Target
Serine/threonine-protein kinase pim-1
Ligand
BDBM50500182
Substrate
n/a
Meas. Tech.
ChEMBL_1543994 (CHEMBL3750239)
Ki
<1.000000±n/a nM
Citation
 Burger, MTNishiguchi, GHan, WLan, JSimmons, RAtallah, GDing, YTamez, VZhang, YMathur, MMuller, KBellamacina, CLindvall, MKZang, RHuh, KFeucht, PZavorotinskaya, TDai, YBasham, SChan, JGinn, EAycinena, AHolash, JCastillo, JLangowski, JLWang, YChen, MYLambert, AFritsch, CKauffmann, APfister, EVanasse, KGGarcia, PD Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies. J Med Chem 58:8373-86 (2015) [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:
BDBM50500182
Synonyms:
CHEMBL3747545
Type:
Small organic molecule
Emp. Form.:
C23H22F3N5O
Mol. Mass.:
441.4489
SMILES:
C[C@@H]1C[C@H](N)CN(C1)c1ccncc1NC(=O)c1ccc(F)c(n1)-c1c(F)cccc1F |r,wU:1.0,3.3,(-2.4,-6.01,;-1.33,-5.39,;0,-6.16,;1.34,-5.39,;2.41,-6,;1.33,-3.85,;,-3.08,;-1.33,-3.85,;,-1.54,;1.33,-.77,;1.33,.77,;,1.54,;-1.33,.77,;-1.33,-.77,;-2.67,-1.54,;-4,-.77,;-4,.47,;-5.34,-1.53,;-6.67,-.76,;-8.01,-1.53,;-8.01,-3.07,;-9.07,-3.69,;-6.67,-3.84,;-5.34,-3.07,;-6.67,-5.38,;-8.01,-6.16,;-9.07,-5.54,;-8,-7.7,;-6.67,-8.46,;-5.34,-7.69,;-5.34,-6.15,;-4.27,-5.53,)|
Structure:
Search PDB for entries with ligand similarity: