isavuconazonium sulfate is hydrolyzed by plasma esterases to yield the active moiety isavuconazole. isavuconazole binds to and inhibits the fungal cytochrome p450 family enzyme lanosterol 14-alpha-demethylase (cyp51), which catalyzes the demethylation of
c-type natriuretic peptide (cnp) (1-22), human acetate is an agonist of natriuretic peptide receptor b (npr-b), an endothelial-derived relaxant and growth inhibitory factor. c-type natriuretic peptide (cnp) (1-22), human acetate inhibits camp synthesis s
cid5721353 is a b-cell lymphoma 6 inhibitor (bcl6 inhibitor) that disrupts bcl6/corepressor complexes in vitro and in vivo, and was shown to bind the critical site within the btb groove.
choline fenofibrate is a choline formulation of fenofibrate, a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.
radiprodil (rgh-896) is an orally active and selective nmda nr2b receptors antagonist. it was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (dpnp).
asapiprant (s-555739) is a potent and selective dp1 receptor antagonist (ki: 0.44 nm). it exhibited high affinity and selectivity for the dp1 receptor.
volinanserin (mdl 100907) is a potent and selective antagonist of the serotonin receptor 5-ht2 (ki: 0.36 nm) and shows 300-fold selectivity for 5-ht2 receptor over 5-ht1c, alpha-1 adrenergic and sigma receptors.
ck1-in-1, compound 1c reported in patent wo2015119579a1, is a casein kinase 1 (ck1) inhibitor. it has ic50s of 15 nm, 16 nm, 73 nm for ck1δ, and ck1ε, p38σ mapk, respectively.
prulifloxacin is a broad-spectrum fluoroquinolone antibiotic. it inhibits bacterial dna synthesis by inhibiting the activity of bacterial dna topoisomerase ii and iv.
bms-599626 (ac480) is a selective inhibitor of her1 and her2 (ic50s: 20 nm and 30 nm), ~8-fold less potent to her4, >100-fold to lck, vegfr2, c-kit, met, etc.
ddd107498 has a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the plasmodium parasite. it targets translation elongation factor 2 (eef2).
bms986195 is a potent, covalent inhibitor of bruton´s tyrosine kinase (btk), >5,000-fold selective over all kinases outside of the tec family (ic50 <1 nm for btk).
bi-3802 is a highly potent bcl6 degrader and inhibits the bric-à-brac (btb) domain of bcl6 with an ic50 value of ≤3 nm. bi-3802 induces the polymerization of bcl6 and promotes bcl6 degration depended on e3 ligase siah1. bi-3802 has antitumor activity[1][2
azd3229 is a potent pan-kit mutant inhibitor for the treatment of gastrointestinal stromal tumors. it demonstrates potent single-digit nm growth inhibition across a broad cell panel.
pd 158780 reversibly inhibits auto and transphosphorylation of all four members of the erbb receptor superfamily: egfr, erbb2, erbb3, and erbb4 (ic50s: 8μm, 49 nm, 52 nm, and 52 nm in cell assay).
ml-216 is a small molecule inhibitor of blm helicase (ic50: 1.8 μm). it showed 28-fold selective against the related helicases recq1, recq5, and e. coli uvrd (ic50s > 50 μm).
t-5224 is a transcription factor c-fos/ap-1 inhibitor, which specifically inhibits the dna binding activity of c-fos/c-jun without affecting other transcription factors.
ddd107498 has a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the plasmodium parasite. it targets translation elongation factor 2 (eef2).
cycloguanil is an active metabolite of the antimalarial compound proguanil. it acts as an inhibitor of dihydrofolate reductase (kis: 0.3 and 1.5 nm for plasmodium and human forms, respectively).
cid 1375606 is a surrogate agonist of orphan g protein-coupled receptor gpr27. characterized by a high level of conservation among vertebrates and a predominant expression in the central nervous system.
ml367 is a potent inhibitor of atpase family aaa domain-containing protein 5 (atad5) stabilization and acts as a probe molecule that has low micromolar inhibitory activity
dmnq is a 1,4-naphthoquinone that acts as a redox-cycling agent, typically increasing intracellular superoxide and hydrogen peroxide formation.dmnq increases ros generation