MMV665917 is an orally active piperazine derivative with anti-Cryptosporidium parvum activity with an EC90 of 15 μM. MMV665917 significantly reduces the parasite load in a porcine model infected with C. hominis, decreases ovarian excretion, alleviates diarrhea symptoms and reduces intestinal mucosal damage. MMV665917 can be used for research on Cryptosporidium parvum disease.

DDP-38003 (Compound 15) is an orally active KDM1A/LSD1 inhibitor with an IC50 value of 84 nM. DDP-38003 exhibits anticancer activity against promyelocytic leukemia.

WJM664 is a potent Plasmodium falciparum PfATP4 inhibitor. WJM664 shows strong activity against malaria parasites. WJM664 blocks gamete development and transmission to mosquitoes by inhibiting PfATP4-mediated Na+-dependent ATPase activity, and acts on multiple stages of the malaria parasite life cycle.

KR-26556 is a sulfonamide type hepatitis B virus (HBV) capsid assembly regulator. KR-26556 exhibits anti-HBV activity with an EC50 of 0.04 μM. KR-26556 has favorable safety characteristics. KR-26556 can be used for research on chronic hepatitis B.

LO-3-62 is a PROTAC-like SMARCA2/4 degrader with a truncated fumaramide handle. LO-3-62 degrades SMARCA2/4 in cells.

LO-3-61, a JQ-1 analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells.

RN341 is a specific type II kinase inhibitor of LRRK2 (IC50: 296 nM). RN341 inhibits LRRK2 phosphorylation and avoids S935 dephosphorylation by stabilizing the open conformation. RN341 rescues LRRK2-mediated kinesin motility block by preventing microtubule binding. RN341 effectively inhibits LRRK2 wild-type and G2019S mutant at the cellular level. RN341 provides a new direction for Parkinson's disease research.

FR-182980 is an orally active ACAT1 inhibitor (IC50: 30 nM). FR-182980 has hypocholesterolemic activity and can be used for research of atherosclerosis.

ZWZH-21 is a selective and orally active HDAC1/2 dual inhibitor with IC50 values of 34 nM for HDAC1 and 41 nM for HDAC2. ZWZH-21 can inhibit HCT116 and SW480 cells growth with IC50 values of 0.524 μM and 1.063 μM, respectively. ZWZH-21 can inhibit proliferation and migration and induces apoptosis in multiple colorectal cancer cells. ZWZH-21 can be used for the research of cancer, such as colorectal cancer.

LAG-3 Hit II is a LAG-3 inhibitor with a KD of 4.32  μM. LAG-3 Hit II can be used for cancers like ovarian cancer, colon adenocarcinoma and melanoma research.

CL-283796 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. CL-283796 reduces low-density lipoprotein (LDL) cholesterol without affecting cholesterol absorption in African green monkeys. CL-283796 can be used for hypercholesterolemia research.

E-2101 is a novel antispastic agent. E-2101 is a competitive CYP2C19 and CYP2D6 inhibitor with Ki values of 15 and 48 μM, respectively. E-2101 is metabolized by Cytochromes P450 to form monohydroxylated (M1 and M2), dihydroxylated (M3), and N-dealkylated metabolites (M4). E-2101 can be used in the research of skeletal muscle spasm.

KY-9 is an antibacterial active compound.

(R)-CFMB is the R-enantiomer of CFMB). CFMB is an agonist of FFAR2- and FFAR3-specific with an EC50 value of 0.8 μM target hFFAR2 and 0.2 μM target rFFAR2.

BAS00602705 is an E-cadherin inhibitor. BAS00602705 exerts its function by blocking the trans-interactions of E-cadherin molecules within junctional complexes, without permanently altering E-cadherin expression levels. BAS00602705 significantly impairs invadopodia formation in pancreatic cancer cells. BAS00602705 can be used for the study of anti-invasive therapeutic strategies in cancers characterized by dysregulated E-cadherin-mediated invadopodia activity, such as pancreatic ductal adenocarcinoma (PDAC).

(Rac)-Z-FA-FMK is the racemate of Z-FA-FMK. (Rac)-Z-FA-FMK is an inhibitor of cathepsin B with a Ki of 1.5 μM. (Rac)-Z-FA-FMK inhibits caspase-2, -3, -6, -7, and -9 with IC50s of 6.147, 15.41, 32.45, 9.077, and 110.7 μM. (Rac)-Z-FA-FMK inhibits the main protease of SARS-CoV-2 replication with an IC50 of 11.39 μM. (Rac)-Z-FA-FMK inhibits the increased IL-1β level induced by LPS and NF-κB transactivation in macrophages.

CRBN ligand-185 is a CRBN ligand. CRBN ligand-185 can be used as a target protein ligand for the synthesis of PROTACs targeting CRBN (Ligands for Target Protein for PROTAC), such as NX-5948.

TBIA (trans bis-isatoic anhydride) is a covalent RNA crosslinker. TBIA selectively induces RNA tertiary interactions (e.g., multi-helix junctions, loop-helix packing). TBIA is promising for research of RNA higher-order structure and disease-associated RNAs (e.g., KRAS-mutant RNAs).

(S)-MDL-101146 is the S-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis.

Ciprokiren (Ro 44-9375) is a Renin inhibitor with IC50s of 0.07 and 0.65 nM for hRenin in buffer and plasma, respectively. Ciprokiren be applied transdermally with similar hemodynamic effects without decrease of plasma renin activity or plasma immunoreactive angiotensin II. Ciprokiren has antihypertensive efficacy and can be used for hypertension research.

SGB-1534 (hydrochloride) is an orally active, selective and competitive antagonist of the alpha 1-adrenoceptor and the 5-HT2 receptor. SGB-1534 (hydrochloride) can inhibit vasoconstriction and lower blood pressure. SGB-1534 (hydrochloride) can be used for the research of cardiovascular disease, such as hypertension.

NCO-700 is a dual cathepsin B and calcium-activated neutral protease (CANP) inhibitor with IC50 values of 0.8 and 46 μM, respectively. NCO-700 reduces the degradation of myocardial fibrin by inhibiting protease activity. NCO-700 also has inhibitory effects on hormone-independent tumor cells, such as prostate cancer cells, and induces apoptosis. NCO-700 can be used to study myocardial ischemia and refractory hormone-independent tumors.

WB156 is a dual MDM2 and GSPT1 degrader. WB156 can recruit CRBN (Cereblon, a substrate receptor of the E3 ubiquitin-ligase complex) to induce the ubiquitination-proteasome pathway-mediated degradation of MDM2 and GSPT1. WB156 is promising for research of cancers, such as leukemia.

ML256 is a covalent lipoprotein-associated phospholipase A2 (Lp-PLA2 inhibitor. ML256 can be used for the study of neoplasms harboring a constitutively active variant of one or both of KRAS or HRAS.

RJG-2036 is a potent covalent inhibitor of human prostaglandin reductase 2 (PTGR2)(IC50=100 nM). RJG-2036 inhibits NADPH-dependent reduction, significantly reducing secretion of proinflammatory cytokines like TNF-α and multiple eicosanoids in LPS-stimulated THP-1 macrophages. RJG-2036 is promising for research of inflammatory diseases.

JSZ16 is a Succinate dehydrogenase (SDH) inhibitor with an IC50 of 30.3  μM. JSZ16 has potent broad-spectrum fungicidal activity, such as Sclerotinia sclerotiorum, Botrytis cinerea and Colletotrichum fragariae, with an EC50 of 4.4 mg/L for Sclerotinia sclerotiorum. JSZ16 influences the cell membrane permeability of pathogenic fungi. JSZ16 can be used for the development of fungicide.

PAD-PF1 is a PAD4 inhibitor (IC50: 15.9 µM). PAD-PF1 binds to an allosteric site of PAD-PF1, which is distinct from substrate and GSK147.

PAD-PF2 is a PAD4 inhibitor with a Kd of  2.82 µM. PAD-PF2 inhibits Ionomycin-induced protein citrullination in human isolated neutrophils.

SB-247853 is a highly specific 5-HT2c receptor antagonist. SB-247853 induces orthostatic intolerance during head-up tilting. SB-247853 can be used in the research of cardiovascular diseases.

ESC1002755 is a 17β-HSD10 inhibitor with an IC50 of 19 nM. ESC1002755 has significant enzyme specificity with non-/uncompetitive inhibition against the cofactor NADH. ESC1002755 shows minimal cytotoxicity towards the HEK293 at 50 μM. ESC1002755 is promising for Alzheimer’s disease and hormone-dependent cancers (such as prostate, bone and colorectal cancer) research.