Table 2  The names, structures, targets, FBDD optimization strategy used, biophysical techniques used, and status in clinical trials of select drugs derived from the FBDD approach.
Drug (Company)  Target  Original Fragment(s) *  Advanced Molecule and Progress in Clinical Trials  Techniques Used
Vemurafenib (Plexxikon) [224,226]  BRAF-V600E   Approved  high-concentration biochemical fragment screening, X-ray crystallography
Venetoclax (AbbVie, Genetech) [227,228,229,230]  BCL-2   Approved  NMR, X-ray crystallography
Ribociclib (Novartis Europharm Limited) [231]  CDK4 and 6  Information Not Available  Approved  Information not Available
PLX3397 (Plexxikon) [232,233,234]  FMS, KIT, and FLT3-ITD   Phase 3  X-ray crystallography, Structure Confirmed by NMR, MS, and HPLC
Verubecestat (Merck) [235,236]  BACE1   Phase 3  NMR, X-ray crystallography, inhibition of cathepsin D
Onalespib (Astex) [237,238]  HSP90   Phase 2  X-ray crystallography, isothermal titration calorimetry, NMR
AZD5099 [239,240]  Topoisomerase II   Phase 1  NMR, Surface Plasmon Resonance, isothermal calorimetry, X-ray cystallography
AT7519 [241,242,243,244]  CDK 1, 2, 4, and 5   Phase 2  NMR, MS, X-ray crystallography
* Structures for some of the fragments are taken directly from Dan Erlanson’s blog at [245].