A selective TLR8 agonist that induces activation of NF-κB at 0.4 uM.

A selective TRPM8 channel blocker with pEC50 of 6.91 in Ca(2+) influx assay, with no activity for TRPV4 (pEC50<4.6).

A selective α2A receptor agonist that can reduce peripheral sympathetic outflow and thus cansues a reduction in peripheral sympathetic tone.

A selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension..

A selective, G protein-biased µ-opioid receptor agonist, does not promote the development of opioid-induced mechanical allodynia (OIMA) and rapidly reverses allodynia in vivo..

A selective, G protein-biased µ-opioid receptor agonist, does not promote the development of opioid-induced mechanical allodynia (OIMA) and rapidly reverses allodynia in vivo..

A selective, non-competitive inhibitor of the kinetoplastid proteasome, inhibits the chymotrypsin-like activity of the T. cruzi proteasome with IC50 of 35 nM.

A selective, nonpeptidic, noncompetitive BACE1 inhibitor with IC50 of 3.15 uM in cell-free assays.

A selective, orally active JAK3 inhibitor that reduces IL-2-mediated JAK3 tyrosine phosphorylation with cellular IC50 of 10-20 uM.

A selective, orally bioactive and brain permeable δ-secretase (AEP.

A selective, potent peptidyl blocker of the big conductance Ca2+-activated K+ channel (BKCa, KCa1.1, MaxiK) with IC50 of 0.25 nM.

A selective, potent peptidyl blocker of the big conductance Ca2+-activated K+ channel (BKCa, KCa1.1, MaxiK).

A selective, reversible inhibitor of MAO-A and serotonin reuptake inhibitor as an antidepressant..

A selective, reversible inhibitor of MAO-A and serotonin reuptake inhibitor as an antidepressant..

A selective, reversible, high-affinity PAI-1 inhibitor that prevents PAI-1 from inactivating tPA and uPA with similar potency (IC50=30 and 25 nM, respectively).

A selective, small molecule inhibitor of PIP5K1C with IC50 of 41 nM, does not ihibits other lipid kinases including PI3Ks.

A selective, water-soluble, in vivo long-lasting AMPA antagonist with Ki of 43 nM.

A sepecific, orally bioavailable SHIP1 activator with no effect on functional androgen, oestrogen, oestrogen-related receptor α, glucocorticoid, mineralocorticoid and progesterone receptor at 30 uM.

A serine protease inhibitor that inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM).

A short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD)..

A short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD)..

A simple DBCO-containing building block used to derivatize carboxyl groups in the presence of activators (e.g. EDC, or DCC) or activated esters (e.g. NHS esters) with DBCO moiety through a stable amide bond.