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.

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 tricyclic antidepressant that inhibits the reuptake of serotonin and norepinephrine and acts as an antagonist at histamine, serotonin, adrenergic, and muscarinic receptors with Ki values in the nanomolar range.

An agonist of α2 adrenergic receptors (Ki = 194 nM); used for sedation, anesthesia, and analgesia in non-human mammals.

An NSAID commonly used in animals to combat pain and inflammation, particularly as associated with osteoarthritis; inhibits both COX-1 and COX-2 (IC₅₀s = 22.3 and 3.9 µM, respectively) and also FAAH (IC₅₀ = 74 µM).

A dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC₅₀ = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+…

A thio analog of the purine base guanine that incorporates into DNA during replication, inducing double-strand breaks that destabilize its structure and result in cytotoxicity; used as a chemotherapeutic for acute leukemia and other types of cancer, including BRCA2-mutated tumors.

Produced in fungi, including yeast, and invertebrates from ergosterol in response to ultraviolet radiation; metabolized first to 25-hydroxyvitamin D2 and subsequently to the active 1,25-dihydroxyvitamin D2.

An amino-amide anesthetic that binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, preventing the generation of an action potential; inhibits the uptake of dopamine in striatal synaptosomes by 47% at 100 µM.

A dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle; inhibits calcium-induced contractions in depolarized rat aorta (IC₅₀ = 1.9 nM), displaying a slow rate of association and dissociation in isolated vascular and…

A classical inhibitor of complex I of the mitochondrial electron transport chain, inhibiting NADH/DB oxidoreductase and NADH oxidase with IC₅₀ values of 28.8 and 5.1 nM, respectively; used in animal models of Parkinson’s disease.

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

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.

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 NSAID that acts as a COX-2 inhibitor (IC₅₀s = 20 and 322 nM for COX-1 and COX-2, respectively).

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

An antimalarial drug used in the treatment of persistent liver forms of P. vivax or P. ovale infection for its ability to kill late-stage gametocytes and hypnozoites.

A phenothiazine classified as an antipsychotic compound; antagonizes dopamine and serotonin receptors (Kis = 0.66, 0.84, 1.2, and 1.8 nM for D2, D3, D4, and 5-HT2A, respectively); also antagonizes histamine, α1- and α2-adrenergic, and muscarinic acetylcholine receptors.

An α2-adrenergic receptor agonist (Kd = 7.6 nM for rat cerebral cortex membranes) that has transient antihypertensive effects; used in managing opioid withdrawal symptoms during detoxification from heroin and methadone.

A racemic mixture of two optically active isomers, the R and S forms; has a half-life of 36-42 hours in circulation, bound to plasma proteins, and accumulates in the liver, where the two isomers are metabolized by different pathways; also used as a rodenticide.

A centrally acting α2-adrenergic receptor agonist that decreases peripheral vascular resistance by centrally inhibiting sympathetic nerve activity; also acts as an agonist of the imidazoline (I1) receptor (Ki = 4-8 nM).

An inhibitor of URAT1 (IC₅₀ = 0.3 µM for hURAT1) that prevents renal urate resorption; also potently inhibits CYP2C9 (Ki = 20 nM) and has been used to study adverse drug-drug interactions.

A selective agonist of GABAB (IC₅₀ = 200 nM); causes skeletal muscle relaxation and blocks spasticity.

A centrally acting M1 muscarinic acetylcholine receptor antagonist (Ki = 0.59 nM in rat) that also inhibits dopamine uptake through the dopamine transporter (Ki = 160 nM); used in the management of Parkinson’s disease symptoms to address involuntary tremor and dystonia.

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

The prototypical blocker of L-type calcium channels that produces excitation-contraction uncoupling in cardiac muscle by preventing the slow-inward current of Ca2+ (IC₅₀ = 0.38 μM in guinea pig aortic strip).

An agonist of both nAChR and mAChR receptors, with reported Ki values ranging from 10 to 10,000 nM for different receptors and different preparations; used to study responses mediated by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling.

A natural naphthoquinone that has allelopathic actions, suppressing growth, photosynthesis, and respiration in plants and other organisms; irreversibly inhibits peptidyl-prolyl cis/trans isomerases of the parvulin family, including human Pin1, yeast Ess1/Ptf1, and E. coli parvulin (Ki = 55.9 nM).

A polypeptide antibiotic effective against Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumoniae.

An intermediate form of vitamin D which is obtained from dietary sources, such as fish, or through the conversion of 7-dehydrocholesterol by ultraviolet light; metabolized to the active form 1,25-dihydroxyvitamin D3 by CYP450 isoforms in the liver.

An irreversible inhibitor of mitochondrial Complex II succinate dehydrogenase, resulting in energy depletion through disruption of the electron transport chain; used in animal models of Huntington’s disease and epilepsy.