A potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.

Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity. At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Pasireotide acetate) usually boasts enhanced water solubility and stability.

NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.

A proton pump inhibitor that reduces stomach acid secretion by inhibition of the H+/K+-ATPase in the parietal cells.

IPAG is a prototypic selective inhibitor of sigma1 receptor that engages the unfolded protein response and induces autophagy in cancer cells.

A PSMA (prostate-​specific membrane antigen) ligand-​tubulysin compound..

A pyrimidine analog reverse transcriptase inhibitor (NRTI) for the treatment of HIV/AIDS.

A retinoic acid analog and selective RARα agonist

K-7174 dihydrochloride is a selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2).

Capadenoson is a selective agonist of adenosine-A1 receptor.

MG624 is a potent and selective neuronal α7 nAChR antagonist with a Ki of 106 nM.

A selective GPR68 positive allosteric modulator (pEC50=6.83) with minimal PAM activity at the related proton-sensing GPCRs GPR4 and GPR65.

SR-11237 is a selective pan retinoid X receptor (RXR) agonist with no retinoid A receptor (RAR) activity. .

A selective protein phosphatase PHLPP inhibitor with IC50 of 4 uM for PP2C domain of PHLPP2.

A selective TRPM8 channel blocker with pEC50 of 6.91 in Ca(2+) influx assay, with no activity for TRPV4 (pEC50<4.6).

A selective Δ6 desaturase inhibitor that displays selectivity over Δ5 and Δ9 desaturases

A selective, competitive inhibitor of HMG-CoA reductase, that is also antilipemic.

A serine protease inhibitor that inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM).

A small molecule binds to the EXO70 (exocyst component of 70 kDa) subunit of the exocyst complex (Kd=253 uM), resulting in inhibition of exocytosis and endosomal recycling in both plant and human cells and enhancement of plant vacuolar trafficking..

A small molecule compound of prostaglandin D2（PGD2) inhibitor.

A small molecule corrector of ΔF508-CFTR with IC50 of 6.0 uM..

A small molecule inhibitor (IC50=0.3 uM) of DEAD-box polypeptide 3 (DDX3), a human host factor required for the replication of several DNA and RNA viruses.