LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.

JMV 2959 (AEZS-123) is a potent ghrelin receptor (GHS-R1A) antaognist with binding IC50 of 32 nM.

Netarsudil (AR-13324) is a potent, selective ROCK inhibitor with Ki of 4.2 nM for ROCK2.

Birinapant (TL32711) is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM, less potent to XIAP.

Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with mean EC50 of 0.43 nM against a panel of 75 RSV A and B clinical isolates.

EPZ-005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

DBCO intermidate 3 is a Click Chemistry intermidate used for antibody-drug conjugates..

CMS121 is a substituted quinoline that has neuroprotective, anti-inflammatory, antioxidative, and renoprotective activities.

Histrelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 0.2 nM in CHO cells expressing the human receptor).

4-Butylresorcinol is a potent inhibitor of tyrosinase and is used in cosmetics as a depigmenting agent.

Antiviral activity against Varicella Zoster

Novel BRD4 inhibitor, suppressing osteoclastogenesis and ovariectomized osteoporosis by blocking RANKL-mediated MAPK and NF-κB pathways

Natural highly potent inhibitor of the serotonin transporter (SERT)

Novel TNKS/2 inhibitor, competing with nicotinamide binding to tankyrases

Natural inhibitor of ERK signaling pathways, inhibiting epithelial-mesenchymal transition via STAT3, showing the growth inhibition of HepG2, HeLa and MGC-803 cancer cell lines

Natural inhibitor of hepatocyte ferroptosis, protecting against drug-induced liver injury

Novel non-nucleoside reverse transcriptase inhibitor (NNRTI)

Inhibitor of VMAT-2, decreasing monamines into synaptic vesicles

Novel potent inhibitor of the CREBBP/EP300 bromodomain, showing >100-fold selectivity over a representative member of the BET bromodomains, BRD4(1)

Natural modulator of miRNA biogenesis, inhibiting the proliferation, migration, and invasion of hepatocellular carcinoma (HCC) cells

Subtype-selective activator of K(Ca)2.1

MM 07 is a biased apelin receptor agonist, with a KD of 300 nM in CHO-K1 cells and a KD of 172 nM in human heart.

Novel inhibitor of cholesterol transport proteins

Antitumor agent to be associated with negative regulation of Met endosomal signaling in renal cancer cells

Inhibitor of Eukaryotic Translation; Antitumor Natural Product

Moderate alpha-l-fucosidase inhibitor

Natural microbial metabolite of isoflavone genistein, increasing the lifespan and improving the thermal and oxidative stress tolerance of C. elegans

Less active enantiomer of Elexacaftor

Metabolite of VX-740

Vesicular monoamine transporter-2 (VMAT2) inhibitor, with 15-​fold greater affinity than GZ-​793A