TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.

BC1618 is a novel Fbxo48 inhibitor and prevent pAmpkα degradation with MEC (minimal efficacious concentration) of 0.6 μM.

LOXO-305 is an investigational, novel, selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. LOXO-305 was designed to reversibly bind BTK, preserve activity in the presence of the acquired resistance, and avoid off-target kinases that have complicated the development of both covalent and investigational non-covalent BTK inhibitors.LOXO-305 is a highly selective, non-covalent BTKi that inhibits both wild type (WT) and C481-mutated BTK with equal low nM potency was developed.

JMX0493 is a potent inhibitor of human adenoviruses (HAdVs) with IC50 of 0.78 μM and displays high selectivity index (SI>100) and 2.5-fold virus yield reduction compared to niclosamide. JMX0493 targets the HAdV entry pathway that prevents viral particle disassembly and subsequent release from the endosome.

ACH-000143 is a novel potent melatonin receptor agonist with EC50 of 0.06 nM/0.32 nM against MT1/MT2. ACH-000143 leads to a reduction in body weight gain similar to dapagliflozin with superior results on hepatic steatosis and triglyceride levels in high-fat diet rats.

Compound 5i is a novel and brain-penetrant O-GlcNAcase inhibitor with IC50 of 46 nM.

Deruxtecan, a topoisomerase I inhibitor, is an exatecan derivative (DX-8951 derivative) with a cleavable pepetide linker and a maleimide group. The maleimide group in Deruxtecan can react with antibody to form antibody-drug conguates (ADC) such as Trastuzumab deruxtecan (DS-8201a), which is a HER2-targeting antibody–drug conjugate.

GSK-114 is a potent and selective selective TNNI3K inhibitor (TNNI3 IC50 = 25nM; B-RafV600E IC50 = 1000 nM). GSK-114 displays significant bias (40-fold) for TNNI3K over B-Raf, exceptional broad spectrum kinase selectivity, and adequate oral exposure to en

ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

Laninamivir (L174000) prodrug; a novel long-acting neuraminidase inhibitor.

GRL-1720 is an irreversible, covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 15 µM.

CU-CPT17e shows strong NF-κB activation in TLR3, TLR8 and TLR9 HEK293 cells with EC50 values of 4.80±0.73, 13.5±0.58 and 5.66±0.17 μM, respectively. CU-CPT17e significantly improves the activity with 13.9±0.9 fold of NF-κB activation and an EC50 value of 4.8±0.7 μM. CU-CPT17e inhibits the proliferation of HeLa cancer cells by triggering apoptosis and arresting the cell cycle at the S phase. The induction of apoptosis by CU-CPT17e in HeLa cells is investigated. HeLa cells are cultured with increasing concentrations of CU-CPT17e or poly I:C or blank control (DMSO) for 24 h. Treatment with CU-CPT17e for 24 h at different concentrations (10 to 40 μM) results in an elevation of apoptotic cell population ranging from 10% to 17%, which is more effective than poly I:C at 5 μg/mL. These results suggest that the antiproliferative activity of CU-CPT17e against HeLa cells might result from its ability to directly induce apoptosis[1].

PF00835231(SARS-CoV-2 inhibitor 5h) is areversible-covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 4.2 µM. Compound 5h blocks the infectivity and cytopathicity of the virus with high potency and without any detectable cytotoxicity even at 200 µM.PF-00835231 is a potent inhibitor of CoV-2 3CLpro with IC50 of 4 nM and shows suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.

Rad150 is an esterized form of the compound RAD 140

PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on PROTAC. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).

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.

GNF-PF-3777 (8-Nitrotryptanthrin) is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 μM.

CA-4948 is a potent IRAK4/FLT3 inhibtor with anti-tumor activity[1].CA-4948 is over 500-fold more selective for IRAK-4 compared to IRAK-1. CA-4948 reduces TNF-α, IL-1β, IL-6 and IL-8 release from TLR-Stimulated THP-1 Cells with an IC50 <250 nM. CA-4948 al

9-(2-Deoxy-2-fluoroarabinofuranosyl)guanine|2'-FANA-G

Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.

Thalidomide-NH-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

Thalidomide-PEG2-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.