Metabolism

BMS-740808 is a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.

LY315920 (Varespladib) is an inhibitor of the IIa, V, and X isoforms of secretory phospholipase A2 (sPLA2).

Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.

NSC 131463 is a dihydrofolate reductase potent inhibitor with an IC50 of 1 nM.

NVP-BEP800 is a novel, fully synthetic, orally bioavailable inhibitor that binds to the NH2-terminal ATP-binding pocket of Hsp90.

Oligomycin A is a mitochondrial ATPase inhibitor. Oligomycin A inhibits ATP5 (mitochondrial ATPases, F1F0) bound to the cell membrane.

Pimobendan (Vetmedin) is a calcium sensitizer with positive inotropic and vasodilator effects. It is also a selective inhibitor of phosphodiesterase III (PDE3).

(S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells.

GSK256066 is an exceptionally high affinity and selective inhibitor of PDE4 that inhibits PDE4 isoforms A-D with equal affinity and has a high HARBS (High-Affinity Rolipram Binding Site) ratio (>17).

PF-04929113 (SNX-5422) is orally bioavailable heat shock protein 90 (Hsp90) inhibitor.

MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.

Cetaben is a unique, PPARα-independent peroxisome proliferator with hypolipidemic activity that inhibits cholesterol synthesis in the human hepatoma Hep-G2 cells resulting in reversible changes in Golgi morphology.

TH-302 is a selectively targeting hypoxic regions of solid tumors hypoxia-activated prodrug.

SNX-2112 is a heat shock protein 90 (Hsp90) inhibitor with anticancer properties currently in clinical trials. SNX-2112 induced autophagy in a time- and dose-dependent manner via Akt/mTOR/p70S6K inhibition. SNX-2112 induces significant apoptosis and autophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent

PF-2545920 is a phosphodiesterase inhibitor selective for the PDE10A subtype.

KW-2478 is an agent that targets the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.

JTT-705 (Dalcetrapib) is a CETP inhibitor.Inhibition of CETP is a target to increase HDL-cholesterol and potentially reduce atherosclerosis.

XL888 is an orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.

IPI-504 is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90).

IPI-493 is a potent and orally bioavailable HSP90 inhibitor with Ki of 21 nM.

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)

Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3.

Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is an active metabolite of vitamin D2.

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.

Paricalcitol is a drug used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure.

SPK-601 (LMV-601) is an inhibitor of the phosphatidylcholine-specific phospholipase C (PC-PLC). SPK-601 also can be used as an antimicrobial agent.

SMND-309 is a metabolite of salvianolic acid B, and exhibits neuroprotective effects in cultured neurons and in permanent middle cerebral artery occlusion rats.

SL-251188, an oxazolidinone derivative, was characterized in baboons as a radioligand for the in vivo visualization of MAO-B using positron emission tomography (PET).

LX 1606 is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.

Aminopterin is an antineoplastic drug. It works as an enzyme inhibitor by competing for the folate binding site of the enzyme dihydrofolate reductase.

IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).

Ginkgetin, a Biflavone from Ginko biloba leaves, inhibits cyclooxygenases-2 and 5-lipoxygenase in mouse bone marrow-derived mast cells.

Punicalin is a highly active carbonic anhydrase inhibitor.

Lp-PLA2 -IN-1 inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.

PF-04991532 is a potent, hepatoselective glucokinase activator with EC50s of 80 and 100 nM in human and rat, respectively.

ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.