Canagliflozin is a highly potent and selective SGLT2 inhibitor for CHO-hSGLT2, CHO-rSGLT2 and CHO-mSGLT2 with IC50 of 4.4 nM, 3.7 nM and 2 nM, respectively.

CAY10415 is a potent, antidiabetic drug of the TZD structural class.

CCX140 is a potent CCR2 antagonist.

Dapagliflozin, also known as BMS-512148, is a drug used to treat type 2 diabetes approved in 2012 by FDA. Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2) which are responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter mechanism causes blood glucose to be eliminated through the urine. In clinical trials, dapagliflozin lowered HbA1c by 0.6 versus placebo percentage points when added to metformin.

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.

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

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.

Epalrestat is an orally active aldose reductase inhibitor that acts on diabetic neuropathy.

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).

GKT137831 is a novel and specific dual Nox1/Nox4 inhibitor with Ki of 140±40 nM and 110±30 nM; a potent inhibitor of fibrosis and hepatocyte apoptosis.

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

GRA Ex-25 is an orally active human glucagon receptor antagonist in a transgenic murine pharmacodynamic model at 10 and 30 mpk.

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

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

Ipragliflozin (ASP1941) is a Novel Selective Sodium-Dependent Glucose Co-Transporter 2 Inhibitor, on Urinary Glucose Excretion in Healthy Subjects

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.

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.

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

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.

LX-4211 is a potent dual SGLT2/1 inhibitor; Antidiabetic agents.

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