Reaction Details |
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Target | RAC-alpha serine/threonine-protein kinase |
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Ligand | BDBM50397782 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_874582 (CHEMBL2186218) |
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IC50 | 840±n/a nM |
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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 Chem55:5291-310 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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RAC-alpha serine/threonine-protein kinase |
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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: | MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQREAPLNNFSVAQC
QLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDF
RSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKI
LKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLS
RERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGI
KDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFEL
ILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKK
LSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
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BDBM50397782 |
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n/a |
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Name | BDBM50397782 |
Synonyms: | CHEMBL2177834 |
Type | Small organic molecule |
Emp. Form. | C33H27N7O2 |
Mol. Mass. | 553.6132 |
SMILES | CC(=O)Nc1cccc(c1)-c1ccc2nc(-c3cccnc3N)n(-c3ccc(CNC(=O)c4ccccc4)cc3)c2n1 |
Structure |
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