Reaction Details |
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Target | Serine/threonine-protein kinase PAK 1 |
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Ligand | BDBM50112349 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1513225 (CHEMBL3610933) |
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IC50 | 54000±n/a nM |
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Citation | Karpov, AS; Amiri, P; Bellamacina, C; Bellance, MH; Breitenstein, W; Daniel, D; Denay, R; Fabbro, D; Fernandez, C; Galuba, I; Guerro-Lagasse, S; Gutmann, S; Hinh, L; Jahnke, W; Klopp, J; Lai, A; Lindvall, MK; Ma, S; Möbitz, H; Pecchi, S; Rummel, G; Shoemaker, K; Trappe, J; Voliva, C; Cowan-Jacob, SW; Marzinzik, AL Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett6:776-81 (2015) [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 |
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Name: | Serine/threonine-protein kinase PAK 1 |
Synonyms: | 2.7.11.1 | Alpha-PAK | Cell division control protein 42 homolog | PAK 1/CDC42 | PAK-1 | PAK1 | PAK1_HUMAN | Serine/threonine-protein kinase PAK 1/PAK 2/PAK 3 | p21-activated kinase 1 | p65-PAK |
Type: | n/a |
Mol. Mass.: | 60640.15 |
Organism: | Homo sapiens (Human) |
Description: | Q13153 |
Residue: | 545 |
Sequence: | MSNNGLDIQDKPPAPPMRNTSTMIGAGSKDAGTLNHGSKPLPPNPEEKKKKDRFYRSILP
GDKTNKKKEKERPEISLPSDFEHTIHVGFDAVTGEFTGMPEQWARLLQTSNITKSEQKKN
PQAVLDVLEFYNSKKTSNSQKYMSFTDKSAEDYNSSNALNVKAVSETPAVPPVSEDEDDD
DDDATPPPVIAPRPEHTKSVYTRSVIEPLPVTPTRDVATSPISPTENNTTPPDALTRNTE
KQKKKPKMSDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTAMDVATGQEVAIKQ
MNLQQQPKKELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYLAGGSLTDVVTETC
MDEGQIAAVCRECLQALEFLHSNQVIHRDIKSDNILLGMDGSVKLTDFGFCAQITPEQSK
RSTMVGTPYWMAPEVVTRKAYGPKVDIWSLGIMAIEMIEGEPPYLNENPLRALYLIATNG
TPELQNPEKLSAIFRDFLNRCLEMDVEKRGSAKELLQHQFLKIAKPLSSLTPLIAAAKEA
TKNNH
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BDBM50112349 |
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n/a |
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Name | BDBM50112349 |
Synonyms: | CHEMBL3609328 |
Type | Small organic molecule |
Emp. Form. | C18H18F2N4 |
Mol. Mass. | 328.3591 |
SMILES | CN1CCN(CC1)C1=Nc2cc(F)ccc2Nc2ccc(F)cc12 |t:8| |
Structure |
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