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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM50325983
Substrate
n/a
Meas. Tech.
ChEMBL_1672661 (CHEMBL4022690)
IC50
>10000±n/a nM
Citation
Wagman, AS; Boyce, RS; Brown, SP; Fang, E; Goff, D; Jansen, JM; Le, VP; Levine, BH; Ng, SC; Ni, ZJ; Nuss, JM; Pfister, KB; Ramurthy, S; Renhowe, PA; Ring, DB; Shu, W; Subramanian, S; Zhou, XA; Shafer, CM; Harrison, SD; Johnson, KW; Bussiere, DE Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3. J Med Chem 60:8482-8514 (2017) [PubMed] Article
More Info.:
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:
BDBM50325983
Synonyms:
6-(2-(4-(2,4-dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-ylamino)ethylamino)nicotinonitrile | CHEMBL412142 | CHIR-99021 | CT 99021 | US11203601, Compound Table 1.19
Type:
Small organic molecule
Emp. Form.:
C22H18Cl2N8
Mol. Mass.:
465.338
SMILES:
Cc1c[nH]c(n1)-c1cnc(NCCNc2ccc(cn2)C#N)nc1-c1ccc(Cl)cc1Cl