The R racemate of LOXO-195, a potent, selective, next-generation Trk tyrosine kinase inhibitor with IC50 of 0.6 nM and <2.5 nM for WT TrkA and WT TrKC, respectively..

The R form of Bay 65-1942. which is a potent, selective, ATP-competitive inhibitor of IKKβ kinase with Ki of 2 nM..

The R enantiomer of Refametinib, a potent, non–ATP-competitive, highly selective, allosteric inhibitor of MEK1/2 with IC50 of 19/47 nM respectively..

The R enantiomer of GLPG-0492, a non-steroidal selective androgen receptor modulator (SARM) for treatment for Duchenne muscular dystrophy (DMD).

The prodrug of TG 100572, a potent, dual receptor tyrosine kinase/Src kinase inhibitor with IC50 of 2-16 nM for VEGFR, FGFR and PDGFR, 0.1-5 nM for Src family.

The prodrug of PF-04928473 (SNX-2112), a potent, orally bioavailable HSP90 inhibitor.

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

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

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

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

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

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

The intermediate of ARS-853.ARS-853 is a selective, covalent inhibitor of KRAS-G12C that inhibits mutant KRAS driven signaling by binding to the GDP bound oncoprotein and preventing activation.

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 first small molecule ligand for the VEGF-A receptor neuropilin 1 (NRP1).

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

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).

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

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 cell-permeable, pivaloyloxymethylester of Stafib-1, which is a potent, selective small molecule inhibitor of transcription factor STAT5b with Ki of 44 nM, >50-fold selectivity over STAT5a.

The calcium salt of levomefolic acid that has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers. .

The antiglucocorticoid RU43044 exerted significant agonist activity and activated MMTV-Luc transcription in osteosarcoma cells but not human breast cancer cells.

The (1R,2R) diastereomer of 2-PCCA, a potent, selective agonist of the orphan GPR88 receptor with EC50 of 373 nM, 5-fold more potent than the (1S, 2S)-isomer..

Thapsigargin is an inhibitor of microsomal Ca2+-ATPase.

Thalidomide-O-amido-C3-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

TH 5427 (TH5427) is a potent, small molecule NUDT5 (NUDIX5) inhibitor with IC50 of 29 nM, 690-fold selectivity for NUDT5 over MTH1 (NUDT1) in vitro.

TGR-1202 R-enantiomer is is the less active enantiomer of TGR-1202 (Umbralisib), TGR-1202 is a potent, selective, orally available PI3Kδ inhibitor with IC50 of 22 nM..

TGF-β receptor inhibitor

Tezampanel (LY 293558, NGX 424) is a competitive antagonist of the AMPA and kainate receptors with selectivity for the GluR5 subtype of the kainate receptor.