FastLane structures, Gene to Lead Services and Fragment Library Screening

Gene to lead services and FastLane off-the-shelf kinase structures

We are currently expanding our portfolio with off-the-shelf structures and off-the-Shelf complexes with pre-screened kinase-bound ligands. CK2 and PIM1 protein kinase are available in ligand-free form for crystallization with our customers ligands, as well as in complex with small-molecule fragment ready to enter a drug discovery program. The fragments originate from our proprietary Global Kinase Library and IOTA 1500 fragment library. We also provide gene to lead services, which include lead generation for your kinase of interest. Our customers may also choose from our library of FastLane structures. We have more than 50 kinases, available for quick delivery in complex with your compounds:

  • • Silver - Proteins ready to be expressed, purified and crystallized according to existing verified protocols. Complex structures can be delivered within 6 to 12 weeks.[+]
    • Kinases (A-M)[+]
      AK1 - Adenylate kinase isoenzyme 1 (a.a. 1-193).
      AK2 - Adenylate kinase isoenzyme 2, mitochondrial (a.a. 1-239).
      AK3L1 - Adenylate kinase isoenzyme 4, mitochondrial (1-223).
      AK5 - Adenylate kinase isoenzyme 5 (a.a. 366-562).
      BMPR2 - Bone morphogenetic protein receptor type-2 (a.a. 189-517).
      CAMK1D - Calcium/calmodulin-dependent protein kinase type 1D (a.a. 1-333).
      CAMK1G - Calcium/calmodulin-dependent protein kinase type 1G (a.a. 18-316).
      CAMK2A - Calcium/calmodulin-dependent protein kinase type II subunit alpha (a.a. 13-302).
      CAMK2B - Calcium/calmodulin-dependent protein kinase type II subunit beta (a.a. 11-303).
      CAMK2D - Calcium/calmodulin-dependent protein kinase type II subunit delta (a.a. 11-309).
      DYRK2 - Dual specificity tyrosine-phosphorylation-regulated kinase 2 (a.a. 146-552).
      FLT1 (VEGFR1) - Tyrosine-protein kinase receptor FLT (a.a. 801-1158).
      GAK - Cyclin-G-associated kinase (a.a. 12-347).
      ITPK1 - Inositol-tetrakisphosphate 1-kinase (a.a. 1-327).
      ITPKC - Inositol-trisphosphate 3-kinase C (a.a. 425-683).
      MAP2K6 - Dual specificity mitogen-activated protein kinase kinase 6 (a.a. 47-334)
      MAP3K5 - Mitogen-activated protein kinase kinase kinase 5 (MAPK/ERK kinase kinase 5), (a.a. 659-951).
      MAPK11 - Mitogen-activated protein kinase 11 (p38b), (a.a. 5-350).
      MAPK6 - Mitogen-activated protein kinase 6 (a.a. 9-327).
      MST4 - Serine/threonine-protein kinase (a.a. 1-300).
      CAMK2G - Calcium/calmodulin-dependent protein kinase type II subunit gamma (a.a. 5-315).
      CAMK4 - Calcium/calmodulin-dependent protein kinase type IV (a.a. 15-340).
      CLK1 - Dual specificity protein kinase CLK1 (a.a. 148-484).
      CLK2 - Dual specificity protein kinase CLK2 (a.a. 135-496).
      CLK3 - Dual specificity protein kinase CLK3 (a.a. 284-638).
      CSNK1G1 - Casein kinase I isoform gamma-1 (a.a. 45-352).
      CSNK1G2 - Casein kinase I isoform gamma-2 (a.a. 43-353).
      CSNK1G3 - Casein kinase I isoform gamma-3 (a.a. 35-362).
      DAPK3 - Death-associated protein kinase 3 (a.a. 9-289).
      DMPK1 - Myotonin-protein kinase (a.a. 11-420).
      DYRK1A - Dual specificity tyrosine-phosphorylation-regulated kinase 1A (a.a. 127-485).
    • Kinases (N-V)[+]
      NEK2 - Serine/threonine-protein kinase (a.a. 1-271).
      PAK4 - Serine/threonine-protein kinase PAK 4 (a.a. 291-591).
      PAK7 - Serine/threonine-protein kinase PAK 7 (a.a. 425-719).
      PAK6 - Serine/threonine-protein kinase PAK 6 (a.a. 383-681).
      PCTK1 - Cyclin-dependent kinase 16 (a.a. 163-478).
      PIK3C3 - Phosphatidylinositol 3-kinase catalytic subunit type 3 (a.a. 268-879).
      PIM1 - Serine/threonine-protein kinase pim-1 (a.a. 92-403).
      PIM2 - Serine/threonine-protein kinase pim-2 (1-311).
      STK10 - Serine/threonine-protein kinase 10 (a.a. 18-317).
      STK16 - Serine/threonine-protein kinase 16 (a.a. 13-304).
      STK17B - Serine/threonine-protein kinase 17B (a.a. 25-329).
      TTK - Dual specificity protein kinase TTK (a.a. 519-808)
      VRK1 - Serine/threonine-protein kinase (a.a. 3-364).
      VRK2 - Serine/threonine-protein kinase (a.a. 14-335)
      PIP4K2A - Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha (a.a. 35-405).
      PIP5K2C - Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma (a.a. 32-421).
      PIP5K2C - Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma (a.a. 32-421).
      PKM2 - Pyruvate kinase isozymes (a.a. 3-530)
      PKMYT1 - Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (a.a. 75-362).
      PTK2B - Protein-tyrosine kinase 2-beta (a.a. 414-692).
      RPS6KA1 - Ribosomal protein S6 kinase alpha-1 (a.a. 413-719).
Premium - Purified proteins stored in our lab and ready to be co-crystallized with costumers compounds. Delivery time 2 to 6 weeks.
Our premium products are available in ligand-free form for crystallization with our customers ligands, as well as in complex with small-molecule fragments ready to enter a drug discovery program. Please
contact us for details.
Stacks Image 7051

Vps34 (PIK3C3)

CK2 kinase structure

CK2 kinase

PIM1 kinase structure

PIM1 kinase

Our Gene to lead services include experimental support within the following areas:
  • Kinase expression and purification and kinase assays
  • Tertiary structure determination of kinase targets and their ligand complexes by X-ray crystallography
  • Screening & fragment-based kinase drug discovery
  • Hit-to-lead discovery
  • Structure-based drug design