Taladegib (formerly LY2940680, LY 2940680, LY-2940680) is a potent and orally bioavailable Hedgehog pathway antagonist of the smoothened receptor being developed by Eli Lilly for the treatment of cancer.

GANT61 (GANT 61; nsc 136476; GANT-61; nsc-136476) is a novel and potent small-molecule inhibitor for GLI1 (glioma-associated oncogene 1) and GLI2-induced transcription with potential anticancer activity.

Smoothened Agonist (SAG), a benzothiophene analog, is a potent and cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

Vismodegib (formerly known as GDC-0449; RG-3616; GDC0449; RG3616; trade name: Erivedge) is a potent, orally bioavailable, first-in-class and specific hedgehog pathway inhibitor with potential anticancer activity.

Erismodegib (formerly LDE-225; NVP LDE-225; LDE225; NVP-LDE22; Sonidegib; trade name of Odomzo) is an orally bioavailable small-molecule antagonist of the Smoothened (Smo) in Hedgehog signaling pathway with potential antitumor activity.

Glasdegib (formerly known as PF-04449913; PF4449913; PF04449913; PF-4449913; Daurismo) is a novel, potent, and orally bioavailable small-molecule inhibitor of Smoothened (Smo) in the Hedgehog (Hh) signaling pathway with potential antitumor activity.

SANT-1 (SANT1; SANT 1) is a novel, potent and selective Sonic hedgehog (Shh) enzyme inhibitor/Smo antagonist with potential antineoplastic activity.

PF-5274857 (PF5274857; PF 5274857) is a novel, potent, orally bioavailable and selective Smoothened (Smo) antagonist with potential antineoplastic activity.

Cyclopamine (formerly HSDB3505; HSDB-3505; 11-deoxojervine), a naturally occuring steroid alkaloid found in Veratrum plant, is reported to be a potent and specific inhibitor of Hedgehog (Hh) signaling pathway with both anticancer and teratogenic activities.

Purmorphamine (also called Shh Signaling Antagonist VI) is a potent purine-based agonist of the hedgehog signaling pathway-smoothened receptor with an EC50 of 1 μM.