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Target
Serine/threonine-protein kinase pim-1
Ligand
BDBM28397
Substrate
PIM peptide substrate
Meas. Tech.
Pim Kinase Dose-Response Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
13±0.5 nM
Citation
 Qian, K; Wang, L; Cywin, CL; Farmer, BT; Hickey, E; Homon, C; Jakes, S; Kashem, MA; Lee, G; Leonard, S; Li, J; Magboo, R; Mao, W; Pack, E; Peng, C; Prokopowicz, A; Welzel, M; Wolak, J; Morwick, 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 Chem 52:1814-27 (2009) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase pim-1
Synonyms:
PIM-1 Kinase | PIM1 | PIM1_HUMAN | Proto-oncogene serine/threonine-protein kinase Pim-1 | Serine/threonine-protein kinase (PIM1) | Serine/threonine-protein kinase PIM | 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:
MLLSKINSLAHLRAAPCNDLHATKLAPGKEKEPLESQYQVGPLLGSGGFGSVYSGIRVSDNLPVAIKHVEKDRISDWGELPNGTRVPMEVVLLKKVSSGFSGVIRLLDWFERPDSFVLILERPEPVQDLFDFITERGALQEELARSFFWQVLEAVRHCHNCGVLHRDIKDENILIDLNRGELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSAAVWSLGILLYDMVCGDIPFEHDEEIIRGQVFFRQRVSSECQHLIRWCLALRPSDRPTFEEIQNHPWMQDVLLPQETAEIHLHSLSPGPSK
  
Inhibitor
Name:
BDBM28397
Synonyms:
(2E)-3-(3-{6-[(4-aminocyclohexyl)amino]pyrazin-2-yl}phenyl)prop-2-enoic acid | pyrazine inhibitor, 23
Type:
Small organic molecule
Emp. Form.:
C19H22N4O2
Mol. Mass.:
338.4036
SMILES:
N[C@H]1CC[C@@H](CC1)Nc1cncc(n1)-c1cccc(\C=C\C(O)=O)c1 |r,wU:4.7,wD:1.0,(-2.78,-3.68,;-2.78,-2.14,;-1.45,-1.37,;-1.45,.17,;-2.78,.94,;-4.12,.17,;-4.12,-1.37,;-2.78,2.48,;-1.45,3.25,;-1.45,4.8,;-.12,5.57,;1.22,4.8,;1.22,3.25,;-.12,2.48,;2.55,2.48,;3.88,3.26,;5.22,2.48,;5.22,.94,;3.88,.17,;3.88,-1.37,;5.22,-2.14,;5.22,-3.68,;6.55,-4.45,;3.88,-4.45,;2.55,.94,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PIM peptide substrate
Synonyms:
n/a
Type:
Biotinylated peptide
Mol. Mass.:
1402.69
Organism:
n/a
Description:
n/a
Residue:
12
Sequence:
ITINAKRRRLSA