| Reaction Details |
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 | Report a problem with these data |
| Target | Serine/threonine-protein kinase PAK 1 [249-545,K299R] |
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| Ligand | BDBM6276 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Z'-LYTEBiochemical Assay |
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| IC50 | 483±n/a nM |
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| 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 Chem288:29105-14 (2013) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Serine/threonine-protein kinase PAK 1 [249-545,K299R] |
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| Name: | Serine/threonine-protein kinase PAK 1 [249-545,K299R] |
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| Synonyms: | PAK1 | PAK1_HUMAN | p21-Activated kinase 1 (PAK1) |
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| Type: | Enzyme |
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| Mol. Mass.: | 33244.90 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Human PAK1 truncation (249-545 aa) with K299R mutation |
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| Residue: | 297 |
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| Sequence: | SDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTAMDVATGQEVAIRQMNLQQQPK
KELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYLAGGSLTDVVTETCMDEGQIAA
VCRECLQALEFLHSNQVIHRDIKSDNILLGMDGSVKLTDFGFCAQITPEQSKRSTMVGTP
YWMAPEVVTRKAYGPKVDIWSLGIMAIEMIEGEPPYLNENPLRALYLIATNGTPELQNPE
KLSAIFRDFLNRCLEMDVEKRGSAKELLQHQFLKIAKPLSSLTPLIAAAKEATKNNH
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| BDBM6276 |
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| n/a |
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| Name | BDBM6276 |
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| 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 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H28N6O |
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| Mol. Mass. | 404.508 |
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| SMILES | CN1CCN(CC1)c1ccc(Nc2ncc3ccc(=O)n(C4CCCC4)c3n2)cc1 |
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| Structure | 
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