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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM50150700
Substrate
n/a
Meas. Tech.
ChEMBL_304613 (CHEMBL828500)
IC50
>20000±n/a nM
Citation
 Engler, TA; Henry, JR; Malhotra, S; Cunningham, B; Furness, K; Brozinick, J; Burkholder, TP; Clay, MP; Clayton, J; Diefenbacher, C; Hawkins, E; Iversen, PW; Li, Y; Lindstrom, TD; Marquart, AL; McLean, J; Mendel, D; Misener, E; Briere, D; O'Toole, JC; Porter, WJ; Queener, S; Reel, JK; Owens, RA; Brier, RA; Eessalu, TE; Wagner, JR; Campbell, RM; Vaughn, R Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. J Med Chem 47:3934-7 (2004) [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:
BDBM50150700
Synonyms:
7-(4-Imidazo[1,2-a]pyridin-3-yl-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl)-3,4-dihydro-1H-[1,4]diazepino[6,7,1-hi]indole-2-carboxylic acid isopropyl ester | CHEMBL363058
Type:
Small organic molecule
Emp. Form.:
C26H23N5O4
Mol. Mass.:
469.4919
SMILES:
CC(C)OC(=O)N1CCn2cc(C3=C(C(=O)NC3=O)c3cnc4ccccn34)c3cccc(C1)c23 |t:12|
Structure:
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