Reaction Details Report a problem with these data
Target
Serine/threonine-protein kinase PAK 1 [249-545,K299R]
Ligand
BDBM6276
Substrate
n/a
Meas. Tech.
Z'-LYTEBiochemical Assay
IC50
483±n/a 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:
BDBM6276
Synonyms:
8-Cyclopentyl-2-[4-(4-methylpiperazin-1-yl)phenylamino]-8H-pyrido[2,3-d]pyrimidin-7-one | 8-cyclopentyl-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one | FRAX019 | N8 Pyrido[2,3-d]pyrimidin-7-one deriv. 68 | Pyrido[2,3-d]pyrimidin-7-one 1
Type:
Small organic molecule
Emp. Form.:
C23H28N6O
Mol. Mass.:
404.508
SMILES:
CN1CCN(CC1)c1ccc(Nc2ncc3ccc(=O)n(C4CCCC4)c3n2)cc1
Structure:
Search PDB for entries with ligand similarity: