XL888 is an orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.

XL388 is a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR).

XL228 is a protein kinase inhibitor targeting IGF1R, the Aurora kinases, FGFR1-3, ABL and SRC family kinases.

XL184 (Cabozantinib) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.

XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for wild type and mutant p110α with IC50 of 40 nM and 40 nM, respectively.

XL019 is an orally bioavailable inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity.

Ximelagatran is an orally active direct thrombin inhibitor.

XCT-790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα); induces cell death in chemotherapeutic resistant cancer cells.

XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM, regulates axin levels and does not affect CRE, NF-κB or TGF-β.

Xanthine amine congener (XAC) is a non-selective adenosine receptor antagonist with Kb values of 83, 25, and 15 nM for rat PC12 cells, human platelets that endogenously express adenosine A2A receptors, and rat fat cells that endogenously express A1 recept

WZB117 is an irreversible inhibitor of glucose transporter 1 (Glut1) that blocks glucose transport in diverse cancer cells (IC50 = ~0.6 µM), reducing extracellular lactate and intracellular ATP levels.

WZ811 is a novel small molecular and potency CXCR4 antagonist with EC50 of 0.3 nM.

WZ8040 is a potent, mutant-selective, irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I) and is 100-fold less potent against wild-type EGFR.

WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM; does not inhibit ERBB2 phosphorylation (T798I).

WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).

WY 14643 (Pirinixic Acid) is a potent peroxisome proliferator and activator of PPARα with ED50 of 1.5 μM.

WS3 is a novel small molecule that promotes β cell proliferation with EC50 of 28 nM(induced R7T1 proliferation).

WP1130(Degrasyn) is a novel selective small molecular deubiquitinase (USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and a Bcr/Abl destruction pathway activator with an IC50 of 1.8 μM for K562 cells.

WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT.

Wnt-C59(C59) is a very potent and highly selective Wnt signaling antagonist with an IC50 ~ 74 pM in the Wnt signaling reporter assay.

Wnt Inhibitor IWP-4 is a potent inhibitor of Wnt/β-catenin signaling (IC50 = 25 nM).

WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4).

WM-8014(WM8014) is a highly potent, selective inhibitors of KAT6A and KAT6B.

WIN 55212-2 (mesylate) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.

WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.

WHI-P258 is a negative control for JAK3 inhibitors.

WHI-P180(Janex 3) is a potent inhibitor of IgE-mediated mast cell responses to allergens in vitro and in vivo. Also inhibits cyclin-dependent kinase 2 (CDK2; IC50 = 1µM) by blocking the ATP site

WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.

WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.

WEHI-345 is a potent and selective inhibitor of RIPK2, with IC50 of 0.13 μM.