An Insecticide, induces G-protein-coupled receptor desensitization via activation of conventional protein kinase C

Novel inhibitor of glutathione S-transferase P1-1 (GSTP1-1)

Novel potent androgen receptor (AR) antagonist that suppresses prostate cancer cell growth

Fulvestrant (ICI 182,780) is a selective estrogen receptor down-regulator (SERD). Fulvestrant is a high affinity estrogen receptor antagonist. Fulvestrant is the first "pure" antiestrogen with no agonistic activity both in vitro and in vivo.

Inhibitor of ROS production, preventing PD symptoms in the LRRK2(R1441G) transgenic (tg) mouse model of PD

Anticholinergic and ganglion-blocking agent

Dual SERT/NET reuptake inhibitor, being the major active metabolite of venlafaxine

Novel specific Rac1 inhibitor, interferring with the interaction of Rac1 with Dock180, a relevant Rac1 activator in glioma invasion, and to reduce Rac1-GTP levels

Novel Inhibitor of HIV-RNaseH, E. coli RNaseH, and human RNaseH1

Natural CYP4X1 inhibitor, reprogramming TAMs via CB2 and EGFR-STAT3 axis

Novel vasorelaxing agent, stimulating soluble guanylyl cyclase, activating K+ channels, and blocking extracellular Ca2+ influx

Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.

A methylated analog of RHI002 (AOB4894) which is a selective inhibitor of human RNaseH2

Water soluble analogue of Kobe0065 (AOB4259) and Kobe02602 (AOB4258), showing inhibitory activity towards Ras-Raf binding

A potent inhibitor of FACT (facilitates chromatin transcription) complex that activates p53 and suppresses NF-kB without genotoxicity. CBLC000 induces chromatin trapping of FACT both in vitro and in vivo. CBLC000 exhibits brad anticancer activity. CBLC000

A selective, positive allosteric modulator at the muscarinic M1 acetylcholine receptor

Coniferyl alcohol is an intermediate in biosynthesis of eugenol and of stilbene and coumarin.

Partial mGluR5 partial antagonist

MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer[1][2].

AMP-activated protein kinase (AMPK) activator. Stimulates AMPK heterotrimer (α1β1γ1) activity (EC50 = 0.3 μM). Thought to directly activate AMPK by antagonizing autoinhibition.

Novel inducer of mitotic arrest, modulating microtubule plus-ends and reduced microtubule dynamics.

Substrate for NAD(P)H:quinone oxidoreductase 1 (NQO1)

Potent inhibitor of small conductance calcium-activated potassium (SK) channels, interacting with the channel at the apamin binding site.

Novel selective inhibitor of primordial germ cell (PGC) development, targeting poly(A)-tail-independent noncanonical translation (PAINT)

Alpinumisoflavone (compound 2) is a flavonoid derivative isolated from the stem bark of Erythrina lysistemon Hutch.

Novel inhibitor of chromosomal instability, potentiating MCAK in vivo and transiently suppressing chromosome mis-segregation in CIN cancer cells

An inhibitor of the ganglionic transmission of the dog urinary bladder and that the blockade of the nicotinic receptor played a main role.

Novel inhibitor of AMA1-RON2 interaction; Inhibitor of c-Src tyrosine kinase activity

A novel cyclin-dependent kinase inhibitor

A water soluble form of the potent p38 (SAPK2a) inhibitor

Psychomotor stimulant

Potent Allosteric Agonist-Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptors

Novel peroxisome proliferator activated receptor γ (PPARγ) ligand

This compound belongs to the class of chemical entities known as aryltetralin lignans. These are lignans with a structure based on the 1-phenyltetralin skeleton.

Sorting inhibitor, increasing lateral root occurrence by acting upstream from the morphological marker of lateral root primordium formation, the mitotic activity

Natural essential oil with antioxidant activity and cytotoxicity on tumor cells

Novel selective activator of the p38 mitogen-activated protein kinase (MAPK) pathway, derepressing a subset of endogenous genes repressed by DNA methylation

Agonist of transient receptor potential channels 3 and 2 (TRPML3 & TRPML2)

CK-548 inhibits the activity of actin-related protein (Arp)2/3 complex by inserting into the hydrophobic core of Arp3 and altering its conformation: inhibits

Novel selective c-Myc inhibitorReference:1) Disruption of Myc-Max heterodimerization with improved cell-penetrating analogs of the small molecule 10074-G5; Oncotarget. 2013 Jun;4(6):936-47. GoTo Paper

Potent and ATP-binding site inhibitor of GSK-3

Antiangiogenic multitarget fibroblast growth factor-2 antagonist and allosteric inhibitor of the angiogenic enzymethymidine phosphorylase

Novel DNMT1 Selective Antagonist

A novel inhibitor of SARS-CoV replication, acting by blocking cathepsin L, a host protease required for processing of SARS-S during viral entry

Novel Specific Inhibitor of Cell Division, targeting FtsZ

Novel Specific Inhibitor of Cell Division, targeting FtsZ

GABAA antagonist, selectively antagonising tonic over phasic GABAergic currents in dentate gyrus granule cells

PCNA-I1 is an inhibitor of proliferating cell nuclear antigen (PCNA) that binds to PCNA trimers (Kd = 0.41 µM) and dose-dependently reduces the level of PCNA associated with chromatin in PC3 cells.

Novel elastase inhibitor, antagonizing IL-36 cytokine activation

Potent, selective, and  competitive 15-hydroxyprostaglandin dehydrogenase (15-PGDH; HPGD) inhibitor

AA92593 has been used as a selective inhibitor of melanopsin.

α-Lapachone shows trypanocidal activity[1].

A natural phytosterol.

An analgesic drug.

Canthin-6-one displays a wide range of biological activities, such as antimycobacterial activity.

An orally bioavailable p38 MAP kinase inhibitor developed to treat inflammatory diseases

Osajin is the major bioactive isoflavone present in the fruit of Maclura pomifera with antitumor, antioxidant and anti-inflammatory activities.

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

Stimulates dopamine release from striatal slices in vitro.

An ATP-competitive CDK inhibitor

Selective growth inhbitor of KM12 colon cancer cell line

Rhododendrol is a natural phenolic compound that has been reported to prevent high-fat diet-induced elevation in body weight and to increase lipolysis in white adipocytes in male mice. RK has shown potential to increase dermal IGF-I production through sen

Inhibitor of 17β-hydroxysteroid dehydrogenases (17β-HSDs)

Dopamine antagonist, blocking presynaptic but stimulating postsynaptic alpha-adrenoceptors

T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream).

6"-O-Malonylgenistin, Free Acid, is an isoflavone derivative.

Novel inhibitor of heterotrimeric Gαi subunits