monocytes and RAW 264.7 murine macrophages. These cells express a reporter gene (SEAP or Lucia luciferase), under control of an IRF-inducible promoter.

AZD8421 is a highly selective CDK2 inhibitor with IC50 of 9 nM and shows selectivity over CDK1, CDK4 and CDK6. AZD8421 shows robust monotherapy activity in a CCNE1 amplified ovarian model OVCAR3 with regressions seen with monotherapy and in combination with palbociclib.

BEBT-809 is a GPR75 antagonist for rat CYP4F2 and CYP4A11 with IC50 of and 15.76 nM and 33.16 nM, respectively.

Tat-NR2B9c (NA-1) is a neuroprotective agent.

VVD-214 (RO7589831) is a synthetic lethal allosteric inhibitor of WRN helicase. VD-214 covalently engages cysteine 727 of WRN in a nucleotide cooperative manner and inhibits ATP hydrolysis and helicase activity, resulting in widespread double-stranded DNA breaks, nuclear swelling, and cell death in MSI-high, but not microsatellite stable cells.

ABBV-303 is a novel c-Met targeted multispecific NK cell engager. ABBV-303 binding to NKG2D and CD16a results in redirection of both innate (NK cells) and adaptive (CD8+ T cells) immune cells to lyse c-Met expressing tumor cells.

A-1155463 is a highly potent and selective BCL-XL inhibitor.

LUNA18 is an 11-mer cyclic peptide inhibitor for the intracellular tough target RAS with Kd (KRAS/G12D) of 0.043 nM and cellular IC50 of 1.4 nM (AsPC-1). LUNA18 orally and dose-dependently exhibits potent anti-cancer activities in a mouse xenograft model. LUNA18 shows 21–47% oral bioavailability in animals such as mouse, rat, monkey, and dog and notably does not require special formulations.

A potent and selective Adenosine receptor A2A agonist

Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.

A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) full agonist with EC50 of 18 nM, >500-fold selectivity over human adrenergic α2A receptor.

LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.

JMV 2959 (AEZS-123) is a potent ghrelin receptor (GHS-R1A) antaognist with binding IC50 of 32 nM.

Nutlin-3a is arbitrarily referred to as enantiomer a because it appears as the first peak from chiral purification of racemic nutlin-3 and its absolute stereocenter assignment is not known.

IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma.

Netarsudil (AR-13324) is a potent, selective ROCK inhibitor with Ki of 4.2 nM for ROCK2.

PF-03758309 is an orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity.

CWHM-12 a novel small molecule inhibitor of αV integrins with IC50s of 1.8/0.8/1.5/0.2 nM for αvβ1/αvβ3/αvβ8; less potency on αvβ5(IC50=61 nM) and on inhibition on αIIbβ3/α2β1/α10β1.

Fmk is an irreversible ribosomal S6 kinase inhibitor 1/2 inhibitor.

A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM).

Nutlin 3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.

CFI-400945 is a potent, highly selective PLK4 inhibitor with Ki of 0.26 nM and IC50 of 2.8 nM, does not significantly inhibits PLK1/2/3 at 50 uM; causes dysregulated centriole duplication, mitotic defects, and cell death in multiple cancer cell lines (A549 GI50=5 nM, OVCAR-3 GI50=18 nM); significantly inhibits human cancer xenografts; causes polyploidy, growth inhibition, and apoptotic death of murine and human lung cancer cells, despite expression of mutated KRAS or p53, produces supernumerary centrosomes and mitotic defects in lung cancer cells.

Birinapant (TL32711) is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM, less potent to XIAP.