ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM. 了解更多

GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK). 了解更多

DPM-1001 is a potent, specific, orally bioavailable and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM, an an analog of the specific PTP1B inhibitor trodusquemine (MSI-1436; IC50=600 nM). DPM-1001 has anti-diabetic property. 了解更多

ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79?nM, 1580?nM and 1330?nM for human uPA, tPA, and plasmin, respectively. 了解更多

NGI-1 (ML414) is a potent oligosaccharyltransferase (OST) inhibitor, directly targeting and blocking the function of the OST catalytic subunits STT3A and STT3B. NGI-1 is a cell permeable inhibitor and can effectively reduce virus infectivity without affecting cell viability. 了解更多

SGL5213 is a potent, oral active and low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor, with IC50 values of 29 nM and 20 nM for hSGLT1 and hSGLT2, respectively. 了解更多

AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. 了解更多

AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity. 了解更多

TVB-3166 is an orally-available, reversible, potent, and selective FASN inhibitor, inducing apoptosis, inhibiting anchorage-independent cell growth under lipid-rich conditions, and inhibiting in-vivo xenograft tumor growth. 了解更多

SMAP-2 (DT-1154) is an orally bioavailable phosphatase 2A (PP2A) activator which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A. 了解更多

GB-88 is a novel selective, orally available PAR2 antagonist, inhibits PAR2 activated Ca2+ release with an IC50 of 2 ?M. 了解更多

GSK467 is a potent and selective inhibitor of KDM5 (also known as JARID1) with a Ki of 10 nM, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members. GSK467 exploits unique binding modes. 了解更多

ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. 了解更多

GNE-207 is a novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP. GNE-207 has excellent CBP potency (CBP IC50?=?1?nM, MYC EC50?=?18?nM), and it exhibits a good pharmacokinetic profile. 了解更多

PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively. 了解更多

AN7973 is the 6-carboxamide benzoxaborole, blocks intracellular parasite development and inhibits Cryptosporidium growth. AN7973 is orally active, possesses favorable safety, stability, and PK parameters, and is an exciting drug candidate for treating cryptosporidiosis. 了解更多

Cefprozil is an orally bioavailable, second generation, broad-spectrum cephalosporin antibiotic that inhibits the growth of both Gram-positive and Gram-negative bacteria. 了解更多

Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome. 了解更多

Dicloxacillin sodium is an oral semisynthetic isoxazolyl antistaphylococcal penicillin. Most active of the isoxazolyl antistaphylococcal penicillins. Stable against penicillinase and active against many of the penicillinase-producing strains of Staphylococcus aureus. Clinical uses include skin and soft-tissue, bone and joint, respiratory tract, and urinary tract infections. 了解更多

Polaprezinc is an orally bioavailable chelate composed of zinc and L-carnosine, with potential gastroprotective, anti-oxidant, anti-ulcer and anti-inflammatory activities. Upon administration, polaprezinc increases the expression of various anti-oxidant enzymes, such as superoxide dismutase 1 (SOD-1), SOD-2, heme oxygenase-1 (HO-1), glutathione S-transferase (GST), glutathione peroxidase (GSH-px), peroxidredoxin-1 (PRDX1; PRXI) and PRXD5 (PRXV) in the gastric mucosa, which protect cells against reactive oxygen species (ROS). 了解更多

Baclofen is a GABA agonist specific for GABA-B receptors. Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing It acts at spinal and supraspinal sites, reducing excitatory transmission. 了解更多

Peretinoin, also known as NIK-333 , orally available, acyclic retinoid with potential antineoplastic and chemopreventive activities. Peretinoin binds to and activates nuclear retinoic acid receptors (RAR), which in turn recruit coactivator proteins and promote, with other transcriptional complexes, the transcription of target genes. As a result, this agent may modulate the expression of genes involved in the regulation of cell proliferation, cell differentiation, and apoptosis of both normal and tumor cells. 了解更多

Norethindrone acetate is used in combination with estrogen as a contraceptive (oral). It is reasonably anticipated to be a human carcinogen. 了解更多

Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome. 了解更多

Lasofoxifene tartrate is a third-generation selective estrogen receptor modulator. 了解更多

Lusutrombopag, also known as S-888711, is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist being developed by Shionogi for chronic liver disease (CLD) patients with thrombocytopenia prior to elective invasive surgery. 了解更多

Pipobroman (trade names Vercite, Vercyte) is an anti-cancer drug that probably acts as an alkylating agent. 了解更多

Pantethine is a dimeric form of pantothenic acid, is an intermediate in the production of Coenzyme A, is available as a dietary supplement, and is used to treat acne and improve the blood-cholesterol profile. 了解更多

Cangrelor Tetrasodium is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. Unlike clopidogrel (Plavix), which is a prodrug, cangrelor is an active drug not requiring metabolic conversion. 了解更多

Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9. 了解更多

Acetylglucosamine or N-acetylglucosamine is potentially for the treatment of irritable bowel syndrome. N-Acetylglucosamine (GlcNAc) is a monosaccharide that usually polymerizes linearly through (1,4)-β-linkages. GlcNAc has been reported to be an inhibitor of elastase release from human polymorphonuclear leukocytes (range 8?C17% inhibition), however this is much weaker than the inhibition seen with N-acetylgalactosamine (range 92?C100%). 了解更多

Lactose is milk sugar. It is a disaccharide composed of one galactose and one glucose molecule. In the pharmaceutical industry, lactose is used to help form tablets because it has excellent compressibility properties. 了解更多

Aminosalicylic Acid, also known as Para-aminosalicylic acid (PAS), is one of the last remaining drugs available to treat extensively drug-resistant (XDR) tuberculosis. It is an antitubercular agent often administered in association with ISONIAZID. 了解更多

AMG-176 is a potent, selective and orally bioavailable MCL-1 inhibitor, with a Ki of 0.13 nM. 了解更多

PUN30119, also known as Imidazole ketone erastin (IKE), is a potent, metabolically stable inhibitor of system xc- and inducer of ferroptosis potentially suitable for in vivo applications. 了解更多

KL1333 is an orally available, small organic molecule that reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL-1333 Improves Energy Metabolism and Mitochondrial Dysfunction in MELAS Fibroblasts. 了解更多

DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor. DC661 inhibits autophagy. DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). 了解更多

SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected. 了解更多

SNJ-1945 is a calpain inhibitor with more favorable retinal penetration, high oral bioavailability, and long half-life. SNJ1945 rescued defective function in lissencephaly. 了解更多

JNJ-38877618 is a novel potent, highly selective, orally bioavailable c-Met tyrosine kinase inhibitor with Kd of 1.2, 2.1 and 21 nM for WT, M1250T and Y1235D mutants MET, respectively. 了解更多

PF-06260933 is a potent, selective, orally available MAP4K4 inhibitor with IC50 of 3.7 nM. 了解更多

AX-024 is an orally available inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation (IC50 value 1 nM). Inhibiting an immediate TCR signal has promise for treating a broad spectrum of human T cell-mediated autoimmune and inflammatory diseases. 了解更多

Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue). It is non-selective and inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively). Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively). 了解更多

Lipoic Acid, also known as R-(+)-alpha-Lipoic acid, is an organosulfur compound derived from octanoic acid. It is made in animals normally, and is essential for aerobic metabolism. It is also manufactured and is available as a dietary supplement in some countries where it is marketed as an antioxidant, and is available as a pharmaceutical drug in other countries. 了解更多

Pyrogallol is a polyphenol compound, which has anti-fungal and anti-psoriatic properties. Pyrogallol is a reductant that is able to generate free radicals, in particular superoxide anions. 了解更多

Harmine, also known as telepathine, is a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds. It occurs in a number of different plants, most notably the Middle Eastern plant harmal or Syrian rue (Peganum harmala) and the South American vine Banisteriopsis caapi (also known as "yage" or "ayahuasca"). Harmine reversibly inhibits monoamine oxidase A (MAO-A), an enzyme which breaks down monoamines, making it a RIMA. Harmine selectively binds to MAO-A but does not inhibit the variant MAO-B. 了解更多

Afloqualone, also known as HQ-495, is a centrally acting muscle relaxant. Afloqualone inhibits vestibular nystagmus probably due to both inhibition of selective polysynaptic transmission and enhancement of the effects of GABA and glycine in the lateral vestibular nucleus (LVN), and its GABA-enhancing effect is thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site. 了解更多

ML355 is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 0.34 μM, shows excellent selectivity over related lipoxygenases and cyclooxygenases, and possesses favorable ADME properties. 了解更多

AZ32是ATM激酶的特异性抑制剂，对小鼠具有良好的BBB渗透性，ATM酶的IC50值<0.0062 uM。它对ATR有足够的选择性，并且具有较高的细胞通透性。 了解更多