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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM50502477
Substrate
n/a
Meas. Tech.
ChEMBL_1807647 (CHEMBL4307006)
Ki
0.080000±n/a nM
Citation
 Zhan, W; Che, J; Xu, L; Wu, Y; Hu, X; Zhou, Y; Cheng, G; Hu, Y; Dong, X; Li, J Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors. Eur J Med Chem 180:72-85 (2019) [PubMed]  Article 
Target
Name:
RAC-alpha serine/threonine-protein kinase
Synonyms:
AKT phosphorylation (p-AKT) | AKT1 | AKT1/PPP1CA | AKT1_HUMAN | C-AKT | PKB | PKB alpha | Protein kinase Akt-1 | Protein kinase B | Protein kinase B (AKT1) | Protein kinase B (Akt 1) | Protein kinase B (Akt) | Protein kinase B alpha | Protein kinase B alpha (AKT1) | Proto-oncogene Akt (Akt1) | Proto-oncogene c-Akt (AKT) | Proto-oncogene c-Akt (AKT1) | RAC | RAC-PK-alpha | RAC-alpha serine/threonine-protein kinase (AKT) | RAC-alpha serine/threonine-protein kinase (AKT1) | RAC-alpha serine/threonine-protein kinase (pAKT)
Type:
Enzyme
Mol. Mass.:
55681.25
Organism:
Homo sapiens (Human)
Description:
P31749
Residue:
480
Sequence:
MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQREAPLNNFSVAQCQLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDFRSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGIKDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
  
Inhibitor
Name:
BDBM50502477
Synonyms:
ASB-183 | ASB183 | Afuresertib | GSK-2110183C | GSK2110183 | GSK2110183C | Gsk-2110183
Type:
Small organic molecule
Emp. Form.:
C18H17Cl2FN4OS
Mol. Mass.:
427.323
SMILES:
[H][C@@](CN)(Cc1cccc(F)c1)NC(=O)c1cc(c(Cl)s1)-c1c(Cl)cnn1C |r,wU:1.1,wD:1.0,(11.52,-5.94,;10.83,-4.68,;10.06,-6.01,;10.83,-7.35,;12.17,-3.88,;13.49,-4.64,;13.48,-6.2,;14.82,-6.95,;16.15,-6.19,;16.19,-4.64,;17.46,-3.84,;14.79,-3.91,;9.41,-3.84,;8.08,-4.6,;8.11,-6.13,;6.85,-3.92,;5.41,-4.51,;4.4,-3.4,;5.15,-2.04,;4.33,-.64,;6.62,-2.35,;2.85,-3.54,;1.85,-2.41,;2.36,-.88,;.42,-3.01,;.5,-4.52,;2.04,-4.83,;2.44,-6.32,)|
Structure:
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