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Target
Serine/threonine-protein kinase pim-1
Ligand
BDBM50517430
Substrate
n/a
Meas. Tech.
ChEMBL_1869079 (CHEMBL4370145)
IC50
0.080000±n/a nM
Citation
 Wang, HL; Andrews, KL; Booker, SK; Canon, J; Cee, VJ; Chavez, F; Chen, Y; Eastwood, H; Guerrero, N; Herberich, B; Hickman, D; Lanman, BA; Laszlo, J; Lee, MR; Lipford, JR; Mattson, B; Mohr, C; Nguyen, Y; Norman, MH; Pettus, LH; Powers, D; Reed, AB; Rex, K; Sastri, C; Tamayo, N; Wang, P; Winston, JT; Wu, B; Wu, Q; Wu, T; Wurz, RP; Xu, Y; Zhou, Y; Tasker, AS Discovery of ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies. J Med Chem 62:1523-1540 (2019) [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:
BDBM50517430
Synonyms:
CHEMBL4446411
Type:
Small organic molecule
Emp. Form.:
C23H25N5O3
Mol. Mass.:
419.4763
SMILES:
C[C@H]1NC(=O)c2cc([nH]c12)-c1cccc2c1nc(NC1(C)CC1)n(CC1(O)CC1)c2=O |r|
Structure:
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