Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention

Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention

Darapladib is a selective and orally active inhibitor of Lp-PLA2 (IC50= 270 pM)

Cangrelor is a P2Y12 inhibitor, and was approved in June 2015 as an antiplatelet drug for intravenous application. Cangrelor is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggrega

Bumetanide

BMS687453 is a potent and selective peroxisome proliferator activated receptor (PPAR) α agonist, with an EC50 of 10 nM for human PPARα and ∼410-fold selectivity vs human PPARγ in PPAR-GAL4 transactivation assays.

BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate.

Betrixaban (PRT-054021) is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a).

Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of  0.62 nM, which used in the treatment of adults with essential hypertension.

AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ.

Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.

Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3.

Aliskiren hemifumarate(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.

A selective, competitive inhibitor of HMG-CoA reductase, that is also antilipemic.

(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).

Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.

GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.

Nepicastat hydrochloride is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors.

Nicainoprolhe is an antiarrhythmic agent,a fast-sodiumchannel blocking drug (class Ib), also protected isolated rat hearts against reperfusion arrhythmias.

Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.

Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.

Ro 48-8071 fumarate is an inhibitor of OSC(Oxidosqualene cyclase; IC50=6.5 nM) that has low-density lipoprotein (LDL) cholesterol lowering activity.

Rostafuroxin: an ouabain-inhibitor counteracting specific forms of hypertension.

Terutroban is a thromboxane/prostaglandin endoperoxide receptor antagonist.

Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist.

Torcetrapib is a CETP inhibitor with IC50 of 37 nM, elevates HDL-C and reduces nonHDL-C in plasma. Phase 3.

WAY-362450 (XL335; Turofexorate isopropyl) is a highly potent, selective, and orally active farnesoid X receptor (FXR) agonist with an EC50 of 4 nM.WAY-362450 is useful for dyslipidemia.

LY-333,531 Hydrochloride is a potent, selective inhibitor of Protein Kinase C isozymes, PKC beta I (IC50 = 4.7 nM) and PKC beta II (IC50 = 5.9 nM). It is potentially beneficial for cancer research.

Obicetrapib is a CETP inhibitor, on the elevation of high-density lipoprotein cholesterol (HDL-C) and reduction of low-density lipoprotein cholesterol (LDL-C), alone and in combination with statin therapy.

A nonpeptide endothelin ETA receptor antagonist. Antihypertensive.