biapenem is a 1-beta-methylcarbapenem antibiotic with a wide range of antibacterial activity. biapenem has similar antibacterial activity to that of imipenem, but is more stable against human renal dehydropeptidase-i and with less neurotoxicity.
baf312 (siponimod), a next-generation s1p receptor modulator, is specific for s1p1 and s1p5 receptors with ec50 of 0.39 nm and 0.98 nm,respectively. the specificity of baf312 for s1p1 and s1p5 receptors exhibits >1000-fold over s1p2, s1p3 and s1p4 recepto
azd1981 is an effective and specific crth2 (dp2) receptor antagonist (ic50: 4 nm), showing >1000-fold selectivity over more than 340 other enzymes and receptors, including dp1. azd1981 has been used in trials studying the treatment and basic science of as
azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
atracurium besylate is a non-depolarizing neuromuscular blocking agent with short duration of action. its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alterna
at101, the r-(-) enantiomer of gossypol acetic acid, binds with bcl-2, bcl-xl and mcl-1 with ki of 0.32 μm, 0.48 μm and 0.18 μm; does not inhibit bir3 domain and bid. phase 2.
astragaloside a (astragaloside iv) is the primary pure saponin isolated from astragalus membranaceus, which has been widely used for the therapy of cardiovascular diseases.
as-604850 is a specific and atp-competitive pi3kγ inhibitor (ic50: 250 nm), 18-fold more selective for pi3kγ than pi3kα, and over 80-fold selectivity for pi3kγ than pi3kδ/β.
anacardic acid is an effective inhibitor of p300 and p300/cbp-associated factor histone acetyltranferases. it also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.
amprenavir is a synthetic derivative of hydroxyethylamine sulfonamide that selectively binds to and inhibits human immunodeficiency virus (hiv) protease.
ampicillin sodium is the sodium salt form of ampicillin, a broad-spectrum semisynthetic derivative of aminopenicillin. ampicillin sodium inhibits bacterial cell wall synthesis by binding to penicillin binding proteins, thereby inhibiting peptidoglycan syn
amg 900 is a potent and highly selective pan-aurora kinases inhibitor for aurora a/b/c with ic50 of 5 nm/4 nm /1 nm. it is >10-fold selective for aurora kinases than p38α, tyk2, jnk2, met and tie2. phase 1.
amonafide(as1413) produces protein-associated dna-strand breaks through a topoisomerase ii-mediated reaction, but does not produce topoisomerase i-mediated dna cleavage.
tubacin is a highly potent and selective, reversible, cell-permeable hdac6 inhibitor with an ic50 of 4 nm, approximately 350-fold selectivity over hdac1.
bix02188 is a specific mek5 inhibitor (ic50: 4.3 nm), also inhibits erk5 catalytic activity (ic50: 810 nm), and does not inhibit closely related kinases mek1/2, jnk2, and erk2.
oligomycin a is an inhibitor of atp synthase, inhibits oxidative phosphorylation and all the atp-dependent processes occurring on the coupling membrane of mitochondria.
copanlisib is a phosphoinositide 3-kinase (pi3k) inhibitor with potential antineoplastic activity. copanlisib inhibits the activation of the pi3k signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell
osi-027 is a selective and potent dual inhibitor of mtorc1 and mtorc2 with ic50 of 22 nm and 65 nm, and more than 100-fold selectivity observed for mtor than pi3kα, pi3kβ, pi3kγ or dna-pk. phase 1.
calcitriol is the physiologically active form of vitamin d. it is formed primarily in the kidney by enzymatic hydroxylation of 25-hydroxycholecalciferol (calcifediol). its production is stimulated by low blood calcium levels and parathyroid hormone. calci
bafetinib (inno-406) is an effective and specific dual bcr-abl/lyn inhibitor (ic50: 5.8/19 nm), and no inhibition of the phosphorylation of the t315i mutant and less effective to c-kit and pdgfr.