Satoprodil (example 2) is a potent N-methyl-D-aspartate (NMDA) receptor negative allosteric modulator with an IC50 value of 123 nM for NR2B.

TRIM25 ligand-1 (Compound 10) is a covalent ligand. TRIM25 ligand-1 can covalently bind to Cys498 in the PRYSPRY domain of TRIM25 and enhance its auto-ubiquitination activity. TRIM25 ligand-1 is selective for TRIM25 in vitro and in live cells.

dAPM-1 (acetate) is a peptidomimetic antibiotic agent. dAPM-1 (acetate) can selectively induces intracellular aggregation in B. subtilis. dAPM-1 (acetate) is active against S. aureus, methicillin-resistant S. aureus (MRSA), B. subtilis, E. faecium, and M. smegmatis with MICs of 8, 4, 4, 8, and 16 µg/ml, respectively.

(3S,4R)-ME-344 is the (3S,4R)-enantiomer of ME-344). ME-344 is a mitochondrial Heme oxygenase 1 (HO-1) inhibitor. ME-344 specifically binds and alters HO-1 structure, and increases HO-1 translocation from the rough endoplasmic reticulum to mitochondria, but only in drug-sensitive cells (such as H460 and SHP-77 cells). ME-344 decreases mitochondrial ATP production and induces ROS, with subsequent disruption of redox homeostasis and mitochondrial function. ME-344 has significant antitumor activity, and can be used for cancers like breast cancer research.

YTHDF2 ligand-1 (Compound 23) is a selective and high-affinity YTHDF2 ligand with a Kd of 1.3 μM (FP assay) and an IC50 of 11 μM (HTRF assay) . YTHDF2 ligand-1 can be used in the study of cancer.

MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC50 = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors.

Debio 1453 is a bactericidal FabI inhibitor potent against N. gonorrhoeae (IC50 = 0.6 nM), including drug-resistant strains. Debio 1453 demonstrates a low propensity for resistance selection and is effective in eradicating both planktonic and intracellular bacteria through a mechanism of concurrently inhibiting FabI and engaging the non-mutable NADH cofactor. Debio 1453 clears antibiotic-resistant N. gonorrhoeae infection in a murine vaginal model. Debio 1453 can be used for gonorrhoea research.

14-3-3σ/ERα stabilizer-2 (Compound 41) is a covalent 14-3-3σ/ERα stabilizer with a Kd of 10.1 nM. 14-3-3σ/ERα stabilizer-2 significantly decreases the dissociation rate of ERα, stabilizing the binary ERα/14-3-3σ interaction. 14-3-3σ/ERα stabilizer-2 can be used for molecular glues research.

AU-461 is an orally active and reversible inhibitor of the gastric H⁺/K⁺ ATPase with IC₅₀ values for rabbit-derived and pig-derived enzymes are 12.15 μM and 4.20 μM respectively. AU-461 competes with activated cationic K⁺ (Kᵢ = 1.64 μM). AU-461 reduces both histamine-stimulated gastric acid secretion and basal gastric acid secretion in rats. AU-461 inhibits ulcer formation caused by ethanol or sodium hydroxide, and restores the plasma gastrin level to normal. AU-461 can be used for the study of peptic ulcers.

HUP-46 is a BBB-penatrable modulator of αSyn dimerization and autophagy. HUP-46 reduces the ratio of pPP2A/PP2A, increases the autophagy marker LC3BII levels, and decreases αSyn dimerization. HUP-46 can be used for research of neurodegenerative diseases.

1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-pc is a phospholipid-porphyrin conjugate. 1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-pc can be utilized in photodynamic therapy research.

ONO-9517601 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.067 μM, TREK-2 IC50= 0.23 μM). ONO-9517601 displays robust efficacy in an MK-801) challenge rat novel object recognition (NOR) paradigm. ONO-9517601 can be used for research on neurological and cognitive disorders.

ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders.

MJ-26 is an inhibitor targeting Menin. MJ-26 has high binding affinity (Ki: 0.56 μM) and significant antiproliferative activity. MJ-26 works by inhibiting Menin-MLL interaction and inducing Menin protein degradation. MJ-26 has significant antitumor effects on acute myeloid leukemia (AML). MJ-26 can be used in AML research.

FLT3/JAK2/BRD4 ligand-1 is a FLT3/JAK2/BRD4 ligand. FLT3/JAK2/BRD4 ligand-1 can be used for synthesis PROTAC FLT3/JAK2/BRD4 Degrader-1.

AAG561 is a corticotropin-releasing factor receptor 1 (CRF1) antagonist. AAG561 can be used for the study of the underlying emotion dysregulation of a mental disease or disorder.

Deutaleglitazar (Aleglitazar-d2) is a agonist of dual peroxisome proliferatory activating receptor (PPARα and PPARγ).

AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML).

(S,R,S)-AHPC-CO-C2-phenylboronic acid is an E3 ligase ligand-linker conjugate that incorporates the VH032-based VHL ligand and linker. (S,R,S)-AHPC-CO-C2-phenylboronic acid can be used for synthesis of PROTAC AF151.

IA107 is a potent, selective, and allosteric IRE1α RNase (IC50 = 16 nM (non phosphorylated), IC50 = 9 nM (phosphorylated)) inhibitor. IA107 can inhibit endoplasmic reticulum stress-induced XBP1 mRNA splicing and protein expression, and has no cytotoxicity.

FB231 is a Parkin activator. FB231 can induce mild mitochondrial stress, resulting in impaired mitochondrial function and activation of the integrated stress response. FB231 can lower the threshold for mitochondrial toxins to induce PINK1/Parkin-mediated mitophagy. FB231 can cause activation of the integrated stress response (ISR) and perturbation to iron-dependent pathways. FB231 can be used for the research of neurological disease, such as Parkinson’s disease.

ML-93 is an orally active SAE inhibitor, with an IC50 value of 0.4 μM. ML-93 inhibits the SUMOylation pathway in HCT116 cells. ML-93 shows robust antitumor activity in the HCT116 colorectal carcinoma xenograft model. ML-93 can be used for the study of colorectal cancer.

VU6002703 (Compound 17) is a BBB-penetrable M4 mAChR positive allosteric modulator (PAM) with an EC50 of 0.6  μM for hM4. VU6002703 can be used for neuropsychiatric and rare genetic CNS disorders research.

CPI-203-PEG1-C3-O-COOH is a conjugate of the BRD4 ligand and the linker. CPI-203-PEG1-C3-O-COOH can be used for synthesizing PROTAC BRD4 degrader ARV-771

WML-01 is a fungicide with EC50s of 0.079, 0.72 and 2.02 μg/mL against F. graminearum, F. fujikuroi and S. sclerotiorum. WML-01 disrupts the cell membrane of F. graminearum and induces deposition of lipid droplets. WML-01 inhibits Deoxynivalenol (DON) biosynthesis with no cross-resistance and strongly suppresses ribosomal subunit assembly, impairing protein synthesis. WML-01 effectively controls the fusarium head blight (FHB) epidemic.

Y502-2304 is a c-Myc G-quadruplex stabilizer. Y502-2304 exhibits potent antiproliferative activity in multiple myeloma (MM) cells. Y502–2304 downregulates c-Myc mRNA and protein expression. Y502-2304 induces apoptosis in MM cells, characterizes by elevated γH2AX levels, increases reactive oxygen species (ROS) generation, and mitochondrial dysfunction. Y502-2304 significantly inhibits tumor growth in a xenograft MM model. Y502-2304 can be used for the study of multiple myeloma.

T-0902611 benzenesulfonate is a specific HCMV inhibitor. T-0902611 benzenesulfonate targets and covalently modifies the HCMV helicase–primase complex. T-0902611 benzenesulfonate can be used in the research of HCMV infection.

JY-21 is a BRD4 PROTAC degrader with a DC50 of 3.797 μM. JY-21 has a potent anticancer activity against MDA-MB-231 cells.

Type II TRK inhibitor 3 (Compound 18d) is a Type II TRK inhibitor with IC50 values of 0.82, 1.82, and 0.12 nM for TRKAWT/G595R/G667C, respectively. Type II TRK inhibitor 3 exhibits antitumor activity.

CTC 96 is an antiviral agent, showing inhibitory effects particularly on herpes viruses and adenoviruses. CTC 96 directly blocks the fusion process between the viral envelope and the cell membrane, preventing the entry of viral nucleic acids and proteins into the cells. CTC 96 can completely block the penetration and intercellular transmission of HSV-1, preventing the synthesis of viral proteins and mRNA. CTC 96 exhibits significant anti-adenovirus activity in rabbit eye models. CTC 96 is also effective against varicella-zoster virus (VZV) and vesicular stomatitis virus (VSV). CTC 96 can be used for broad-spectrum antiviral research.