Eluxadoline Dihydrochloride is an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist.

Lascufloxacin, also known as KRP-AM-1977, is a potent antibacterial drug candidate. Lascufloxacin showed a broad spectrum of activity against various clinical isolates. Especially, lascufloxacin showed the most potent activity against gram-positive bacteria among the quinolones tested. Furthermore, lascufloxacin showed incomplete cross-resistance against existing quinolone-resistant strains. Enzymatic analysis indicated that lascufloxacin showed potent inhibitory activity against both wild-type and mutated target enzymes. Lascufloxacin may be useful in treating infections caused by various pathogens, including quinolone-resistant strains.

Miransertib, also known as ARQ 092, is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). ARQ 092 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. ARQ-092 demonstrated high enzymatic potency against AKT1, AKT2, and AKT3, as well as potent cellular inhibition of AKT activation and the phosphorylation of the downstream target PRAS40. ARQ-092 also served as a potent inhibitor of the AKT1-E17K mutant protein and inhibited tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.

A novel potent, selective, orally bioavailable inhibitor of voltage-gated potassium channel KCNH3 with IC50 of 9.0 nM.

EC330 is a leukemia inhibitory factor (LIF) inhibitor.

DL-AP5 is a Broad spectrum EAA antagonist.

BAY-1316957 (BAY 1316957) is a highly potent, selective, orally available human prostaglandin E2 receptor subtype 4 (hEP4-R) antagonist with IC50 of 15.3 nM.

DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).

nor-NOHA is a potent, selective, competitive, and high affinity inhibitor of arginase. nor-NOHA inhibits arginase from rat liver (IC50 = 2 μM) and mouse macrophages (IC50 = 50 μM).

H-89 is a specific adenylyl cyclase inhibitor (DDA) and a cyclic AMP-dependent protein kinase inhibitor. H-89 blocks the action of equine growth hormone on in vitro maturation of equine oocytes. H-89 decreases the gain of excitation-contraction coupling and attenuates calcium sparks in the absence of beta-adrenergic stimulation. H-89 potentiates adipogenesis in 3T3-L1 cells by activating insulin signaling independently of protein kinase A.

GSK2798745 is an inhibitor of the transient receptor potential vanilloid 4 (TRPV4) with IC50 of 1.8nM.

CPI 0610 is a potent, selective, and cell-active BET bromodomain inhibitor with IC50 of 39 nM for BRD4-BD1 in TR-FRET assay.

CDK9-IN-8 is a highly potent, selective CDK9 inhibitor with IC50 of 12 nM, shows good selectivity in CDKs kinase profiling assay against CDK kinases and cell proliferation inhibition.

Pritelivir, also known as AIC-316 and BAY 57-1293, is a potent helicase primase inhibitor. BAY 57-1293 inhibits replication of herpes simplex virus (HSV) type 1 and type 2 in the nanomolar range in vitro by abrogating the enzymatic activity of the viral primase-helicase complex. In various rodent models of HSV infection the antiviral activity of BAY 57-1293 in vivo was found to be superior compared to all compounds currently used to treat HSV infections. The compound shows profound antiviral activity in murine and rat lethal challenge models of disseminated herpes, in a murine zosteriform spread model of cutaneous disease, and in a murine ocular herpes model. It is active in parenteral, oral, and topical formulations.

Proxalutamide (GT-0918) is a nonsteroidal antiandrogen (NSAA) – specifically, a selective high-affinity silent antagonist of the androgen receptor (AR) for the potential treatment of COVID-19, prostate cancer, and breast cancer.

Mozavaptan, also known as OPC 31260, is a vasopressin receptor antagonist marketed by Otsuka. In Japan, it was approved in October 2006 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH) due to ADH producing tumors.

AZD5718 (AZD-5718, AZD 5718) is a novel potent 5-lipoxygenase activating protein (FLAP) inhibitor with binding IC50 of 6.3 nM; exhibits LTB4 inhibition in human whole blood assays with IC50 of 39 nM; reduce the production of pro-inflammatory and vasoactive leukotrienes both in vitro and in vivo.

IU1-47 is a potent, selective small-molecule inhibitor of USP14 with IC50 of 0.6 uM, shows 10-fold more potent over IU1 and retains specificity for USP14; accelerates the rate of degradation of wild-type tau, the pathological tau mutants P301L and P301S, and the A152T tau variant in primary neuronal cultures, a specific residue in tau, lysine 174, is critical for the IU1-47-mediated tau degradation by the proteasome; stimulates autophagic flux in primary neurons.

MALAT1 inhibitor 5 (Malat1 inhibitor 5) is a selective small molecule targeting of Metastasis-associated lung adenocarcinoma transcript 1 (Malat1/MALAT1 mouse/human), a highly conserved long non-coding RNA; does not affect Neat1 lncRNA levels.

ML372 is a small molecule SMN modulator that increases SMN protein in patient fibroblasts with EC50 of 37 nM; possesses good potency, pharmacokinetics, tolerance, and CNS penetration that are able to increase levels of SMN protein in several model cell lines; increase SMN protein levels in vivo, restore motor function, and prolong survival of SMNΔ7 SMA Mice; improves the righting reflex and extended survival of a severe mouse model of SMA.

CCT241736 is a novel, orally bioavailable Dual FLT3-Aurora Kinase Inhibitor.

Bz-Nle-Lys-Arg-Arg-AMC is a substrate for dengue virus NS2B-NS3 and yellow fever virus NS3 protease.

An E3 ligase ligand-linker conjugate for PROTAC.

Bis(tributylammonium) difluoromethylenediphosphonate

Afobazole is a multi-targeted anxiolytic drug with neuroprotective activities. It binds to the sigma-1, melatonin MT1, and MT3 receptors, as well as monoamine oxidase A (MAO-A, Kis = 5.9, 160, 0.97, and 3.6 µM, respectively, in a radioligand binding assay). Afobazole (5 mg/kg) decreases the latency to enter, as well as increases the number of entries into and percentage of time spent in, the open arms of the elevated plus maze, indicating anxiolytic-like activity in passive stress-coping BALB/c, but not active stress-coping C57BL/6, mice. It decreases stroke volume and neuronal and oligodendroglial cell death in the brain in a rat model of ischemia induced by middle cerebral artery occlusion (MCAO) when administered at doses of 0.3 and 3 mg/kg.

OSMI-1 is a cell-permeable, small molecule O-GlcNAc transferase (OGT) inhibitor with IC50 of 2.7 uM.

AUNP-12 (Aurigene-012) is a PD-1 inhibitor peptide, blocks the PD-1/PD-L1, PD-1/PD-L2 and PD-L1/CD80 pathways.

BRD0705 is a potent, paralog-selective GSK3α inhibitor with IC50 of 66 nM, 8-fold selectivity over GSK3β (IC50=515 nM).

RGX-104, also known as SB 742881, is a liver X receptor beta agonist with potential immunomodulating and antineoplastic activities. Upon oral administration, RGX-104 selectively targets and binds to LXRbeta, thereby activating LXRbeta-mediated signaling, leading to the transcription of certain tumor suppressor genes and the downregulation of certain tumor promoter genes. This particularly activates the expression of apolipoprotein E (ApoE), a tumor suppressor protein, in tumor cells and certain immune cells. This activates the innate immune system, resulting in depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs), tumor cells and endothelial cells in the tumor microenvironment. This reverses immune evasion, enhances anti-tumor immune responses and inhibits proliferation of tumor cells.

(R)-IMPP is a cell-permeable inhibitor of the secretion of proprotein convertase subtilisin/kexin type 9 (PCSK9; IC50 = 4.8 µM).