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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, MT; Nishiguchi, G; Han, W; Lan, J; Simmons, R; Atallah, G; Ding, Y; Tamez, V; Zhang, Y; Mathur, M; Muller, K; Bellamacina, C; Lindvall, MK; Zang, R; Huh, K; Feucht, P; Zavorotinskaya, T; Dai, Y; Basham, S; Chan, J; Ginn, E; Aycinena, A; Holash, J; Castillo, J; Langowski, JL; Wang, Y; Chen, MY; Lambert, A; Fritsch, C; Kauffmann, A; Pfister, E; Vanasse, KG; Garcia, 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
More Info.:
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,)|