ALW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor, used for cancer treatment.

NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.

UniPR1331 (UniPR-1331) is a selective, orally available antagonist of Eph/ephrin interaction with pIC50 of 5.45, IC50 of 2.9 uM.

UniPR129 is a potent but problematic Eph/ephrin antagonist. UniPR129 has the potential for the research of cancer disease.

BT5528 is a bicyclic peptide toxin conjugate, an EphA2 activator. BT5528 is made up of a bicyclic peptide and Auristatin E, is derivated from BCY6099. BT5528 shows potent anti-tumor activity without bleeding or coagulation toxicity in rats model.

Targefrin is a potent, selective antagonist targeting ligand binding domain of receptor tyrosine kinase EphA2 (EphA2-LBD), binds to EphA2-LBD with Kd of 21 nM (ITC) and shows IC50 value of 10.8 nM in biochemical assays.

WCDD301 is a high-affinity, orally available agonist of EphA4 receptor.