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Targetp21-Activated kinase 1 (PAK1)
LigandBDBM6276
Substrate/Competitorn/a
Meas. Tech.Z'-LYTEBiochemical Assay
IC50 483± 0 nM
Citation Licciulli, SMaksimoska, JZhou, CTroutman, SKota, SLiu, QDuron, SCampbell, DChernoff, JField, JMarmorstein, RKissil, JL FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J Biol Chem288:29105-14 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
p21-Activated kinase 1 (PAK1)
Name:p21-Activated kinase 1 (PAK1)
Synonyms:n/a
Type:Enzyme
Mol. Mass.:33244.90
Organism:Homo sapiens (Human)
Description:Human PAK1 truncation (249-545 aa) with K299R mutation
Residue:297
Sequence:
SDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTAMDVATGQEVAIRQMNLQQQPK
KELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYLAGGSLTDVVTETCMDEGQIAA
VCRECLQALEFLHSNQVIHRDIKSDNILLGMDGSVKLTDFGFCAQITPEQSKRSTMVGTP
YWMAPEVVTRKAYGPKVDIWSLGIMAIEMIEGEPPYLNENPLRALYLIATNGTPELQNPE
KLSAIFRDFLNRCLEMDVEKRGSAKELLQHQFLKIAKPLSSLTPLIAAAKEATKNNH
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  Blast E-value cutoff:
BDBM6276
NameBDBM6276
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
TypeSmall organic molecule
Emp. Form.C23H28N6O
Mol. Mass.404.508
SMILESCN1CCN(CC1)c1ccc(Nc2ncc3ccc(=O)n(C4CCCC4)c3n2)cc1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a