Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity.

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.

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.

BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.

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.

4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.

Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist.

NS8593 hydrochloride is a potent and selective small conductance Ca2+-activated K+ channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca2+), and does not affect the Ca2+-activated K+ channels of intermediate and large conductance (hIK and hBK channels, respectively).

Sulfopin is a covalent, highly selective inhibitor of Pin1 with Ki of 17 nM in the FP assay. Sulfopin also blocks Myc-driven tumors in vivo without any toxicity.

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.

Chrysoeriol, a natural flavonoid extracted from the tropical plant Coronopus didymus, exhibits potent antioxidant activity. Chrysoeriol shows significant inhibition of lipid peroxidation.

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.

CGS-15943| is a highly potent, non-selective adenosine receptor antagonist.

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.

An E3 ligase ligand-linker conjugate for PROTAC.

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.

Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function.

Novel allosteric agonist of Sphingosine 1-phosphate receptor 2 (S1PR2)

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

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.

α-Conotoxin MII is a highly potent and selective competitive antagonist for α3β2 subunit-containing nicotinic receptors (IC50 = 0.5 - 3.5 nM at α3β2 expressed in Xenopus oocytes). Also potently blocks β3-containing neuronal nicotinic receptors. Displays > 200-fold selectivity for α3β2 over α2β2, α4β2 and α3β4.

Lasmiditan, also known as COL-144 and LY573144, is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (K1=2.21 μM) without vasoconstrictor activity that seemed effective when given as an intravenous infusion in a proof-of-concept migraine study. Lasmiditan showed efficacy in its primary endpoint, with a 2-hour placebo-subtracted headache response of 28.8%, though with frequent reports of dizziness, paresthesias, and vertigo.