APX-115 (Ewha 18278) is a first-in-class, orally active, pan-NADPH oxidase (Nox) inhibitor with Ki of 1.08, 0.57, 0.63 nM for Nox1, Nox2, and Nox4, respectively.

LGD-6972 is a selective and orally active glucagon receptor antagonist. LGD-6972 has the potential for type 2 diabetes research.

BGP-15 is a PARP inhibitor and insulin sensitizer.

BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.

ZLN005 is a novel transcriptional regulator of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α).

AZD9977 is a first-in-class, potent, selective, mineralocorticoid receptor (MR) modulator with IC50 of 0.37. 0.08 and 0.08 uM for human, mouse and rat MR, respectively.

ETC-1002(ESP-55016) is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).

glucagon receptor antagonists-4 is a highly potent glucagon receptor antagonist.

Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.

LX2761 is a locally acting SGLT1 inhibitor that is highly potent in vitro and delays intestinal glucose absorption in vivo to improve glycemic control.

Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.

Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.

ZLN024 Hcl is a novel AMPK allosteric activator; activated α1β1γ1 and α2β1γ1 by around 2–2.5 fold with an EC50 of about 1–2 uM. IC50 value: 1-2 uM (EC50) [1] Target: AMPK activator ZLN024 activated AMPK in L6 myotubes and stimulated glucose uptake and

Troglitazone(CS-045), PPARγ agonist, is an anti-diabetic thiazolidinedione (TZD) with anti-inflammatory and anti-tumor activity.

Tofogliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2).

Rosiglitazone(BRL-49653) is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ(PPARγ).

Ro 28-1675 (Ro 0281675) is a potent allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM.

LY2922470 (LY-2922470) is a potent, selective, orally available GPR40 agonist with EC50 of 7 nM.

JTT-551 sodium (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.

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.

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.

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.