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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM15138
Substrate
n/a
Meas. Tech.
ChEMBL_874386 (CHEMBL2183039)
IC50
>100000±n/a nM
Citation
 Ashwell, MA; Lapierre, JM; Brassard, C; Bresciano, K; Bull, C; Cornell-Kennon, S; Eathiraj, S; France, DS; Hall, T; Hill, J; Kelleher, E; Khanapurkar, S; Kizer, D; Koerner, S; Link, J; Liu, Y; Makhija, S; Moussa, M; Namdev, N; Nguyen, K; Nicewonger, R; Palma, R; Szwaya, J; Tandon, M; Uppalapati, U; Vensel, D; Volak, LP; Volckova, E; Westlund, N; Wu, H; Yang, RY; Chan, TC Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors. J Med Chem 55:5291-310 (2012) [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:
BDBM15138
Synonyms:
5-indazolyl pyridine 11g | 5-{5-[(2S)-2-amino-3-phenylpropoxy]pyridin-3-yl}-3-methyl-1H-indazole | A-674563 | Biochemistry 469551 Compound 11 | indazole-pyridine, 7
Type:
Small organic molecule
Emp. Form.:
C22H22N4O
Mol. Mass.:
358.4363
SMILES:
Cc1n[nH]c2ccc(cc12)-c1cncc(OC[C@@H](N)Cc2ccccc2)c1 |r|
Structure:
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