Bicalutamide

A Gcn5 and pCAF HAT inhibitor.

A synthetic intermediate useful for pharmaceutical synthesis.

A bactericidal thioamide effective against M. tuberculosis (MIC = ~0.5 &microg/ml), M. leprae (MIC = 0.8-1.6 mg/L), and M. avium inhibits mycolic acid biosynthesis (Ki = 2 nM).

A neutral RAR&alpha-selective antagonist (Ki = 2.5 nM) antagonizes agonist-induced coactivator recruitment and moderately decreases SMRT binding to RAR but does not significantly affect nuclear receptor corepressor binding.

Stabilizes HIF from degradation in the proteasome and increases endogenous production of erythropoietin by inhibiting HIF-1&alpha prolyl hydroxylase (IC₅₀ = 0.49 &microM) investigated in clinical trial for treatment of patients with

SKF 38393 is a partial agonist of the dopamine D₁-like receptors D₁ and D₅ (K_is = 1 and ~0.5 nM, respectively).

A derivative of GABA that acts as an antagonist of GABAA receptors (Ki = 74-150 nM) elicits seizures when administered intravenously in mice effective against GABAA receptor isoforms from mice, rats, and humans.

SEIT is a potent inhibitor of NOS in vitro but lacks good in vivo efficacy due to poor cellular penetration. The Ki values are 19, 39, and 29 nM using purified human iNOS, eNOS, and nNOS, respectively.

A reversible inhibitor of both agonist and antagonist binding to diverse GPCRs blocks the binding of radiolabeled ligands to human opioid, adrenergic, muscarinic, dopaminergic, adenosine, and purinergic receptors with IC₅₀ values of 0.1

A prodrug for methylprednisolone has superior water solubility compared to the active glucocorticoid.

A methylated derivative of PRIMA-1 that restores tumor-suppressor function to mutant p53 and induces cell death in various cancer cell lines synergizes with chemotherapeutic drugs to induce tumor cell apoptosis.

A selective, positive allosteric modulator of mGluR2, stimulating the human and rat receptors with EC50 values of 33.2 and 96 nM, respectively can be used on cells, tissues, or animals.