Highly potent, selective, competitive, and reversible inhibitor of monoamine oxidase B (MAO-B)

Novel fluorescent-labeled selective adenosine A2B receptor antagonist

Potent competitive antagonist and positive modulator of the P2X2 receptor

Positive modulator of ATP effects at P2X2 receptors

Potent competitive antagonist and positive modulator of the P2X2 receptor with >100-fold selectivity versus P2X4, P2X7, and several investigated P2Y receptor subtypes (P2Y(2,4,6,12))

Unique inhibitor of bacterial chromosomal partitioning, increasing the efficacy of bortezomib and sorafenib through regulation of stress granule formation

Naturally occurring inhibitor of FOXO1a nuclear export

Highly potent and selective VDR-coactivator inhibitor

Novel inhibitor of upstream IκB kinase (IKK), specifically inhibiting the IκB phosphorylation and degradation and the subsequent nuclear translocation of NF-κB

Novel selective 5-HT6 receptor antagonist, enhancing cognition and memory and potently decreasing food intake and body weight in rodents

Selective 5-HT4 agonist

Novel potent and selective inhibitor of SETD2

Novel selective CB2 agonist (CB2: 17.4 nM and CB1: 5585 nM)

Novel bacterial polyyne contributing to the antioomycete and plant-protective effects of P. protegens

Novel PROTAC, targeting steroid hormone receptors for ubiquitination and degradation

The most potent and selective ERRα degrader

Novel selective and potent Fak degrader

Novel SirReal-based PROTAC, inducing isotype-selective Sirt2 degradation, resulting in the hyperacetylation of the microtubule network coupled with enhanced process elongation

Proteolysis targeting chimeras (PROTAC), providing broad tissue distribution and knockdown of the targeted RIPK2 protein in tumor xenografts

Proteolysis targeting chimeras (PROTAC), providing broad tissue distribution and knockdown of the targeted ERRalpha protein in tumor xenografts

Novel potent degrader of H-PGDS protein via the ubiquitin-proteasome system and in the suppression of prostaglandin D2 (PGD2) production

Novel potent epidermal growth factor receptor (EGFR) degrader, inducing EGFRdel19 and EGFRL858R/T790M degradation with DC50 values of 0.51 and 126 nM, showing potent anti-proliferative activity against HCC827 and H1975 cell lines with IC50 values of 0.83

Novel degrader of HMGCR protein, potently blocking cholesterol biosynthesis with less compensatory upregulation of HMGCR

Novel potent and selective p38α and p38β degrader

Novel PI3K degrader, showing a significant and complete degradation effect on PI3K kinase at a concentration of 10 μM within 8 h

Novel noncovalent CDK12/13 dual inhibitor, inducing potent and selective CDK12-CycK degradation without affecting CDK13, suppressing DDR-associated genes and induced synthetic lethality with Olaparib

Novel SLC-targeting chimeric degrader, targeting SLC9A1 and other SLC9 family members, effectively impairing pH homeostasis and differentially killing cancer cell lines

Novel highly potent degrader against EGFRL858R/T790M and EGFRdel19, reaching the lowest DC 50 values among all reported EGFR-targeting PROTACs

Novel potent cereblon degrader with DC50 of 200 nM, and 64% protein degradation, as quantified by western blot

Prodrug of NBDHEX, selectively inhibiting glutathione transferase (GST P1-1) with better water solubility, and more potent anticancer activities