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Target
Serine/threonine-protein kinase pim-1
Ligand
BDBM11835
Substrate
PIM substrate p21
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
120±20 nM
Citation
 Pogacic, V; Bullock, AN; Fedorov, O; Filippakopoulos, P; Gasser, C; Biondi, A; Meyer-Monard, S; Knapp, S; Schwaller, J Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity. Cancer Res 67:6916-24 (2007) [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:
BDBM11835
Synonyms:
1-(3-{6-[(cyclopropylmethyl)amino]imidazo[1,2-a]pyridazin-3-yl}phenyl)ethan-1-one | CHEMBL200528 | Cancer Res 676916 Compound K00135 | Imidazol[1,2-b]pyridazine 1
Type:
Small organic molecule
Emp. Form.:
C18H18N4O
Mol. Mass.:
306.3617
SMILES:
CC(=O)c1cccc(c1)-c1cnc2ccc(NCC3CC3)nn12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PIM substrate p21
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1281.47
Organism:
n/a
Description:
n/a
Residue:
10
Sequence:
RKRRQTSMTD