JTT-551 (JTT551, JTT 551) is a novel potent, selective inhibitor of protein tyrosine phosphatase 1B (PTP1B) with Ki of 0.22 uM, displays >45-fold and >136-fold selectivity over TCPTP, CD45 and LAR.

Inhibitor of ATP-sensitive K+ channel activity in MIN 6 cells. Has also been shown to bind sulfonylurea receptors as well.

GSK2330672 is a highly potent, nonabsorbable ASBT(apical sodium-dependent bile acid transporter) inhibitor (hASBT IC50=42 ± 3 nM) .

DS-8500a (DS8500a) is a novel potent, selective, orally available GPR119 agonist with EC50 of 51.5 nM in human GPR119-expressing CHO-K1 cells, displays no significant effect on 66 receptors, channels, or transporters.

DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.

DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9. IC50 value: 15 Nm.

CCX140 is a potent CCR2 antagonist.

A novel potent, selective, orally active human 11β-HSD1 inhibitor with IC50 of 3.0 nM.

BI 135585 (BI-135585, BI135585) is a potent, selective, orally active 11β-HSD1 inhibitor with IC50 of 4.3 nM and 53 nM in human adipocytes and primary human adipose tissue, respectively.

Beloranib is being studied as a first-in-class obesity therapy that demonstrates a unique mechanism of action through methionine aminopeptidase 2 (MetAP2 ) inhibition.

Alendronate (Fosamax)

A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.

A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.

A novel potent, selective, orally available DPP-4 inhibitor with IC50 of 9 nM.

A imidazoline compound that stimulate insulin release by inhibition of ATP-dependent K+ channels and inducing of Ca2+ mobilization in mouse pancreatic beta-cells.

A highly potent, selective, orally active renin inhibitor with IC50 of 2.1 nM in hPRA assay.