ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.

HSD-016 (HSD016) is a potent, selective, and efficacious 11β-HSD1 inhibitor with IC50 of 149 and 530 nM for mouse and human 11β-HSD1, respectively.

INCB13739 (INCB-13739) is a potent, selective, oral 11βHSD1 inhibitor (IC50=1.1 nM) with high seelctivity over other dehydrogenases, glucocorticoid and mineralocorticoid receptors..

(E/Z)-4-hydroxy Tamoxifen is an active metabolite of tamoxifen that is formed by the action of cytochrome P450 2D6 in human liver.

(R)-(-)-Rolipram is a potent and cAMP-specific PDE4 inhibitor with IC50 of 0.22 uM; 2.5-fold more potent than (+)-rolipram (IC50= 2.58 uM) in inhibiting membrane-bound PDE 4.

(R)-Baclofen(STX209) is a selective GABAB receptor agonist.

(S)-Timolol maleate, is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively).

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Lipoic acid is a selective, small molecule large-conductance Ca(2+)-activated K(+) channel (BKCa, KCa1.1, MaxiK) positive modulator with EC50 of 11 uM. Lipoic acid shows a favorable selectivity profile on Nav, Cav, SK, and IK channels. Lipoic acid causes distinct activation from a concentration of 0.3 and 10 µM Lipoic acid left-shifted the voltage activation curve by 60 mV. Lipoic acid reduces spontaneous phasic contractions in guinea pig urinary bladder strips at 1 uM, while having only a modest effect on contractions evoked by electrical field stimulation (EFS) and no effect on high K+-induced contractions.

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17-AAG(NSC 330507; CP 127374) is a potent HSP90 inhibitor with IC50 of 5 nM, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells.

22-Oxacalcitriol is a Vitamin D3 analog which is Non-calcemic as well as a VDR ligand. 22-Oxacalcitriol has been shown to decrease parathyroid hormone (PTH) mRNA expression in vitro. Additionally has been noted to exhibit similar effects to calcitriol in

5-Azacytidine is a potent growth inhibitor and a cytotoxic agent. 5-Azacytidine acts as a demethylating agent by inhibiting DNA methyltransferase (Dnmt), forming covalent adducts with cellular DNMT1 depleting enzyme activity. 5-Azacytidine also improves t

5-Fluorouracil is a potent antitumor agent that affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools.

A doxorubicin analog that demonstrates anti-cancer activity without cardiotoxicity, does not inhibit topoisomerase IIβ activity at 100 uM.