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TargetPAK1
LigandBDBM101618
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1513380
IC50 14±n/a nM
Citation Karpov, ASAmiri, PBellamacina, CBellance, MHBreitenstein, WDaniel, DDenay, RFabbro, DFernandez, CGaluba, IGuerro-Lagasse, SGutmann, SHinh, LJahnke, WKlopp, JLai, ALindvall, MKMa, SM÷bitz, 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 Lett6:776-81 (2015) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
PAK1
Name:PAK1
Synonyms:2.7.11.1 | Alpha-PAK | PAK-1 | Serine/threonine-protein kinase PAK 1 | 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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM101618
NameBDBM101618
Synonyms:US8530652, 114
TypeSmall organic molecule
Emp. Form.C25H30N8OS
Mol. Mass.490.624
SMILESCN(C)C[C@@H](NC(=O)N1Cc2c(Nc3nc(C)nc4ccsc34)n[nH]c2C1(C)C)c1ccccc1
Structure
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n/a