The target discovery process.
In order to minimise attrition rates in drug development projects, a target discovery process is implemented to select and characterise the most suitable candidate kinase targets, before lead identification and lead optimisation are embarked upon. The process consists of 1) target selection, 2) target assessment, and 3) target validation. This rational approach to target discovery, as a prerequisite for lead discovery, ensures that new therapeutic targets fulfil a set of general criteria, as well as indication-specific, descriptive and functional ones. The approach should ultimately maximise the likelihood of achieving target-selective inhibition by small-molecule inhibitors with minimal in vivo side effects and a therapeutic effect based on a sound biological hypothesis.
Egner
Ursula
U
Research Center Europe, Enabling Technologies, Schering AG, 13342 Berlin, Germany. ursula.egner@schering.de
Krätzschmar
Jörn
J
Kreft
Bertolt
B
Pohlenz
Hans-Dieter
HD
Schneider
Martin
M
D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020411:Oligonucleotide Array Sequence Analysis; D011506:Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D013379:Substrate Specificity
D011506:Proteins