MEPB is a modulator of AF-2 of the androgen receptor. MEPB increases co-repressor binding of AR. MEPB can bind to the BF3 pockeet of AR specifically, thereby modulating the binding of co-regulators to the AF2 domain. MEPB alleviates degeneration in spinal bulbar muscular atrophy mouse model.

FLM-5011 is a lipoxygenase inhibitor. FLM-5011 can diminish myocardial ischaemia injury and shows anti-inflammatory effect. FLM-5011 can be used for the researches of inflammation and cardiovascular disease, such as myocarditis.

Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.

Gamhepathiopine is a thienopyrimidinone compound. Gamhepathiopine exerts antimalarial effects by targeting the Qo site of Plasmodium falciparum cytochrome b and inhibiting the activity of complex III in the electron transport chain.

dRRM-1 is a DCAF15-dependent molecular glue degrader of RBM39 and RBM23. dRRM-1 can rescue the self-degradation of DCAF15. dRRM-1 can be used for the research of cancer.

BWD is a PSMA ligand (IC50 = 35.86). BWD exhibits excellent in vitro stability and high affinity. BWD can enhance tumor uptake and retention. BWD can inhibit tumor growth in vivo. BWD can be studied in anticancer research.

BIRB-1017 is a potent inhibitor of p38 MAP kinase. BIRB-1017 can be used in inflammation research.

PQM-244 (Compound 5c) is an orally active and multi-target modulator of TRPV1 and CB1 and CB2 receptors. PQM-244 has significant peripheral antinociceptive effects on both neurogenic and inflammatory phases. PQM-244 also has potential antioxidant activity with an IC50  of  14.15 µM for radical scavenging DPPH. PQM-244 can be used for chronic pain and inflammatory disease research, such as diabetes, atherosclerosis and Alzheimer’s disease.

4-Hydroxy xylazine O-glucuronide (lithium) is a metabolite of the α2-adrenergic receptor agonist xylazine. 4-Hydroxy xylazine O-glucuronide (lithium) can be synthesized from xylazine via the intermediate metabolite 4-hydroxy xylazine.

ECC-5004 (Compound 1) is a GLP-1 receptor agonist with an EC50 of 0-20 nM. ECC-5004 exhibits strong inhibitory effects on OATP1B1, with an IC50 < 1 μM. ECC-5004 can be used to study diseases such as diabetes, obesity, and non-alcoholic fatty liver disease.

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.

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.

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).

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