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MAO Inhibitor
Bifemelane hydrochloride is an antidepressant MAO inhibitor. Reverses catalepsy induced by tetrabenazine in mice and increases locomotor activity in MPTP-treated marmosets. -
LSD1/BHC110 & MAO inhibitor
Tranylcypromine hydrochloride is a non-selective MAO-A/B inhibitor. -
Fluorescent P450 substrate
3-Cyano-7-ethoxycoumarin is a fluorogenic substrate suitable for the continuous determination of cytochrome P450 mixed-function monooxygenases. It is a fluorescent probe useful in microsomal dealkylase studies. -
cytochrome P450 substrate
Methoxyresorufin is a fluorometric substrate for cytochrome P450 linked enzymes. -
HMG-CoA reductase inhibitor
Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. -
CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. -
HMG-CoA Reductase inhibitor
Clinofibrate is a lipid clearing agent that appears to modify lipid metabolism, diminishing the steroid induced accumulation of lipids within osteocytes. It also can effectively reduce the plasma fibrinogen level.
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PDE10A inhibitor
PF-2545920 is a phosphodiesterase inhibitor selective for the PDE10A subtype.
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CETP inhibitor
JTT-705 (Dalcetrapib) is a CETP inhibitor.Inhibition of CETP is a target to increase HDL-cholesterol and potentially reduce atherosclerosis. -
CETP inhibitor
Torcetrapib (CP-529414) is a CETP inhibitor with IC50 of 37 nM. -
Cathepsin K Inhibitor
Odanacatib is an inhibitor of cathepsin K,an enzyme involved in bone resorption. -
Hsp90 inhibitor
IPI-504 is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90). -
CYP3A Inhibitor
Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits intestinal transport proteins, increasing the overall absorption of several HIV medications, including atazanavir, darunavir and tenofovir alafenamide fumarate. - Adarotene belongs to the so-called class of atypical retinoids. The presence of the phenolic hydroxyl group on Adarotene structure allows a rapid O-glucuronidation as a major mechanism of elimination of the drug, favoring a fast excretion of its glucuronide metabolite in the urines.
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ACE inhibitor/Beta blocker
Moxonidine is a new-generation centrally-acting antihypertensive drug. It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction. -
PDE-2 Inhibitor
BAY 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human). - Calcifediol is a major circulating metabolite of vitamin D3 and acts as a competitive inhibitor with an apparent Ki of 3.9 μM. It also suppresses PTH secretion and mRNA (ED50=2 nM)
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Collagen proline hydroxylase inhibitor
Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor. -
SGK1 inhibitor
EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. -
SGK1 inhibitor
EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. -
Androgen Receptor antagonist
Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity. - Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is an active metabolite of vitamin D2.
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Cathepsin Inhibitor
Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively. - Luliconazole is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.
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Vitamin D Analog
Lexacalcitol (KH1060) is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 [1alpha,25-(OH)2D3], as judged by in vitro antiproliferative and cell differentiating assays. -
DHFR inhibitor
Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells. -
DGAT1 Inhibitor
PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM. - Paricalcitol is a drug used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure.
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PPAR-γ antagonist
T0070907 was identified as a potent and selective PPARgamma antagonist. With an apparent binding affinity (concentration at 50% inhibition of [(3)H]rosiglitazone binding or IC(50)) of 1 nm, T0070907 covalently modifies PPARgamma on cysteine 313 in helix 3 of human PPARgamma2. -
RARα agonist
Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro. -
PDE1 inhibitor
Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor. -
anticancer and radioprotection agent
Geniposidic acid is an effective anticancer and radioprotection agent. -
antitumor agent
Lonidamine (AF-1890), an antitumor agent, is a hexokinase, mitochondrial pyruvate carrier (Ki 2.5 μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporters inhibitor, which also inhibits mitochondrial complex II. - Levothyroxine, also L-thyroxine or T4, is a synthetic form of the thyroid hormone thyroxine, which is normally secreted by the follicular cells of the thyroid gland.
- Miglitol inhibits glycoside hydrolase enzymes called alpha-glucosidases. It is primarily used in diabetes mellitus type 2 for establishing greater glycemic control by preventing the digestion of carbohydrates (such as disaccharides, oligosaccharides, and polysaccharides) into monosaccharides which can be absorbed by the body.

