The first small molecule inhibitor of ThiD; IkB kinase (IKK) inhibitor; antibiotic

PKCβ-selective inhibitor

Novel inhibitor of Src protein tyrosine kinase SH2

Novel DNA gyrase B inhibitor

Potent non-steroidal antiandrogen

Novel non-steroidal antiandrogen, downregulating c-myc messenger RNAs

Potent vertebrate GABAa antagonist

Potent serotonin SR-1A/SR-1B and moderate SR-2C agonist

Novel allosteric inhibitor of soluble adenylyl cyclase (sAC)

Novel Potent Dual Orexin Receptor Agonist

Novel Potent and Selective Orexin-1 Receptor Antagonist

Novel potent and selective KOR antagonist

Selective inhibitor of the dopamine transporter (DAT), blocking cocaine-induced locomotor stimulation and acting as a positive allosteric modulator of the human CB1 (hCB1) receptor

Novel allosteric RORγt inverse agonist

Potent indirect activator of AMPK

Specific ligand to CB2-positive spleen tissue of rats and mice

Selective and reversible Monoamine_oxidase_A>monoamine oxidase A (MAO-A) inhibitor

Potent and selective competitive antagonist of 5-HT4 receptors

Selective collagenase inhibitor, inducing the conformational change in the side-chains of the S1 pocket of MMP-1

Novel inhibitor of β-amyloid-induced cytotoxicity

Novel stimulator of host immune defenses, Inducing the transcription of putative immune effectors in C. elegans

Novel stimulator of autophagy, inhibiting Mycobacterium tuberculosis survival in macrophages, and targeting Pik1

Novel non-peptidic RANTES antagonist

Potent agonist of S1P1 receptors

Specific and competitive H2 receptor antagonist

Prodrug of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148

Novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor

Photosensitiser for the treatment of age-related macular degeneration

Novel P2X3 antagonist

Novel potent and selective CB2 probe (Ki for CB2: 0.8 nM and >12000 selectivity over CB1)