CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain.

GSK-3b inhibitors; GSK-3b inhibitors;

Lalistat 2 is a specific inhibitor of lysosomal acid lipase (LAL) with no effect on other forms of lipase.

GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein[1].

OUL35 (NSC39047) is a potent and selective inhibitor of mono-ADP-ribosyltransferase PARP10/ARTD10 with IC50 of 330 nM, displays remarkable selectivity towards ARTD10 over other enzymes in the human protein family.

IGF-1R/SRC inhibitor

useful for the treatment of cystic fibrosis; modulating CFTR activity; altering the lifespan of a eukaryotic organism;

cytotoxity (targeted to DNA topoisomerase II); anti-cancer activity; fungicides;

VEGF inhibitor

6-Maleimidocaproic acid contains a maleimide group and a terminal carboxylic acid. The terminal carboxylic acid can be reacted with primary amine groups in the presence of activators (e.g. EDC, or DCC) to form a stable amide bond. The maleimide group will react with a thiol group to form a covalent bond, enabling the connection of biomolecule with a thiol.

NOX-6-18 is a potent, selective GPR132 antagonist with IC50 of 17 nM.

CPI-360 is a compound in design and preparation of wew palladium precatalysts for C-C and C-N cross-coupling reactions.

BMS-P5 is a Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor with pIC50 values in the range of 5-​7.5. BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Administration of BMS-P5 to multiple myeloma-bearing mice delays appearance of symptoms and disease progression Targeting PAD4 may be beneficial for treatment of multiple myeloma.

Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Mc-MMAE is a drug-linker conjugate for ADC.

glucocerebrosidase activator;

anti-inflammatory, COX inhibitory activities and ulcerogenic liability

antitubercular activity; fungicidal activity;

AG1478 HCl is an inhibitor of epidermal growth factor receptor protein.

DB2313 is a first-in-class potent small-molecule inhibitor of PU.1. DB2313 disrupts the interaction of PU.1 with target gene promoters and leads to down-regulation of canonical PU.1 transcriptional targets.

BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively.

NFATc1-IN-1 (compound A04) is a potent inhibitor of RANKL-induced osteoclast formation, with an IC50 of 1.57 μM. NFATc1-IN-1 shows anti-osteoclastogenic effects through reducing the RANKL-induced nuclear translocation of NFATc1. NFATc1-IN-1 can be used for osteoclastic diseases research.

potential leads for chaperone therapy for Gaucher disease

MitoBloCK-10 (MB-10) is a potential attenuator of protein import into mitochondria via targeting Tim44, inhibits the import of substrates that use the TIM23 import pathway.

antagonist of the NK3 receptor; altering the lifespan of a eukaryotic organism;

restore E-cadherin expression in the SW620 colon adenocarcinoma cell line

useful for the treatment of cystic fibrosis

AES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC50 values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.

NBD-556 is small molecule mimetic of CD4, NBD-556 recognizes the HIV-1 envelope protein gp120 and induces restructuring of gp120 analogous to CD4 binding.