Focal adhesion kinase (FAK) is considered as an attractive target for oncology, and small- molecule inhibitors are reported to be in clinical testing. In a surface plasmon resonance (SPR)-mediated fragment screening campaign, we discovered bicyclic scaffolds like 1 H- pyrazolo [3, 4-d] pyrimidines binding to the hinge region of FAK. By an accelerated knowledge-based fragment growing approach, essential pharmacophores were added. ...