Target
Serine/threonine-protein kinase PAK 4
Ligand
BDBM50112355
Substrate
n/a
Meas. Tech.
ChEMBL_1513393 (CHEMBL3611548)
IC50
779±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 4
Synonyms:
KIAA1142 | PAK4 | PAK4_HUMAN | p21-Activated kinase 4 (PAK4)
Type:
Protein
Mol. Mass.:
64098.01
Organism:
Homo sapiens (Human)
Description:
O96013
Residue:
591
Sequence:
MFGKRKKRVEISAPSNFEHRVHTGFDQHEQKFTGLPRQWQSLIEESARRPKPLVDPACITSIQPGAPKTIVRGSKGAKDGALTLLLDEFENMSVTRSNSLRRDSPPPPARARQENGMPEEPATTARGGPGKAGSRGRFAGHSEAGGGSGDRRRAGPEKRPKSSREGSGGPQESSRDKRPLSGPDVGTPQPAGLASGAKLAAGRPFNTYPRADTDHPSRGAQGEPHDVAPNGPSAGGLAIPQSSSSSSRPPTRARGAPSPGVLGPHASEPQLAPPACTPAAPAVPGPPGPRSPQREPQRVSHEQFRAALQLVVDPGDPRSYLDNFIKIGEGSTGIVCIATVRSSGKLVAVKKMDLRKQQRRELLFNEVVIMRDYQHENVVEMYNSYLVGDELWVVMEFLEGGALTDIVTHTRMNEEQIAAVCLAVLQALSVLHAQGVIHRDIKSDSILLTHDGRVKLSDFGFCAQVSKEVPRRKSLVGTPYWMAPELISRLPYGPEVDIWSLGIMVIEMVDGEPPYFNEPPLKAMKMIRDNLPPRLKNLHKVSPSLKGFLDRLLVRDPAQRATAAELLKHPFLAKAGPPASIVPLMRQNRTR
  
Inhibitor
Name:
BDBM50112355
Synonyms:
CHEMBL3609326
Type:
Small organic molecule
Emp. Form.:
C25H23Cl2FN6O
Mol. Mass.:
513.394
SMILES:
CCn1c2nc(Nc3ccc(N4CCNCC4)c(F)c3)ncc2cc(-c2ccc(Cl)cc2Cl)c1=O
Structure:
Search PDB for entries with ligand similarity: