Target
Serine/threonine-protein kinase PAK 2
Ligand
BDBM101618
Substrate
n/a
Meas. Tech.
ChEMBL_1513381 (CHEMBL3611421)
IC50
190±n/a nM
Citation
 Karpov, ASAmiri, PBellamacina, CBellance, MHBreitenstein, WDaniel, DDenay, RFabbro, DFernandez, CGaluba, IGuerro-Lagasse, SGutmann, SHinh, LJahnke, WKlopp, JLai, ALindvall, MKMa, SMöbitz, HPecchi, SRummel, GShoemaker, KTrappe, JVoliva, CCowan-Jacob, SWMarzinzik, 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 2
Synonyms:
PAK2 | PAK2_HUMAN | Serine/threonine-protein kinase PAK 1/PAK 2/PAK 3 | Serine/threonine-protein kinase PAK 2 | Serine/threonine-protein kinase PAK 2 (PAK2) | p21-Activated kinase 2 (PAK2)
Type:
Enzyme
Mol. Mass.:
58037.40
Organism:
Homo sapiens (Human)
Description:
Q13177
Residue:
524
Sequence:
MSDNGELEDKPPAPPVRMSSTIFSTGGKDPLSANHSLKPLPSVPEEKKPRHKIISIFSGTEKGSKKKEKERPEISPPSDFEHTIHVGFDAVTGEFTGMPEQWARLLQTSNITKLEQKKNPQAVLDVLKFYDSNTVKQKYLSFTPPEKDGFPSGTPALNAKGTEAPAVVTEEEDDDEETAPPVIAPRPDHTKSIYTRSVIDPVPAPVGDSHVDGAAKSLDKQKKKTKMTDEEIMEKLRTIVSIGDPKKKYTRYEKIGQGASGTVFTATDVALGQEVAIKQINLQKQPKKELIINEILVMKELKNPNIVNFLDSYLVGDELFVVMEYLAGGSLTDVVTETCMDEAQIAAVCRECLQALEFLHANQVIHRDIKSDNVLLGMEGSVKLTDFGFCAQITPEQSKRSTMVGTPYWMAPEVVTRKAYGPKVDIWSLGIMAIEMVEGEPPYLNENPLRALYLIATNGTPELQNPEKLSPIFRDFLNRCLEMDVEKRGSAKELLQHPFLKLAKPLSSLTPLIMAAKEAMKSNR
  
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:
Search PDB for entries with ligand similarity: