LDE225 (NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively. Phase 3.

LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM.

LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM.

LY2940680 binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling.

LY3039478 a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested.

LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM.

LY900009 (LY-900009) is an orally active small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein.

MK-4101 is a potent SMO Inhibitor of the Hedgehog Pathway, highly active against Medulloblastoma and Basal Cell Carcinoma.

MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma.

MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range.

NCB-0846 is a novel,first-in-class,orally TNIK inhibitor with an IC50 value of 21 nM,that have shown strong anti-tumor efficacy against several cancer models.

NSC 668036 is an inhibitor of the Dishevelled (Dvl) protein PDZ domain (Kd = 240 μM for mouse Dvl1 PDZ domain).

PAT-048 (PAT048) is a potent, selective, noncompetitive autotaxin inhibitor with IC50 of 1.1 nM against the lysoPLD activity of human ATX.

PAT-505 (PAT 505, PAT505) is a potent, selective, noncompetitive, and orally active autotaxin inhibitor with IC50 of 2.0 nM against the lysoPLD activity of human ATX.

PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor

PF-5006739 is a potent inhibitor of casein kinases 1 delta (CK1δ) and 1 epsilon (CK1ε)

PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.

PF-794 (PF794) is a potent, specific and ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with IC50 of 39 nM in cell-free assays.

PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.

PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification

Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM and also is an inducer of osteoblast differentiation with EC50 of 1 μM.

QS 11 is a GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor.