L-165041 is a potent PPARδ agonist (Ki = 6 nM).

SB-612111 is a potent, selective nociceptin/orphanin FQ receptor (NOP receptor) antagonist with Ki of 0.33 nM.

A potent blocker of high-conductance Ca2+-activated K+ (BKCa, KCa1.1) channels that binds to the α-subunit of BKCa with Ki of 1.9 nM.

A potent, orally active microsomal triglyceride transfer protein (MTP) inhibitor that inhibits both human and rodent MTP with IC50 of 2 nM.

LMI070 (NVS-SM1) is a highly potent, selective and orally active small molecule SMN2 splicing modulator.

LMPTP inhibitor 1 is a potent molecule for diabetes which can increase liver IR phosphorylation in vivo and reverses high-fat diet-induced diabetes by inhibiting the IR phosphatase LMPTP.

LOC-14 is a small molecule reversible Protein disulfide isomerase (PDI) inhibitor with Kd of 62 nM.

Loflucarban is an antiinfective drug

LOXO-195 is a next-generation TRK kinase (TKI) inhibitor, with IC50s of 0.6±0.1 nM, <2.5 nM for TRKA and TRKC respectively.

LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).

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.