Guiding farnesyltransferase inhibitors from an ECLiPS® library to the catalytic zinc

Compounds 8 and 41 are potent analogs of farnesyltransferase inhibitors that were identified from an ECLiPS® library screen. X-ray crystallographic analyses of inhibited complexes show that the side-chain pyridyl of 8 and the imidazoyl of 41 coordinate to the active site zinc.