DS39201083 is a potent novel analgesic without mu opioid agonist activity. DS39201083 had a unique bicyclic skeleton and was a more potent analgesic than conolidine, as revealed in the acetic acid-induced writhing test and formalin test in ddY mice. The compound showed no agonist activity at the mu opioid receptor.

NV-5440 is a novel cell penetrant, potent and selective class I glucose transporters (GLUT1) inhibitor, selectively inhibiting mTORC1

NC-1 is a novel highly active allosteric inhibitor of protein tyrosine phosphatase, non-receptor type 22 (PTPN22) which is a lymphoid-specific tyrosine phosphatase (LYP).

BMS-986260 is a potent, selective, and orally bioavailable TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 demonstrated functional activity in multiple TGFβ-dependent cellular assays, excellent kinome selectivity, favorable pharmacokinetic properties, and curative in vivo efficacy in combination with anti-PD-1 antibody in murine colorectal cancer (CRC) models.

Samidorphan, also known as ALKS-33 and RDC-0313, is an opioid modulator with μ-antagonist properties. It is under development by Alkermes for the treatment of major depressive disorder and possibly other psychiatric conditions.

Onvansertib fumarate is a A polo-like kinase 1 inhibitor, an antineoplastic

RK-582 is an orally efficacious spiroindolinone-based tankyrase inhibitor for the treatment of colon cancer. It exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered.

IACS-9439 is a potent, highly selective,and orally bioavailable CSF1R inhibitor. Treatment with IACS-9439 led to a dose-dependent reduction in macrophages,promoted macrophage polarization toward the M1 phenotype, and led to tumor growth inhibition in MC38 and PANC02 syngeneic tumor models.

MG-6267 is the first dual inhibitor of AChE and microRNA-15b biogenesis, protecting SH-SY5Y neuroblastoma cells from amyloid-beta (Aβ)-induced cytotoxicity

SSK1 is a senolytic prodrug, which was designed from gemcitabine, by chem. modifying gemcitabin to incorporate a site cleavable by SA-β-gal following delivery of the prodrug in vivo, to release the active parent drug gemcitabine. SSK1 can be used to reduce one or more symptoms associated with a Senescence-associated disease or disorder in a subject. SSK1 is specifically activated by β-gal and eliminates mouse and human senescent cells independently of senescence inducers and cell types. In aged mice, SSK1 effectively cleared senescent cells in different tissues, decreased the senescence- and age-associated gene signatures, attenuated low-grade local and systemic inflammation, and restored physical function.

ropsacitinib, also known as PF-06826647 and Tyk2-IN-8, is an orally administered, tyrosine kinase 2 (TYK2) inhibitor, that is in development with Pfizer for the treatment of plaque psoriasis and inflammatory bowel disease.

OP-5244 is a potent and orally bioavailable CD73 inhibitor.

Peptide5 is a connexin43 mimetic peptide. Peptide5 reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Peptide5 exhibits analgesic effects in models of neuropathic pain.

SPR519 is a potent dual inhibitor of PI3Kα and mTOR kinases with IC50 (PI3Kalpha) = 30 nM and IC50 (mTOR) = 10 nM. SPR519 exhibits an EC50 of low sub-micromolar range among various tested cancer cell lines such as A2780 (0.23 μM), PC3 (0.48 μM), and SKOV3 (0.50 μM).

Lenacapavir, also known as GS-6207, is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs). Lenacapavir demonstrated picomolar potency in vitro with no cross resistance to existing antiretroviral classes and potent antiviral activity in persons with HIV-1. In persons with HIV-1, there was no preexisting resistance to lenacapavir regardless of treatment history.

C5-RIBOTAC is a RIBOTAC degrader, targeting the SARS-CoV-2 RNA genome

CG416 is a tropomyosin receptor kinase (TRK) degrader that targets the intracellular kinase domain of TRK. CG416 reduced levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells and inhibited downstream PLCγ1 signaling at sub-nanomolar concentrations. CG416 also degraded human wild-type TRKA.

BI 730357 is a RORγ Antagonist for the treatment of autoimmune diseases.