FR 900098 is a derivative of fosmidomycin that inhibits DOXP reductoisomerase, demonstrates antimalarial activity with IC50 of 170, 170, and 90 nM for HB3, A2, and Dd2 P. falciparum strains, respectively..

ENMD-1068 is a novel selective PAR2 antagonist without inhibitory activity against thrombin-mediated PAR3 and PAR4 signaling.

DAPH-1 (CGP 52411) is a small molecule that directly inhibits prion protein Sup35 prionogenesis with IC50 of 0.58 uM, inhibits and reverses the formation of Aβ42 fibers and reduces their toxicity to neurons in culture.

A potent 20S proteasome inhibitor with IC50 of 49 nM (inhibition of proteasomal chymotrypsin-like proteolytic activity)..

CJ-13610 is a potent 5-Lipoxygenase (5-LO) inhibitor that suppresses 5-LO product formation with IC50 of 70 nM.

A potent, selective 5-HT2B receptor agonist with pKi of 7.1, >10-fold selectivity over 5-HT2A, 5-HT2C, and other 5-HT subtypes.

A potent, selective and ATP-competitive CK2 inhibitor with Ki of 0.5-1 uM.

Methylnaltrexone Bromide is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation.

FPL64176 is a potent L-type Ca++ channel activator with EC50 of 16 nM.

JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.

2'-Deoxyadenosine is the DNA nucleoside A, which pairs with deoxythymidine (T) in double-stranded DNA.

Sugammadex is an agent for reversal of neuromuscular blockade by the agent rocuronium in general anaesthesia. It is the first selective relaxant binding agent (SRBA). Sugammadex is a modified γ-cyclodextrin, with a lipophilic core and a hydrophilic periphery. This gamma cyclodextrin has been modified from its natural state by placing eight carboxyl thio ether groups at the sixth carbon positions. These extensions extend the cavity size allowing greater encapsulation of the rocuronium molecule. These negatively charged extensions electrostatically bind to the quaternary nitrogen of the target as well as contribute to the aqueous nature of the cyclodextrin.

JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.

Lanreotide acetate (BIM 23014 acetate) is a somatostatin analogue with antineoplastic activity. Lanreotide acetate is used for treatment for carcinoid syndrome.

SC10914 is a highly potent PARP inhibitor (PARP1 IC50 = 7.87 nM) with potent anti-proliferative activity against human BRCA deficient tumor cells (MDA-MB-436, BRCA1 deficient, IC50 = 4.03 nM, Capan-1 BRCA2 deficient, IC50 = 11.66 nM) and PTEN deficient tumor cells (HGC-27,PTEN deficient, IC50 = 0.35 μM). SC10914 showed potent anti-tumor activity in BRCA1/2 mutant tumor models and better pharmacokinetics profile has the potential to be selected as the clinical candidate for the treatment of treatment of BRCA1/2 deficient cancers.

BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities.

Fmoc-Val-Cit-PAB is a linker for antibody-drug-conjugation (ADC).

TAK 653 (also known as NBI 1065845) is an oral small molecule, positive allosteric modulators of AMPA (AMPA-PAM) receptors

Necrostatin-34 (Nec-34), a RIPK1 kinase inhibitor, stabilizes RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain.

Cyclam (1,4,8,11-tetraazacyclotetradecane) is an organic compound. It is a white solid that is soluble in water. The compound is notable as a macrocyclic ligand, which binds strongly to many transition metal cations. The compound was first prepared by the reaction of 1,3-dibromopropane and ethylenediamine.

Artemisitene is an antimalarial agent and the oxidized form of Artemisinin. Artemisinin precursors are the important basic substances for biosynthesis of Artemisinin, including Artemisinic acid, Artemisinin B, Artemisitene, etc.

Pimozide is an antipsychotic agent that acts as an antagonist of the D2, D3, and D4 receptors and the 5-HT7 receptor, also is an inhbitor of STAT5.

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.

ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy.

A novel Glucocorticoid receptor modulator.

TG-89 is a JAK inhibitor. It has IC50 values of 6, 25, 17 and 169 nM against JAK2, FLT3, RET and JAK3 respectively.

Ginkgolic acid C17:1 (GAC 17:1) 通过废除上游的 JAK2 和 Src 来抑制 STAT3 的组成性激活。Ginkgolic acid C17:1 可以诱导 PTEN 和 SHP-1 的大量表达。Ginkgolic acid C17:1 诱导肿瘤细胞凋亡。

Novel lipid-lowering agent, acting as an AMPK activator, increasing ABCA1 protein expression and improving hepatic lipid metabolism and leukocyte trafficking in experimental hepatic steatosis

CAY10781 is an inhibitor of the protein-protein interaction between NRP-1 and VEGF-A

Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib can be used for the research of multiple sclerosis (MS).