Orteronel (Synonyms: TAK-700)

TAK-700 (Orteronel) is a potent and highly selective rat and human 17,20-lyase inhibitor with IC50 of 54 nM and 38 nM, respectively. TAK700 binds to a...

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TH 302

TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM. The 2-nitroimidazole moiety of hypoxia-act...

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Cilomilast (SB 207499)

Cilomilast (Ariflo, SB-207499) is a potent LPDE4 and HPDE4 inhibitor with IC50 of 100 nM and 120 nM, respectively. Cilomilast is a drug which wa...

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GSK 256066

GSK256066 is a selective PED4B inhibitor with IC50 of 3.2 pM. GSK-256066 has been demonstrated to have exceptional potency in vitro and in vivo and is...

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PF 2545920

PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM. The PDE10A enzyme is expressed primarily in the brain, mostly in the stria...

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Pimobendan

Pimobendan (Vetmedin) is a selective inhibitor of phosphodiesterase III (PDE III) with an IC50 value of 0.32 μM. Pimobendan is a positive inotrope....

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BMS 740808

BMS-740808 is a highly potent, selective inhibitor of blood coagulation factor Xa (fXa) with Ki with 0.03 nM. BMS740808 also shows the high affinity f...

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Rivaroxaban (Xarelto)

Rivaroxaban (Xarelto, BAY 59-7939) is an oral, direct inhibitor of Factor Xa with a Ki of 0.4 nM and IC50 of 0.7 nM for purified human FXa.Inhibition ...

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Apixaban (BMS 562247-01)

Apixaban (BMS-562247-01) is a highly selective, reversible, and direct inhibitor of Human Factor Xa and Rabbit Factor Xa with Kiof 0.08 nM and 0.17 nM...

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Roflumilast

Roflumilast (Daxas, Daliresp) is a drug which acts as a selective, long-acting inhibitor of the enzyme PDE-4 with an IC50 of 0.8 nM. It has antiinflam...

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Anacetrapib (MK 0859)

Anacetrapib (MK-0859) is a potent and selective rhCETP and C13S CETP mutant inhibitor with IC50 of 7.9 nM and 11.8 nM, respectively. Anacetrapib (MK08...

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Dalcetrapib (JTT 705)

Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM. Dalcetrapib induces a conformational change in CETP, when added to human plasma. C...

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MK 8245

MK-8245 is an inhibitor of stearoyl-CoA desaturase (SCD) which targets the liver with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 an...

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LX 1606

LX1606 is and orally bioavailable, tryptophan hydroxylase (THP) inhibitor prodrugs. Upon administration, LX-1606 is converted to its active metabolite...

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CPI 613

CPI-613 is a lipoic acid analog that targets the mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase. In vitro,...

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URB 597 (KDS-4103)

URB597 is a relatively selective fatty acid amide hydrolase (FAAH) inhibitor with IC50 of 4.6 and 0.5 nM in brain membranes and intact neurons, respec...

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