Idronoxil, also known as Phenoxodiol, is a synthetic flavonoid derivative. Phenoxodiol activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis (XIAP), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex, thereby preventing DNA replication and resulting in tumor cell death.

CK-2127107(CK-107, Reldesemtiv) is a novel orally active fast skeletal troponin activator, selectively activates fast skeletal myofibrils with EC50 of 3.4 uM.

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.

GNF2133 is a selective DYRK1A inhibitor with an IC50 value of 6 nM.

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.

ASP4132(ASP-4132,ASP 4132) is a potent adenosine monophosphate-activated protein kinase (AMPK) activator with EC50 of 18 nM, which shows moderately aqueous solublity and oral activity.

LY3325656 is a novel GPR142 agonist and is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.

Taniborbactam (VNRX-5133) is a boronic-acid-containing pan-spectrum β-lactamase inhibitor against the class A, C, and D serine β-lactamases (SBLs).

DBPR112 is a potent EGFR mutation inhibitor against EGFRL858R/T790M double mutations with IC50 of 48 nM and also exhibits 10-fold potency better than Osimertinib, against EGFR and HER2 exon 20 insertion mutations.

M8891 is a methionine aminopeptidase-2 (MetAP-2) selective inhibitor with Ki and IC50 of 4.33 nM and 54 nM, respectively.

BAY-298 is a potent, and selective antagonists of the luteinizing hormone receptor with IC50 of 96 nM, 23 nM and 78 nM against human, rat, and cynomolgus monkey LH receptors.

VUF16839 is a high-affinity non-imidazole histamine H3 receptor agonist with pKi of 8.5 and pEC50 of 9.5, which shows weak activity on CYP enzymes and good metabolic stability.

DS54360155 is an orally potent analgesic without μ-opioid receptor agonist activity.

AGX51 is a small-molecule Id antagonist and inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduced viability.

GS-6207 (GS6207, GS-CA1) is a potent, selective inhibitor of HIV-1 capsid function with potency and potential to be clinically effective against a broad range of HIV-1 strains..

3AC is an inhibitor of SH2 domain-containing inositol-5’-phosphatase 1 (SHP-1). It is selective for SHP-1 over SHP-2 and phosphatase and tensin homolog (PTEN). 3α-Aminocholestane induces hyperactivation of the tyrosine kinase SYK in patient-derived Ph+ acute lymphoblastic leukemia (ALL) cells and selectively induces cytotoxicity in these cells over mature B cell lymphoma cells. It reduces leukemia burden and increases survival in a tyrosine kinase inhibitor-resistant patient-derived Ph+ ALL mouse xenograft model when administered at a dose of 50 mg/kg. 3α-Aminocholestane reduces cell viability of OPM2 multiple myeloma (MM) cells in a concentration-dependent manner and of RPMI8226 MM cells when used at concentrations greater than or equal to 12.5 μM. It halts the cell cycle at the G0/G1 or G2/M stages in the highly proliferative OPM2 or less proliferative RPMI8226 cell lines, respectively. It induces apoptosis via activation of caspase-3, caspase-9, and poly(ADP-ribose) polymerase (PARP) in OPM2 cells but not in RPMI8226 cells. 3α-Aminocholestane reduces tumor burden and increases survival in an OPM2 mouse xenograft model.

Nimbolide is a natural inhibitor of pancreatic cancer growth and metastasis through ROS-mediated apoptosis. It inhibits epithelial-to-mesenchymal transition.

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).

OP-3633 is a potent steroidal glucocorticoid receptor (GR) antagonist with IC50 of 29 nM and shows excellent selectivity against GR over progesterone receptors (PR) and androgen receptors (AR).

UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM). UDM-001651 was evaluated in a monkey thrombosis model and shown to have robust antithrombotic efficacy and no prolongation of kidney bleeding time. This combination of excellent efficacy and safety margin strongly validates PAR4 antagonism as a promising antithrombotic mechanism.

VU6003586 is a novel allosteric modulators of mGlu5 with EC50 of 174 nM.

Ziresovir (RO-0529, AK0529) is a potent, selective and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein inhibitor with EC50 of 3 nM.

DS44960156 is a selective Methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor, with IC50 values of 1.6 μM and >30 μM for MTHFD2 and MTHFD1, respectively.

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.

BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay.

RA306 (RA-306) is a selective, potent, orally active, ATP-competitive CaMKII inhibitor, inhibits CaMKII delta (IC50=15 nM), gamma (IC50=25 nM), and alpha (IC50=61 nM) isoforms.RA306 displays a good selectivity profile vs. kinases and non-kinase targets, as compared with KN-93.RA306 also displays a good cellular activity in cardiomyocytes from human, rat, and mice, with IC50s in the 200 nM range.Isoproterenol-induced phosphorylation of Thr17-PLN, normalized to total PLN, was fully inhibited by RA306 in a dose-dependent manner, with IC50s of 140 nM in rat, 205 nM in mouse, and 220 nM in human cardiomyocytes.

BPN14770 (BPN-14770) is an allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 and 7.4 nM for human PDE4D7 and PDE4D3 respectively, displays 16-fold less potent against monomeric form of PDE4D lacking the UCR1 dimerization domain (PDE4D2