A potent nuclear receptor TR3 (Nur77)-specific targeting compound that can induce melanoma autophagy through a mitochondrial signaling pathway.

LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.

Salbutamol is an agonist of the β2-adrenergic receptor (β2-AR; Kd = 759 nM in a radioligand binding assay using CHO cells expressing the human receptor).

IP6K1 inhibitor TNP is a potent, selective inositol hexakisphosphate kinase IP6K with IC50 of 0.47 uM (IP6K1), does not inhibit either human or yeast Vip/PPIP5K.

SMIFH2 is a small molecule formin homology 2 domains inhibitor of formin-mediated actin assembly, targets formins from evolutionarily diverse organisms including yeast, nematode worm, and mice with IC50s of 5-15 uM.

NNC-711 is a potent and selective inhibitor of GABA uptake by GAT-1 with IC50 of 0.04 uM.

Polyvinylimidazole (Vimdemer) is a weak basic polyelectrolyte and has been already used as a model polyelectrolyte to study adsorption properties on various minerals.

Ganosporeric acid A, a natural product, is isolated from the ether-soluble fraction of the spores of Ganoderma lucidum (Curt.: Fr.) P. Karst. Ganosporeric acid A can be used for the research of liver injury.

VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer.

Glutaurine containing glutamine and taurine residues is an orally active hormone of the parathyroid. Glutaurine, as a hormone, is isolated from parathyroid gland oxyphil cells. Glutaurine can be used for the research of antiepileptic and anti-amnesia.

Dextromilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Dextromilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1).

CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).

PCSK9 degrader 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) degrader. PCSK9 degrader 1 does not affect PCSK9 function.

L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR.

Strophanthidin is a naturally available cardiac glycoside. Strophanthidin 0.1 and 1 nmol/L increases and 1~100 µmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal. Strophanthidin increases both diastolic and systolic intracellular Ca2+ concentration.

Ocedurenone is a corticosteroid receptor antagonist. Ocedurenone can be used for the research of kidney disease (WO2018054357, compound I).

AA38-3 is a serine hydrolase (SH) inhibitor. AA38-3 can inhibit three SHs, ABHD6, ABHD11, and FAAH.

ASP-4058 hydrochloride is a next-generation, selective and orally active agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.

Icapamespib (PU-HZ151) is a potent HSP90 inhibitor with an EC50 of 5 nM. Icapamespib is able to cross blood-brain barrier.

Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value ＜1 nM in vitro. Dazucorilant can be used for the research of neurological disorders.

DHODH-IN-17, a 2-anilino nicotinic acid, is a human DHODH inhibitor (IC50=0.40 μM). DHODH-IN-17 can be used for theresearch of acute myeloid leukemia (AML).

Terevalefim (ANG-3777), an hepatocyte growth factor (HGF) mimetic, selectively activates the c-Met receptor.

Gemnelatinib is a tyrosine kinase inhibitor (WO2018077227, implementation example 1). Gemnelatinib can be used for the research of cancer.

Fosgonimeton is a hepatocyte growth factor receptor agonist (WO2017210489).

Avotaciclib (BEY1107) is an orally active cyclin dependent kinase 1 (CDK1) inhibitor. Avotaciclib can be used for the research of cancer.

Ipivivint (SM08502), a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer.

CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.

Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively).

JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM. JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth.

SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer.