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Target
Serine/threonine-protein kinase PAK 3
Ligand
BDBM101618
Substrate
n/a
Meas. Tech.
ChEMBL_1513382 (CHEMBL3611422)
IC50
99±n/a nM
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 Lett 6:776-81 (2015) [PubMed]  Article 
Target
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:
MSDGLDNEEKPPAPPLRMNSNNRDSSALNHSSKPLPMAPEEKNKKARLRSIFPGGGDKTNKKKEKERPEISLPSDFEHTIHVGFDAVTGEFTPDLYGSQMCPGKLPEGIPEQWARLLQTSNITKLEQKKNPQAVLDVLKFYDSKETVNNQKYMSFTSGDKSAHGYIAAHPSSTKTASEPPLAPPVSEEEDEEEEEEEDENEPPPVIAPRPEHTKSIYTRSVVESIASPAVPNKEVTPPSAENANSSTLYRNTDRQRKKSKMTDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTALDIATGQEVAIKQMNLQQQPKKELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYLAGGSLTDVVTETCMDEGQIAAVCRECLQALDFLHSNQVIHRDIKSDNILLGMDGSVKLTDFGFCAQITPEQSKRSTMVGTPYWMAPEVVTRKAYGPKVDIWSLGIMAIEMVEGEPPYLNENPLRALYLIATNGTPELQNPERLSAVFRDFLNRCLEMDVDRRGSAKELLQHPFLKLAKPLSSLTPLIIAAKEAIKNSSR
  
Inhibitor
Name:
BDBM101618
Synonyms:
US8530652, 114
Type:
Small organic molecule
Emp. Form.:
C25H30N8OS
Mol. Mass.:
490.624
SMILES:
CN(C)C[C@@H](NC(=O)N1Cc2c(Nc3nc(C)nc4ccsc34)n[nH]c2C1(C)C)c1ccccc1
Structure:
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