Biologically Active Small Molecules

A nucleoside analog that inhibits ribonucleotide reductase and DNA polymerase-&alpha (IC₅₀s = 65 and 3.9 nM, respectively) and is cytotoxic to K562 myelogenous leukemia cells (IC₅₀ = 5 nM) as well as various other leukemias

A PPAR&alpha agonist used clinically to treat dyslipidemia and cardiovascular disease exhibits EC50 values of 50 and 55 &microM for mouse and human PPAR&alpha, respectively.

A PPAR&alpha agonist used clinically to treat dyslipidemia and cardiovascular disease exhibits EC50 values of 50 and 55 &microM for mouse and human PPAR&alpha, respectively.

A PPAR&alpha agonist used clinically to treat dyslipidemia and cardiovascular disease exhibits EC50 values of 50 and 55 &microM for mouse and human PPAR&alpha, respectively.

A PPAR&alpha agonist used clinically to treat dyslipidemia and cardiovascular disease exhibits EC50 values of 50 and 55 &microM for mouse and human PPAR&alpha, respectively.

A SERM that impairs the activation of ERs by 17&beta-estradiol potently binds both ER&alpha and ER&beta (Ki = 0.9 and 1.2 nM, respectively) enhances the release of gonadotropin-releasing hormone, culminating in ovulation.

A SERM that impairs the activation of ERs by 17&beta-estradiol potently binds both ER&alpha and ER&beta (Ki = 0.9 and 1.2 nM, respectively) enhances the release of gonadotropin-releasing hormone, culminating in ovulation.

A SERM that impairs the activation of ERs by 17&beta-estradiol potently binds both ER&alpha and ER&beta (Ki = 0.9 and 1.2 nM, respectively) enhances the release of gonadotropin-releasing hormone, culminating in ovulation.

A SERM that impairs the activation of ERs by 17&beta-estradiol potently binds both ER&alpha and ER&beta (Ki = 0.9 and 1.2 nM, respectively) enhances the release of gonadotropin-releasing hormone, culminating in ovulation.

A tricyclic antidepressant that potently inhibits serotonin and norepinephrine reuptake (Kis = 7.4 and 96 nM, respectively) also an antagonist at histamine, muscarinic acetylcholine, &alpha1-adrenergic, and dopamine receptors (Kds = 31, 37, 38,

A centrally acting &alpha2-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).

A centrally acting &alpha2-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).