U-0126 is a selective MAP Kinase Kinase inhibitor, displaying a preference for MEK-1 (IC50 = 72 nM) and MEK-2 (IC50 58nM).

Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.

UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM.

Uprosertib is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.

UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.

V-9302 is a competitive antagonist of transmembrane glutamine flux, selectively and potently targeting the amino acid transporter ASCT2.

Valbenazine(NBI-98854) is a potent and selective VMAT2 inhibitor..

Velaresol, also known as BW12C or BW12C79, is a oxyhaemoglobin stabilizer.

Verdiperstat is a selective, irreversible and orally active myeloperoxidase inhibitor, with an IC50 of 630 nM, and is used in the research of neurodegenerative brain disorders.

Verucerfont(GSK561679) is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively.

Vilanterol trifenatate (GW642444)is a novel, inhaled, long-acting β(2) agonist with inherent 24-h activity under development as a once-daily combination therapy with an inhaled corticosteroid for COPD and asthma.

Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.

VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.

VU0155041 is a Potent, positive allosteric modulator/allosteric agonist at mGlu4 receptors (EC50 = 798 and 693 nM at human and rat mGlu4 receptors respectively).

VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors.

Wogonin is a cell-permeable and orally available flavonoid that displays anti-inflammatory and anticancer properties.

WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively, without significant inhibition on 139 other kinases.

Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects.

XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.

YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1.

YK11 is the newest ingredient in the SARMs family in recent years

YO-01027 (Dibenzazepine, DBZ) is a dipeptidic g-secretase inhibitor with IC50 of 2.6 and 2.9 nM for APPL and Notch, respectively.

YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.

YW1159 is an inhibitor of Wnt signaling with an IC50 value of 1.2 nM in a reporter assay.

YY-20394 is a novel PI3K inhibitor suppresses tumor progression by immune modulation.

ZB716 is a steroidal, orally bioavailable SERD (selective estrogen receptor downregulator) that binds to ER with high affinity and exerts its antiestrogenic effect on ER-expressing breast cancer cells.

ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.

Z-FA-FMK is an irreversible cysteine protease inhibitor, and also inhibits effector caspases.

Ziyuglycoside I has anti-wrinkle activity, could be used as an active ingredient for cosmetics.

Ziyuglycoside II has a wide range of clinical applications including hemostasis, antibiosis, anti-inflammation and anti-oxidation.