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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM145920
Substrate
n/a
Meas. Tech.
TR-FRET Assay
pH
7.5000±n/a
IC50
5±n/a nM
Comments
extracted
Citation
 Vennemann, M; Bär, T; Maier, T; Hölder, S; Beneke, G; Dehmel, F; Zülch, A; Strub, A; Beckers, T; Ince, S; Rehwinkel, H; Liu, N; Bömer, U Fused pyrimidines US Patent  US8957064 Publication Date 2/17/2015 
Target
Name:
RAC-alpha serine/threonine-protein kinase
Synonyms:
AKT phosphorylation (p-AKT) | C-AKT | 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-PK-alpha | RAC-alpha serine/threonine-protein kinase (AKT) | RAC-alpha serine/threonine-protein kinase (AKT1) | RAC-alpha serine/threonine-protein kinase (pAKT) | AKT1/PPP1CA | AKT1_HUMAN | AKT1 | PKB | RAC
Type:
Enzyme
Mol. Mass.:
55681.25
Organism:
Human
Description:
P31749
Residue:
480
Sequence:
MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQREAPLNNFSVAQCQLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDFRSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGIKDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
  
Inhibitor
Name:
BDBM145920
Synonyms:
US8957064, 48.1
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
COC(=O)c1cnn2cc(c(nc12)-c1ccc(CN2CCC(CC2)c2n[nH]c(n2)-c2ccccn2)cc1)-c1c(F)cccc1F |(-11.96,4.7,;-11.56,3.21,;-10.07,2.81,;-8.98,3.9,;-9.67,1.32,;-10.58,.08,;-9.67,-1.17,;-8.21,-.69,;-6.88,-1.46,;-5.54,-.69,;-5.54,.85,;-6.88,1.62,;-8.21,.85,;-4.21,1.62,;-2.88,.85,;-1.54,1.62,;-1.54,3.16,;-.21,3.93,;1.13,3.16,;1.13,1.62,;2.46,.85,;3.79,1.62,;3.79,3.16,;2.46,3.93,;5.13,.85,;5.13,-.69,;6.59,-1.17,;7.5,.08,;6.59,1.32,;8.98,.47,;10.07,-.61,;11.56,-.22,;11.96,1.27,;10.87,2.36,;9.38,1.96,;-2.88,3.93,;-4.21,3.16,;-4.77,-2.03,;-5.54,-3.36,;-7.08,-3.36,;-4.77,-4.7,;-3.23,-4.7,;-2.46,-3.36,;-3.23,-2.03,;-2.46,-.69,)|
Structure:
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