Reaction Details |
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Target | Serine/threonine-protein kinase PAK 3 |
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Ligand | BDBM50112347 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1513388 (CHEMBL3611428) |
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IC50 | 19±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 3 |
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Name: | Serine/threonine-protein kinase PAK 3 |
Synonyms: | OPHN3 | PAK3 | PAK3_HUMAN | Serine/threonine-protein kinase PAK 1/PAK 2/PAK 3 | Serine/threonine-protein kinase PAK 3 | p21-Activated kinase 3 (PAK3) |
Type: | Enzyme |
Mol. Mass.: | 62298.33 |
Organism: | Homo sapiens (Human) |
Description: | O75914 |
Residue: | 559 |
Sequence: | MSDGLDNEEKPPAPPLRMNSNNRDSSALNHSSKPLPMAPEEKNKKARLRSIFPGGGDKTN
KKKEKERPEISLPSDFEHTIHVGFDAVTGEFTPDLYGSQMCPGKLPEGIPEQWARLLQTS
NITKLEQKKNPQAVLDVLKFYDSKETVNNQKYMSFTSGDKSAHGYIAAHPSSTKTASEPP
LAPPVSEEEDEEEEEEEDENEPPPVIAPRPEHTKSIYTRSVVESIASPAVPNKEVTPPSA
ENANSSTLYRNTDRQRKKSKMTDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTA
LDIATGQEVAIKQMNLQQQPKKELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYL
AGGSLTDVVTETCMDEGQIAAVCRECLQALDFLHSNQVIHRDIKSDNILLGMDGSVKLTD
FGFCAQITPEQSKRSTMVGTPYWMAPEVVTRKAYGPKVDIWSLGIMAIEMVEGEPPYLNE
NPLRALYLIATNGTPELQNPERLSAVFRDFLNRCLEMDVDRRGSAKELLQHPFLKLAKPL
SSLTPLIIAAKEAIKNSSR
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BDBM50112347 |
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n/a |
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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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