VU6005649 is a dual mGlu7/8 positive allosteric modulator with EC50s of 649 nM and 2.6 μM for mGlu7 and mGlu8, respectively.

VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.

VUF11207 is a highly potent CXCR7 agonist. VUF11207 induces recruitment of β-arrestin2 to the CXCR7 followed by internalization of the receptor.

VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK (Extracellular Signal-Regulated Kinase); antitumor agent.

VX-680 (MK-0457, Tozasertib) is a pan-Aurora inhibitor of Aurora A, Aurora B and Aurora C with Kiapp of 0.6 nM, 18 nM and 4.6 nM, respectively.

VX-809 is a CFTR modulator with EC50 of 0.1 μM.

WAY-362450 (XL335; Turofexorate isopropyl) is a highly potent, selective, and orally active farnesoid X receptor (FXR) agonist with an EC50 of 4 nM.WAY-362450 is useful for dyslipidemia.

WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.

WM-1119(WM1119) is a highly potent, selective inhibitors of KAT6A and KAT6B.

WNK-IN-11 is a potent, selectiive and orally active inhibitor of WNK1 kinase.

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

WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

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.

XMD16-5 is a novel TNK2 inhibitor.

XMD8-87 is a novel TNK2 inhibitor.

YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.

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

YL-0919 is a novel synthetic compound with combined high affinity and selectivity for serotonin transporter and 5-HT1A receptors.

YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.

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

YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.

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.

YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity.

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.