An antibacterial and coccidiostat compound that shows selective toxicity for HMLER breast cancer stem cells (IC₅₀ = ~24 μM); 8 μM treatment of 4T1 and MCF-7-Ras breast cancer cell lines decreases cancer stem cell growth ~2-fold and ~3-fold, respectively; 5 mg/kg inhibits mammary…

An orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC₅₀ = 63.5 nM), as well as a variety of other CYP isoforms.

Pargyline is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension. At 10 mg/kg iv, pargyline induces a moderate decrease of systolic blood pressure in unanaesthetized hypertensive rats but not normotensive WKR or Sprague-Daley rats. The…

An inhibitor of protein synthesis in eukaryotes (IC₅₀ = 5-50 μM) that functions by interfering with translational elongation; can either induce or inhibit apoptosis depending on cell type.

A cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

The primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper and present in natural hot pepper extracts; elicits a sensation of burning pain by activation of TRPV1 on small, non-myelinated polymodal C-type nociceptive nerve fibers and has been widely…

A dipyridinyl compound that demonstrates high in vitro and ex vivo selectivity for COX-2 over COX-1.

A DNA alkylating agents that induces DNA interstrand and intrastrand crosslinks, cytotoxicity, and apoptosis; inhibits the growth of PC-3 prostate cancer cells with IC₅₀ values of 0.074 or 0.77 μM for sequential dosing or single dosing, respectively.

A prodrug for A-771726 that regulates T lymphocyte progression through the cell cycle by selectively inhibiting de novo pyrimidine synthesis; used to slow the disease progression of rheumatoid arthritis and as an immunosuppressive agent to prevent rejection of transplant allografts and xenografts.

An agonist of muscarinic receptors (EC₅₀ = 1.8-17 µM for human M2).

A selective α2-adrenergic receptor agonist (Ki = 183 nM) that lowers intraocular pressure by decreasing aqueous humor synthesis and increasing drainage through uveoscleral outflow; protects rat retinal ganglion cells against glutamate excitotoxicity by inhibiting glutamate release and…

A histamine H1 receptor antagonist (Ki = 9 nM) that is effective against HCV (EC₅₀ = 44 nM), preventing viral entry into host cells.

An immunomodulatory and antiproliferative compound that interacts directly with the protein CRBN (IC₅₀ = 8.5 nM), a ubiquitously-expressed E3 ligase, and DDB1 complexes.

A second-generation antipsychotic designed to antagonize both D2 and 5-HT2A receptors with little effect on cholinergic and β-adrenergic receptors; affects α2-adrenergic and histamine H1 receptors.

A potent antagonist of dopamine receptors (IC₅₀s = 1.0 and 0.9 nM for D2 and D3, respectively);,also avidly binds α1- and α2-adrenergic receptors, histamine H1 receptor, and serotonin (5-HT) receptors 5-HT1D and 5-HT2A (Kis = 10, 80, 3.4, 19, 1.2 nM, respectively).

An HDAC inhibitor, antitumor agent that at 10 μM can induce oxidative stress contributing to apoptosis and differentiation in MCF-7 breast cancer cells; inhibits T. gondii tachyzoite propagation in human fibroblasts (EC₅₀ = 80 nM) and inhibits P. falciparum growth in human red blood…

An anti-protozoal agent; prevents misfolding of prion protein (EC₅₀ = 0.3 μM), blocks voltage-dependent sodium channels (IC₅₀ = 3.3 μM), inhibits aldehyde oxidase (IC₅₀ = 3.3 μM), antagonizes the riboflavin-binding protein (Ki = 6.7 μM), inhibits…

An inhibitor of Nav, blocking human Nav1.2, Nav1.5, and Nav1.8 with IC₅₀ values of 10, 62, and 96 μM, respectively.

A potent, clinically-useful immunosuppressant; binds to FK-506 binding protein 12 (Ki = 0.2 nM) to inhibit calcineurin; regulates NO neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and IP3 receptors.

A potent and selective inhibitor of type 3 PDEs, inhibiting recombinant PDE3A and PDE3B with IC₅₀ values of 0.45 and 1.0 μM, respectively; has positive inotropic (stimulates cardiac muscle contractions) and vasodilatory effects when administered in vivo.

An irreversible inhibitor of AChE (IC₅₀ = 4.15 µM) and BuChE (IC₅₀ = 37 nM); used in modifying the course of neurodegenerative diseases.

A mixture of the natural macrocyclic lactones avermectin B1a and avermectin B1b that has both insecticidal and anthelmintic actions.

An acyclic nucleoside phosphonate that acts as a reverse transcriptase inhibitor; demonstrates antiviral activity against herpes viruses, hepatitis B virus, and HIV in animal and clinical models of infections.

Blocks and reverses platelet aggregation induced by such triggers as collagen, U-46619, and ADP (IC₅₀ = 1.1, 2.1, and 4.1 µM, respectively); reduces tyrosine phosphorylation in stimulated platelets and inhibits recombinant human Syk and Src (IC₅₀ = 2.8 and 27.3 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 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 butyrophenone derivative which is used in the treatment of schizophrenia and delirium; binds to the dopamine D2 receptor (Ki = 0.1 nM), antagonizing dopamine signaling.

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).

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…