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)..

A derivative of the neurotransmitter GABA that acts as a GABAB receptor agonist.

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.

LUT014 is a novel BRAF agonist.

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.

Z62954982 is a potent, specific Rac1 inhibitor, reduces the intracellular levels of Rac1-GTP in a concentration-dependent manner with IC50 of 12 uM, 4 times more effective than NSC23766 (IC50=50 uM).

YM-1 is a close derivative of MTK-077 that allosterically promotes Hsp70 binding to unfolded substrates, specificly binds to Hsp70 with Kd of 4.9 uM.

Rottlerin (Mallotoxin.

AAL993 (ZK260253) is a potent, orally active VEGFR inhibitor with IC50 of 130, 23 and 18 nM for VEGFR-1, 2 and 3, respectively.

A peptide mimetic of the C-terminal Cys-Val-Ile-Met of K-Ras4B that potently inhibits FTase (Farnesyltransferase) with IC50 of 0.5 nM.

A hyperpolarization-activated cyclic nucleotide-gated (HCN) channel.

C75 is an inhibitor synthetic fatty-acid synthase (FASN) and inhibits prostate cancer cells PC3 (IC50: 35 μM).

Biperiden Hcl (NSC 170950, NSC 84989) is a centrally-acting antiparkinsonian agent that functions as a selective central M1 cholinoreceptors blocker..

Dilazep dihydrochloride is an inhibitor of adenosine uptake. Dilazep dihydrochloride has cerebral and coronary vasodilating action through enhancement of effect of adenosine. Dilazep dihydrochloride also inhibits the ischemic damage, platelet aggregation, and membrane transport of nucleosides.