Blockers of human T cell Kv1.3 potassium channels using de novo ligand design and solid-phase parallel combinatorial chemistry

Blockers of the human Kv1.3 potassium channel were designed using Biosym/MSIʹs ligand design program LUDI. Parallel combinatorial synthesis of the resultant substituted phenyl-stilbenes on solid phase, followed by 125I Charybdotoxin (125I ChTx) screening, yielded 12 Kv1.3 channel blockers with modest activity.