ML303 is a pyrazolopyridine influenza virus nonstructural protein 1 (NS1) antagonist (IC90 = 155 nM), with an EC50 of 0.7 μM for Influenza A virus H1N1.
NBT(Nitro BT;p-Nitrotetrazolium blue) is a substrate for dehydrogenases; is used with the alkaline phosphatase substrate 5-Bromo- 4-Chloro-3-Indolyl Phosphate (BCIP) in western blotting and immunohistological staining procedures.
Scopine is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock. Target: α1-Adrenergic ReceptorScopine is a tropane alkaloid found in a variety of plants including Mandragora root, Senecio mikanoides (Delairea odorata), Scopolia carniolica and Scopolia lurida. Scopine can be prepared by the hydrolysis of scopolamine. From Wikipedia.
Methyl 3-O-methylgallate (M3OMG) possesses antioxidant effect and can protect neuronal cells from oxidative damage.
Manidipine is a calcium channel blocker that is used clinically as an antihypertensive. Target: Calcium ChannelManidipine is a dihydropyridine calcium antagonist, which causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. Manidipine was well tolerated in clinical trials, with most adverse effects related to vasodilation . Manidipine is a lipophilic, third-generation dihydropyridine calcium channel antagonist with a high degree of selectivity for the vasculature, thereby inducing marked peripheral vasodilation with negligible cardiodepression. manidipine represents a first-line treatment option for patients with essential mild-to-moderate hypertension . Manidipine has neutral effects on glucose and lipid metabolism and is generally well tolerated. Manidipine thus represents a first-line option for lowering BP in patients with mild-to-moderate hypertension .
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
Ruxolitinib phosphate is a potent JAK1/2 inhibitor with IC50s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.
pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
LY354740 is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
Ethynodiol diacetate is a steroidal progestin which is used as a hormonal contraceptive, it has relatively little or no potency as an androgen,has significant estrogenic effects.
RMI 10874 is a tilorone analogue. Tilorone is a small-molecule, orally bioavailable antiviral agent. RMI 10874 completely abolishes lung colonization of an H-2 negative (GR9.B9) MCA-induced fibrosarcoma clone.
GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.
Piperidolate hydrochloride is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs).
BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has potential for the treatment of poorly controlled asthma.
Campathecin is a potent DNA enzyme topoisomerase I inhibitor, with an IC50 of 679 nM.
Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).
Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist).
PF 03716556 is a potent, and selective acid pump (H+,K+ ATPase) antagonist, with pIC50 value of 6.009.IC50 value:6.009 (pIC50)Target: H+,K+ ATPasePF-03716556 inhibited the activity of H+, K+-ATPase with pIC50 of 6.026 ± 0.112, 6.038 ± 0.039 and 6.009 ± 0.209 at pH 6.4 for porcine, canine and human ion-leaky membrane vesicles, respectively. PF-03716556 (PF03716556) is useful for treatment of gastroesophageal reflux disease.
Framycetin (Fradiomycin B; Neomycin B) is an aminoglycoside antibiotic. It inhibits hammerhead ribozyme with a Ki of 13.5 μM.
Sulfamethazine is a sulfonamide antibacterial.Target: AntibacterialSulfamethazine is an antibiotic used to treat bronchitis, prostatitis and urinary tract infections. Sulfamethazine blocks the synthesis of dihydrofolic acid by inhibiting dihydropteroate synthase. In addition, sulfamethazine is a structural analog and competitive antagonist of para-aminobenzoic acid (PABA) and can inhibit normal bacterial utilization of PABA for the synthesis of folic acid, which is an important metabolite in DNA synthesis [1, 2].
KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.
WAY-262611 is a wingless β-Catenin agonist that increases bone formation rate with an EC50 of 0.63 μM in TCF-Luciferase assay.
Tiotropium Bromide hydrate is an anticholinergic and bronchodilator and a muscarinic receptor antagonist.Target: mAChRTiotropium bromide (Ba 679 BR) is a novel potent and long-lasting muscarinic antagonist that has been developed for the treatment of chronic obstructive airways disease (COPD). Binding studies with [3H]tiotropium bromide in human lung have confirmed that this is a potent muscarinic antagonist with equal affinity for M1-, M2- and M3-receptors and is approximately 10-fold more potent than ipratropium bromide. In vitro tiotropium bromide has a potent inhibitory effect against cholinergic nerve-induced contraction of guinea-pig and human airways, that has a slower onset than atropine or ipratropium bromide. tiotropium bromide dissociates slowly from M3-receptors (on airway smooth muscle) but rapidly from M2 autoreceptors (on cholinergic nerve terminals) . Tiotropium bromide is a quaternary ammonium derivative that binds to muscarinic receptors. However, although tiotropium binds with high affinity to muscarinic receptors of M1-, M2- and M3-subtypes, it dissociates very slowly from M1- and M3-receptors but more rapidly from M2-receptors, thereby giving it a unique kinetic selectivity .
BMS-538203 is a highly efficient HIV integrase inhibitor and antiviral agent.IC50 value:Target: HIV integraseIn the current study we demonstrate a hit-to-clinical candidate pathway that resulted in 50- and 2000-fold improvements in enzyme-inhibition and antiviral activity without an increase in molecular weight or change in molecular topology. The original hit , 1 (mw = 268) was optimized in a stepwise manner. Potential covalent protein-binding moieties were removed by reducing the number of the ketone groups. High enzyme inhibition activity was achieved by optimizing the aryl-portion of the molecule. Protein binding was reduced by replacing the standard amide by the corresponding methyl-hydroxamide. This eventually led to the discovery of BMS-538203 compound 2 (mw = 269) a highly efficient inhibitor and antiviral agent.