Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetSerine/threonine-protein kinase pim-1
LigandBDBM28394
Substrate/CompetitorPIM peptide substrate
Meas. Tech.Pim Kinase Dose-Response Assay
pH7.5±n/a
Temperature295.15±n/a K
IC50 57±1.8 nM
Citation Qian, KWang, LCywin, CLFarmer, BTHickey, EHomon, CJakes, SKashem, MALee, GLeonard, SLi, JMagboo, RMao, WPack, EPeng, CProkopowicz, AWelzel, MWolak, JMorwick, T Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode. J Med Chem52:1814-27 (2009) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Serine/threonine-protein kinase pim-1
Name:Serine/threonine-protein kinase pim-1
Synonyms:PIM-1 Kinase | PIM1 | Proto-oncogene serine/threonine-protein kinase Pim-1 | Serine/threonine-protein kinase (PIM1) | Serine/threonine-protein kinase PIM1 | Serine/threonine-protein kinase pim-1 (PIM1)
Type:Protein
Mol. Mass.:35681.82
Organism:Homo sapiens (Human)
Description:P11309
Residue:313
Sequence:
MLLSKINSLAHLRAAPCNDLHATKLAPGKEKEPLESQYQVGPLLGSGGFGSVYSGIRVSD
NLPVAIKHVEKDRISDWGELPNGTRVPMEVVLLKKVSSGFSGVIRLLDWFERPDSFVLIL
ERPEPVQDLFDFITERGALQEELARSFFWQVLEAVRHCHNCGVLHRDIKDENILIDLNRG
ELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSAAVWSLGILLYDMVCGDI
PFEHDEEIIRGQVFFRQRVSSECQHLIRWCLALRPSDRPTFEEIQNHPWMQDVLLPQETA
EIHLHSLSPGPSK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM28394
NameBDBM28394
Synonyms:(2E)-3-{3-[6-(4-methyl-1,4-diazepan-1-yl)pyrazin-2-yl]phenyl}prop-2-enoic acid | pyrazine inhibitor, 1
TypeSmall organic molecule
Emp. Form.C19H22N4O2
Mol. Mass.338.4036
SMILESCN1CCCN(CC1)c1cncc(n1)-c1cccc(\C=C\C(O)=O)c1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
PIM peptide substrate
Name:PIM peptide substrate
Synonyms:n/a
Type:Biotinylated peptide
Mol. Mass.:1402.69
Organism:n/a
Description:n/a
Residue:12
Sequence:
Biotin-AKRRRLSA