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Target
RAC-gamma serine/threonine-protein kinase
Ligand
BDBM50170284
Substrate
n/a
Meas. Tech.
ChEMBL_1905007 (CHEMBL4407365)
IC50
1.3±n/a nM
Citation
 Dong, X; Zhan, W; Zhao, M; Che, J; Dai, X; Wu, Y; Xu, L; Zhou, Y; Zhao, Y; Tian, T; Cheng, G; Jin, Z; Li, J; Shao, Y; He, Q; Yang, B; Weng, Q; Hu, Y Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design. J Med Chem 62:7264-7288 (2019) [PubMed]  Article 
Target
Name:
RAC-gamma serine/threonine-protein kinase
Synonyms:
AKT3 | AKT3_HUMAN | PKB gamma | PKBG | Protein kinase Akt-3 | Protein kinase B (Akt 3) | Protein kinase B, gamma | RAC-PK-gamma | RAC-gamma serine/threonine-protein kinase | STK-2 | Serine/threonine-protein kinase AKT | Serine/threonine-protein kinase AKT3
Type:
Enzyme
Mol. Mass.:
55769.36
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
479
Sequence:
MSDVTIVKEGWVQKRGEYIKNWRPRYFLLKTDGSFIGYKEKPQDVDLPYPLNNFSVAKCQLMKTERPKPNTFIIRCLQWTTVIERTFHVDTPEEREEWTEAIQAVADRLQRQEEERMNCSPTSQIDNIGEEEMDASTTHHKRKTMNDFDYLKLLGKGTFGKVILVREKASGKYYAMKILKKEVIIAKDEVAHTLTESRVLKNTRHPFLTSLKYSFQTKDRLCFVMEYVNGGELFFHLSRERVFSEDRTRFYGAEIVSALDYLHSGKIVYRDLKLENLMLDKDGHIKITDFGLCKEGITDAATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEDIKFPRTLSSDAKSLLSGLLIKDPNKRLGGGPDDAKEIMRHSFFSGVNWQDVYDKKLVPPFKPQVTSETDTRYFDEEFTAQTITITPPEKYDEDGMDCMDNERRPHFPQFSYSASGRE
  
Inhibitor
Name:
BDBM50170284
Synonyms:
GSK2141795 | GSK2141795C | Uprosertib
Type:
Small organic molecule
Emp. Form.:
C18H16Cl2F2N4O2
Mol. Mass.:
429.248
SMILES:
Cn1ncc(Cl)c1-c1cc(oc1Cl)C(=O)N[C@H](CN)Cc1ccc(F)c(F)c1 |r,wD:16.18,(2.37,-.54,;3.52,.49,;3.36,2.02,;4.77,2.65,;5.8,1.51,;7.33,1.67,;5.03,.17,;5.65,-1.23,;7.16,-1.55,;7.32,-3.09,;5.91,-3.71,;4.88,-2.57,;3.35,-2.73,;8.65,-3.86,;9.99,-3.09,;8.65,-5.4,;9.99,-6.17,;11.32,-5.4,;12.65,-6.17,;9.99,-7.71,;11.32,-8.48,;12.65,-7.71,;13.99,-8.48,;13.99,-10.02,;15.32,-10.79,;12.65,-10.79,;12.65,-12.33,;11.32,-10.02,)|
Structure:
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