VU6080824 (Compound 5s), a derivative of ML-133), is an inward-rectifier potassium channel (Kir2.1) inhibitor with an IC50 of 0.35  μM. VU6080824 has superior thallium flux and manual patch clamp (MPC) functional potency.

SVC112 is a translation elongation inhibitor that prevents the cyclic dissociation of EF2 from the ribosome, thereby inhibiting the elongation step of translation. SVC112 shows activity in growth inhibition among cancer cell lines of various origins (acute myeloid leukemia (AML), multiple myeloma (Myeloma), colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC)). SVC112 preferentially impedes ribosomal processing of mRNAs, and decreaseds CSC-related proteins including Myc and Sox2. SVC112 induces apoptosis in hematologic cancer cell lines, while phosphorylation of c-Myc correlates with sensitivity to SVC112 in colorectal cancer cell lines. SVC112 inactivates HNSCC stem cells in vitro and prevents the regrowth of HNSCC tumor xenografts in mice. SVC112 can be used for the study of HNSCC.

Lin28 degrader MG-Lin3 is a molecular glucose degrading agent that targets the Lin28 protein. Lin28 degrader MG-Lin3 significantly reduces the Renilla luciferase signal at 100 µM. Lin28 degrader MG-Lin3 inhibits the maturation of tumor microRNA let-7. Lin28 degrader MG-Lin3 can be used for cancer research.

5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases.

DJ-89 (Compound 77) is a potent soluble epoxide hydrolase (sEH) inhibitor with an IC50 value of 0.51 nM . DJ-89 inhibits sEH from hydrolyzing epoxyeicosatrienoic acids (EETs), reducing the production of pro-inflammatory substances. DJ-89 is promising for research of acute and chronic inflammatory diseases (such as rheumatoid arthritis).

β-Blocker B-24/76 is a beta adrenoceptor blocker. β-Blocker B-24/76 exhibits beta 1-adrenoceptor blocking and beta 2-adrenoceptor stimulating properties. β-Blocker B-24/76 can suppress the increased ornithine decarboxylase activity in hypertrophied hearts. β-Blocker B-24/76 can be used for the research of cardiovascular disease.

Metralindole is an inhibitor of human cyclin-dependent kinase CDK2 and human protein kinase CK2 holoenzyme. Metralindole shows good potential as a non-small cell lung cancer inhibitor.

(Z)-1,2-Dimethoxy-4-(3-fluoro-2-propenyl)benzene is a fluorine analog of Methyl eugenol (ME) and is attractive to oriental fruit fly B. dorsalis.

SCH-1518291 (Compound 27) is an orally active PDE10A inhibitor. SCH-1518291 exhibits antipsychotic activity in an ADHD rat model. SCH-1518291 can be used in research on neurological disorders such as psychosis.

BRP-821 is a soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 0.4 nM. BRP-821 can be used for the researches of inflammation, cardiovascular, metabolic and neurological disease .

PGE 9262932 is a quinolone antibacterial agent. PGE 9262932 can be used for the research of infection.

WCK-1152 is a fluoroquinolone antibacterial agent. WCK-1152 is active against resistant pathogens bearing mutations of DNA gyrase and/or topoisomerase IV which also express efflux pumps. WCK-1152 can be used for the research of infection, such as respiratory infections caused by resistant pneumococci and staphylococci.

DC-756 is a fluoroquinolone antibiotic. DC-756 possesses potent activity against Gram-positive and Gram-negative pathogens comparable to Trovafloxacin, with MIC, against Ofloxacin-resistant strains 16-fold better than Trovafloxacin. DC-756 is well absorbed orally in rats and found to have good photostability. DC-756 can be used to study bacterial resistance.

Dopamine D3 receptor ligand-6 (Compound 196476) is a selective dopamine D3 receptor (D3) antagonist. Dopamine D3 receptor ligand-6 is promising for research of substance use disorders (such as opioid and psychostimulant addiction).

4'-Acetyl-chrysomycin A is an analog of chrysomycin A. 4'-Acetyl-chrysomycin A has antibacterial activity.

L-759656 is a selective cannabinoid CB2 receptor agonist, with the Ki of 11.8 nM for the human CB2 receptor. L-759656 potently inhibits Forskolin-stimulated cyclic AMP production in Chinese Hamster Ovary (CHO) cells, with an EC50 of 3.1 nM. L-759656 can be used for the study of immune-related diseases and inflammatory diseases.

(±)-WB 4101 is a highly selective α1-adrenergic receptor antagonist. (±)-WB 4101 blocks norepinephrine-induced vascular smooth muscle contraction to exert antihypertensive and benign prostatic hyperplasia (BPH)-relieving effects. (±)-WB 4101 is promising for research of hypertension and BPH.

PSEC13 is an activator of HSF-1/DAF-16 axis. PSEC13 can upregulate heat shock proteins. PSEC13 can form hydrogen bonds with key residues in the HSP-16.2 active site. PSEC13 can be used to enhance proteostasis and extend lifespan through the modulation of HSP-16.2. PSEC13 could promote the nuclear translocation of daf-16, upgrading the proportion of intermediate. PSEC13 can be studied in research for aging and age-related diseases.

F-14258 is a 5-HT1B/1D receptor agonist. F-14258 can achieve receptor specific analgesia through local administration. F-14258 can be used for research on ear pain.

AR-DBD ligand-Linker Conjugate 1 is a conjugate of AR-DBD ligand and linker. AR-DBD ligand-Linker Conjugate 1 can be used to synthesize PROTAC LYA914.

PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.

TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT2A receptor (such as depression).

Socrodeucitinib (Compound Example 58) is an orally active and selective tyrosine kinase 2 (TYK2) inhibitor with an IC50 value of 1.41 nM. Socrodeucitinib exerts anti-inflammatory activity by inhibiting TYK2-mediated cytokine signaling pathways and reducing the secretion of inflammatory factors. Socrodeucitinib is promising for research of autoimmune diseases such as psoriasis and inflammatory diseases.

ISM5939 is an orally active and selective ENPP1 inhibitor with an IC50 of 0.63 nM for 2,3-cGAMP degradation and 9.28 nM for ATP hydrolysis. ISM5939 has antitumor activity.

E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research.

ZSA-215 is a potent and orally active STING agonist with an EC50 of 3.3 μM. ZSA-215 enhances STING signaling through promoting the phosphorylation of STING and interferon regulatory factor 3 (IRF3) and secretion of IFN-β. ZSA-215 inhibits tumor regression and long-term survival of mice in MC38 colon cancer model. ZSA-215 can be used to the study of colon cancerr.

Eprazole trisulfide dimer is a trisulfide dimer of Ilaprazole), an orally active proton pump inhibitor that irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Eprazole trisulfide dimer can be utilized in research on gastric ulcers.

TBS6b is a potent and selective ACKR3 molecular glue degrader. TBS6b degrades ACKR3 via the ubiquitin-proteasome pathway. TBS6b inhibits hepatocellular carcinoma cell proliferation, migration, and invasion. TBS6b is relevant to hepatocellular carcinoma (HCC) research.

Y-36912 is an orally active, highly selective and affinity 5-HT4 receptor agonist (Ki = 1.5 nM). Y-36912 can accelerate gastric emptying and increase bowel frequency and stool weight. Y-36912 can be used for research on gastrointestinal conditions.

DDS5 is a CD28 inhibitor with a kd of 175.57 µM. DDS5 significantly inhibits CD28-CD80 interaction (IC50: 332 µM). DDS5 can be used for research of immune-mediated diseases, including inflammatory bowel disease and rheumatoid arthritis.