The compound (Akt-I-1,2) inhibited both Akt1 and Akt2 with IC50 values of 2.7 and 21 μM respectively.

The dimethyl ester of N-oxalyl-d-phenylalanine (NOFD), a specific HIF asparaginyl hydroxylase (FIH) inhibitor with Ki of 83 uM, but not HIF prolyl hydroxylase (>1 mM).

The distomer of BRS-3 agonist Compound A, shows no activity for bombesin receptor subtype-3 (BRS-3) with EC50>10 uM..

The first in a class, potent and highly selective, direct renin inhibitor with IC50 of 0.6 nM.

The first potent and selective proton-sensing GPCR GPR4 antagonist with IC50 of 67 nM, with no activity against TDAG8 and OGR1 (IC50>10 uM).

SCB-4380 (SCB 4380, SCB4380) is the first potent, selective inhibitor for PTPRZ (protein tyrosine phosphatase receptor-type Z) with IC50 of 0.4 uM against human Z-ICR-catalyzed hydrolysis. SCB-4380 also strongly inhibits PTPRG (IC50=0.4 uM), and shows little inhibition on PTPRA, PTPRM, PTPRS, PTPRB, PTPN1 and PTPN6. SCB-4380 inhibites PTPRZ activity in C6 glioblastoma cells, and suppresse cell migration and proliferation in vitro and tumor growth in a rat allograft model.

BAY 73-6691 is a drug developed by Bayer for the treatment of Alzheimer's disease. It was the first compound developed that acts as a phosphodiesterase inhibitor selective for the PDE9A subtype.

The first potent, selective, CNS penetrating inward rectifier potassium channel Kir7.1 (KCNJ13) inhibitor with IC50 of 0.31 uM.

The first selective, cell-permeable inhibitor of GAG sulfotransferases with IC50 of 2.0-2.5 uM .

The first small-molecule inhibitor of renal outer medullary potassium channel (ROMK, Kir1.1) and Kir7.1 with IC50 of 294 nM for ROMK.

The less active enantiomer of GNE-140, inhibits LDHA activity (18-fold less potent that (R)-GNE-140).

The L-lysylamide prodrug of 5F-203 (NSC703786), a potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway.

The major circulating metabolite of vitamin D3.

The more active enantiomer of (±)-U-50488, a potent, selective kappa-opioid receptor agonist with no μ-opioid antagonist effects.

The one form of glutamic acid found in nature, is the most potent natural inhibitor of glutathione synthesis.

The orally active prodrug of candoxatrilat (UK-73967), potent neutral endopeptidase EC 3.4.24.11 (atriopeptidase) inhibitor..

The orally bioavailable prodrug of Galiellalactone, a direct inhibitor of STAT3, prevents the transcription of STAT3 regulated genes.

Human growth hormone-releasing factor stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary.

The pivaloyloxymethyl ester prodrug of Stafib-2, which is a potent, selective STAT5b inhibitor with Ki of 9 nM.

The prodrug of AUDA, a potent inhibitor of sEH (soluble epoxide hydrolase) with IC50 of 50 nM and 100 nM for mouse sEH and human sEH, respectively.

The prodrug of cidofovir diphosphate that inhibits cytomegalovirus (CMV) viral replication by selectively inhibiting viral DNA polymerases.

The prodrug of modafinil that is a mild central nervous system stimulant drug used to relieve excessive sleepiness and inattention..