Novel Bcl-XL antagonist

Nicotinic acetylcholine receptor agonist

Selective nonimidazole H3 receptor inverse agonist

Novel and selective H3 receptor antagonist

Multidrug Resistance (MDR) Modulator

Novel adenosine A2A receptor (A2AR) antagonist

Novel potent and orally active adenosine kinase inhibitor

Novel potassium channel opener, more potent enantiomer

Negative control for A-192621

Selective adenosine kinase (AK) inhibitor

Novel blocker of the activation of the TRPV1 channel by capsaicin, inducing hypothermia involving tail-skin, vasodilation at thermoneutrality, decreasing body temperature

Temperature-Neutral Transient Receptor Potential Vanilloid-1 (TRPV1) Antagonist with Analgesic Efficacy

Fluorogenic A9 Peptide Probe, Interacting with Its Receptor Model HER2-DIVMP

Selective TRPV1 antagonist

Natural IDO1 inhibitor, cytotoxic and antiplasmodial agent

Novel natural anticancer agent, exhibiting potent cytotoxicity against PANC-1 human pancreatic cancer cell line under the normoglycemic condition

Novel, potent, mutant-selective BET bromodomain inhibitor, showing >100-fold selectivity for the L/V mutant over wild-type and excellent DMPK properties

Inhibitor of cyclin-dependent kinases

Novel ATP-competitive GSK-3ß inhibitor, exhibiting potent antiproliferative activity

Endogenous peripheral TRPV1 ligand

Dual human A2a antagonist/MAO-B inhibitor

Potent and selective activator of protein kinase A (PKA) type I and II

Potent activator of cGMP-dependent protein kinase Ia, Ib and type II as well as of cGMP- gated ion channels

Unique cytoprotective mediator, inhibiting oxidative stress; Novel probe of the protein S-guanylation

Antitumor agent, displaying cytotoxicity against the human cancer cell lines, including MDA231, T-47D, Hs578t, SaoS2, K562, SKHep1,and Hep3B

Novel inhibitor of nitric oxide formation in macrophages independent of effects on TNF

Specific non-nucleoside RT inhibitor (NNRTI) of HIV-1 RT

Inhibitor of RNA synthesis

Building Block

Potent and selective inhibitor of NTPDase1