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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM50194671
Substrate
n/a
Meas. Tech.
ChEMBL_396656 (CHEMBL871549)
IC50
>25000±n/a nM
Citation
 DiMauro, EF; Newcomb, J; Nunes, JJ; Bemis, JE; Boucher, C; Buchanan, JL; Buckner, WH; Cee, VJ; Chai, L; Deak, HL; Epstein, LF; Faust, T; Gallant, P; Geuns-Meyer, SD; Gore, A; Gu, Y; Henkle, B; Hodous, BL; Hsieh, F; Huang, X; Kim, JL; Lee, JH; Martin, MW; Masse, CE; McGowan, DC; Metz, D; Mohn, D; Morgenstern, KA; Oliveira-dos-Santos, A; Patel, VF; Powers, D; Rose, PE; Schneider, S; Tomlinson, SA; Tudor, YY; Turci, SM; Welcher, AA; White, RD; Zhao, H; Zhu, L; Zhu, X Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. J Med Chem 49:5671-86 (2006) [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:
BDBM50194671
Synonyms:
4-methyl-3-(2-(methylamino)quinazolin-6-yl)-N-(2-(1-methylpiperidin-4-yloxy)-5-(trifluoromethyl)phenyl)benzamide | CHEMBL386661
Type:
Small organic molecule
Emp. Form.:
C30H30F3N5O2
Mol. Mass.:
549.5867
SMILES:
CNc1ncc2cc(ccc2n1)-c1cc(ccc1C)C(=O)Nc1cc(ccc1OC1CCN(C)CC1)C(F)(F)F
Structure:
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