Target
RAC-alpha serine/threonine-protein kinase [E49C,C296S,C310S,C344S]
Ligand
BDBM153712
Substrate
n/a
Meas. Tech.
iFLik Assay
pH
7.4±n/a
Kd
2.2e+3± 7e+2 nM
Comments
extracted
Citation
 Fang, ZSimard, JRPlenker, DNguyen, HDPhan, TWolle, PBaumeister, SRauh, D Discovery of inter-domain stabilizers-a novel assay system for allosteric akt inhibitors. ACS Chem Biol 10:279-88 (2015) [PubMed]  Article 
Target
Name:
RAC-alpha serine/threonine-protein kinase [E49C,C296S,C310S,C344S]
Synonyms:
AKT1 | AKT1_HUMAN | PKB | Protein kinase B (Akt1 E49C, C296S, C310S and C344S ) | RAC
Type:
Protein
Mol. Mass.:
55608.09
Organism:
Homo sapiens (Human)
Description:
Human Akt1 containing mutations E49C, C296S, C310S and C344S
Residue:
480
Sequence:
MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQRCAPLNNFSVAQCQLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDFRSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLSKEGIKDGATMKTFSGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMSGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
  
Inhibitor
Name:
BDBM153712
Synonyms:
5,7-diphenyl-N-(thiophen-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (8d)
Type:
Small organic molecule
Emp. Form.:
C23H18N4S
Mol. Mass.:
382.481
SMILES:
C(Nc1ncnc2n(cc(-c3ccccc3)c12)-c1ccccc1)c1cccs1
Structure:
Search PDB for entries with ligand similarity: