An anthelmintic antibiotic that at 0.001 µg/ml is fully effective at inhibiting growth in an H. contortus larval development assay.

A trisubstituted thiophene that selectively inhibits USP7 and the closely related USP47 (EC₅₀s = 4.2 and 4.3 μM, respectively); accelerates the degradation of the USP7 substrate HDM2 in several multiple myeloma cell lines (EC₅₀ =11 μM).

A non-selective inhibitor of NOS isoforms in vitro (IC₅₀s = 0.71, 0.78, and 5.8 µM for rat nNOS, bovine eNOS, and rat iNOS, respectively); shows good anti-nociceptive effects without affecting blood pressure via inhibition of eNOS in vivo.

A non-sedating ophthalmic antihistamine that antagonizes histamine H1 receptors (IC₅₀ = 1.58 nM) and prevents the release of pro-inflammatory mediators from mast cells and eosinophils.

An antitumor antibiotic that induces apoptosis in mature monocytic U937 and myelocytic HL-60 acute myeloid leukemia cells at 0.2-1 μM; triggers a ROS-dependent sphingomyelin-ceramide pathway that activates the MEKK1-SEK1-JNK.

An inhibitor of class I HDACs with IC50 values of 0.9, 0.9, 1.2, and >20 μM for recombinant human HDAC 1, 2, 3, and 8, respectively; displays a wide spectrum of antitumor activity, particularly in tumors normally refractory to conventional anticancer agents.

An NSAID that potently inhibits both COX-1 and COX-2 (IC₅₀s = 5 and 8 nM, respectively); used, in a variety of different formulations, as an analgesic.

An inhibitor of CTP:phosphocholine cytidylyl transferase with antimetastatic properties.

A potent MAO inhibitor that preferentially targets MAO-A over MAO-B (Kis = 0.054 and 58 µM, respectively); also inhibits the sigma receptor σ1 on Jurkat human T lymphocyte cells (IC₅₀ = 31 nM).

The active metabolite of irinotecan that potently inhibits DNA topoisomerase I; more cytotoxic to HT-29 colon cancer cells (IC₅₀ = 8.8 nM) compared to irinotecan (IC₅₀ > 100 nM).

A high-affinity, lipophilic, non-selective ligand of the β-adrenergic receptors (Kis = 0.114 and 0.4 nM for β2- and β3-adrenoceptors, respectively); acts as a receptor antagonist (beta blocker) or inverse agonist for β1 and β2 receptors but functions as an agonist at the…

A carbamate pesticide that reversibly inhibits acetylcholinesterase.

A full agonist of the serotonin 5-HT1A receptor and antagonist of 5-HT2A (Kis = 1 and 49 nM, respectively); also binds to dopamine D4 receptors (Kis = 4-24 nM); reduces 5-HT in the prefrontal cortex and dorsal raphe of conscious rats while increasing extracellular noradrenaline and dopamine.

A nitrogen mustard alkylating agent used as a chemotherapeutic agent against advanced transitional cell carcinoma; serves as a prodrug that is metabolized to its active DNA alkylating form, isophosphoramide mustard.

A sympathomimetic β2-adrenoceptor agonist that relaxes bronchial smooth muscle and at higher doses acts as an anabolic steroid, promoting skeletal muscle protein synthesis.