γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain.

A small-molecule probe that selectively kills cells induced to express mutant RAS.

Roseoflavin is a chemical analog of FMN and riboflavin that has antimicrobial activity.

A potent and specific antagonist of platelet activating factor (PAF) receptor that inhibits PAF-induced human platelet and neutrophil aggregation in vitro with IC50 of 0.17 and 0.36 uM, respectively.

AZD-0364 is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.

NNMTi is a nicotinamide N-methyltransferase (NNMT) inhibitor that promotes myoblast differentiation.

ZL-006 (ZL 006, ZL006) is a brain penetrant small molecule inhibitor of PSD-95/nNOS interaction that prevents glutamate-induced excitotoxicity and cerebral ischemic damage in vivo.

A potent, selective, noncompetitive inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) with IC50 of 7 uM.

A potent, full dopamine D1 agonist.

An adenosine A1 receptor agonist (EC50= 8.2 nM)..

Zaprinast (M&B 22948) is a potent, cGMP-specific phosphodiesterase inhibitor with IC50 of 0.5-0.76 and 0.15 uM for PDE5 and PDE6 respectively, also is an agonist for GPR35 (EC50=16/840 nM for rat/human GPR35).

Olinone is a selective inhibitor for the BET BRD1 with Kd of 3.4/3.7/8.6 uM for BRD4-BrD1/BRD3-BrD1/BRD2-BrD1, respectively, shows high selectivity over BET BRD2 (Kd>300 uM).

CP-91149 is a GP (glycogen phosphorylase) inhibitor. CP-91149 promotes glycogen resynthesis, but not its overaccumulation. CP-91149 has the potential for Type II (insulin-dependent) diabetes study.

A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1.

A specific inhibitor of mitochondrial Na(+)-Ca(2+) exchanger (mNCE) with IC50 of 1.5 uM in INS-1 cells.

PF-04856264 is a potent, selective Nav1.7 blocker with IC50 of 28 nM, dispalys >1,000-fold selectivity over Nav1.5.

A potent, selective N-methyl-D-aspartate (NMDA) antagonist with selectivity for the NR2B subunit.

ALX-5407 is a potent, selective, orally active inhibitor of GlyT1 glycine transporter with IC50 of 3 nM.

A potent, selective sodium-coupled citrate transporter (NaCT or SLC13A5) with IC50 of 0.51 uM, >20-fold selectivity over NaDC1 and NaDC3.

SCH-28080 is a potent, orally active, reversible inhibitor of gastric H+,K+-ATPase with IC50 of 20 nM.

Lubiprostone(SPI-0211;RU0211) is a gastrointestinal agent used for the treatment of idiopathic chronic constipation.

Luliconazole(NND 502) is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.

Lurasidone is an atypical antipsychotic, inhibits Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C with IC50 of 1.68 nM, 2.03 nM, 0.495 nM, 6.75 nM and 10.8 nM, respectively.

Lusutrombopag（S-888711） is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist being developed by Shionogi for chronic liver disease (CLD) patients with thrombocytopenia prior to elective invasive surgery.

LUT014 is a novel BRAF agonist.

LXR-623 is a novel Liver X Receptor modulator

LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. It can be used for the treatment of uveal melanoma.

LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50s of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β respectively.

SR1555 is a selective RORγ inverse agonist (IC50=1.5 uM) that suppresses T(H)17 cells and stimulates T regulatory cells.

KT-5823 is a potent, highly specific PKG (cGMP-dependent protein kinase) inhibitor with Ki of 0.234 uM, displays little to no activity for MLCK, cAPK, and PKC.