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Target
Serine/threonine-protein kinase PAK 1 [249-545,K299R]
Ligand
BDBM50112347
Substrate
n/a
Meas. Tech.
Z'-LYTEBiochemical Assay
IC50
7.7±0.0 nM
Citation
 Licciulli, S; Maksimoska, J; Zhou, C; Troutman, S; Kota, S; Liu, Q; Duron, S; Campbell, D; Chernoff, J; Field, J; Marmorstein, R; Kissil, JL FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J Biol Chem 288:29105-14 (2013) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase PAK 1 [249-545,K299R]
Synonyms:
PAK1 | PAK1_HUMAN | p21-Activated kinase 1 (PAK1)
Type:
Enzyme
Mol. Mass.:
33244.90
Organism:
Homo sapiens (Human)
Description:
Human PAK1 truncation (249-545 aa) with K299R mutation
Residue:
297
Sequence:
SDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTAMDVATGQEVAIRQMNLQQQPKKELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYLAGGSLTDVVTETCMDEGQIAAVCRECLQALEFLHSNQVIHRDIKSDNILLGMDGSVKLTDFGFCAQITPEQSKRSTMVGTPYWMAPEVVTRKAYGPKVDIWSLGIMAIEMIEGEPPYLNENPLRALYLIATNGTPELQNPEKLSAIFRDFLNRCLEMDVEKRGSAKELLQHQFLKIAKPLSSLTPLIAAAKEATKNNH
  
Inhibitor
Name:
BDBM50112347
Synonyms:
CHEMBL3609327 | FRAX597
Type:
Small organic molecule
Emp. Form.:
C29H28ClN7OS
Mol. Mass.:
558.097
SMILES:
CCn1c2nc(Nc3ccc(cc3)N3CCN(C)CC3)ncc2cc(-c2ccc(cc2Cl)-c2cncs2)c1=O
Structure:
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