MLi-2 is an a potent, highly selective, orally available, brain penetrant inhibitor of LRRK2 with an IC50 of 0.76 nM.

Cytosporone B is the first naturally occurring agonist for nuclear orphan receptor Nur77. The molecule binds with high affinity (IC50=0.278 nM) to the ligand-binding domain of Nur77 and stimulates Nur77-dependent activities. Nur77 is also involved in glucose homeostasis, where it induces genes involved in gluconeogenesis. Csn-B physically binds to Nur77 and activates its transactivational activity and translocation to mitochondria to induce apoptosis. It inhibits cancer cell proliferation and tumor growth.

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BDA-366 is a Small-Molecule Bcl2 BH4 Antagonist for Lung Cancer Therapy.

CP-609754, also known as CP-609,754, LNK 754 and OSI 754, is a potent arnesyltransferase inhibitor with potential anticancer activity.

Lixivaptan is a highly potent, non-peptide, oral capsule that works by reducing the action of a hormone (vasopressin) that blocks fluid excretion.

CU-CPT9a is an antagonist of toll-like receptor 8 (TLR8). It inhibits activation of NF-κB induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells (IC50 = 0.5 nM). CU-CPT9a reverses R-848-induced increases in NF-κB p65, IRAK-4, and TRAF3 protein levels in HEK-Blue cells.

ASLAN003 is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. ASLAN003 inhibits protein synthesis via activation of AP-1 transcription factors. ASLAN003 induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.

CAS 1822358-25-7

MSAB is a selective inhibitor of Wnt/β-catenin signaling. MSAB shows potent anti-tumor effects selectively on Wnt-dependent cancer cells in vitro and in mouse cancer models. MSAB binds to β-catenin, promoting its degradation, and specifically downregulates Wnt/β-catenin target genes.

An orally available, brain penetrant p75NTR ligand that blocks p75-mediated cell death, also increases proliferation and survival of hippocampal neural progenitors.

AWZ1066S is a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis.

INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between the BET proteins and acetylated lysines on histones.

BI 409306 is an inhibitor of phosphodisterase 9A（PDE9A）.

LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders[1].

KL1333 is an orally available, small organic molecule that reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL-1333 Improves Energy Metabolism and Mitochondrial Dysfunction in MELAS Fibroblasts.

LJ570 is the first PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation. LJ570 is a potent partial agonist of both PPARα and γ subtypes. LJ570 inhibited the Cdk5-mediated phosphorylation of PPARγ at serine 273 that is currently considered the mechanism by which some PPARγ partial agonists exert antidiabetic effects similar to thiazolidinediones, without showing their typical side effects. LJ570 may be useful for treatment of dyslipidemic type 2 diabetes.

O(6)-Benzylguanine is an MGMT inhibitor that prevents the repair of DNA damage induced by chemotherapeutics. It allows apoptosis and other mechanisms of cell death to occur.

Lyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor..

LGD-6972 is a selective and orally active glucagon receptor antagonist. LGD-6972 has the potential for type 2 diabetes research.

A potent PI3K inhibitor with IC50 3 nM, does not inhibit PI4K activity.

Mianserin is a psychoactive drug of the tetracyclic antidepressant (TeCA) therapeutic family. It is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA) and has antidepressant, anxiolytic (anti-anxiety), hypnotic (sedating), antiemetic (nausea and vomiting-attenuating), orexigenic (appetite-stimulating), and antihistamine effects.

Mianserin hydrochloride is a tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.

WC5-2 is a Resorufin derivatives as high-​specificity fluorescent probes in detecting cytochrome P4501A1. The activity of CYP1A1 in different enzyme sources (such as human or animal tissue prepn. liq., recombination expressed CYP1A1 single enzyme, or histocyte biol. samples) can be detected by quant. detn. of fluorescent emission spectrum at 560-​630nm with fluorescence detector at excitation wavelength of 480-​530nm.

Prolyl Endopeptidase Inhibitor 1 (Boc-Pro-prolinal) is a potent prolyl endopeptidase (PEP; PE) inhibitor, with a Ki value of 15 nM. Prolyl Endopeptidase Inhibitor 1 has anti-amnesic effect.

BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.

A neuropeptide derived from the same precursor polypeptide as neurotensin, and with similar but subtly distinct expression and effects..

CGP-42112 (CGP42112A) is a highly potent, selective Angiotensin-II subtype 2 receptor(AT2 receptor) agonist with Ki of 0.24 nM.

A potent melanocortin MC3 and MC4 receptor antagonist with IC50 of 0.23 nM and 0.06 nM, respectively.

JNJ63576253, also known as TRC253, is a potent and orally active androgen receptor antagonist. TRC253 specifically binds to both wild-type and certain mutant forms of AR, thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot translocate to the nucleus.