Reaction Details |
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Target | RAC-alpha/RAC-beta/RAC-gamma serine/threonine-protein kinase |
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Ligand | BDBM50189603 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_368583 (CHEMBL866827) |
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IC50 | >5000±n/a nM |
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Citation | Borzilleri, RM; Bhide, RS; Barrish, JC; D'Arienzo, CJ; Derbin, GM; Fargnoli, J; Hunt, JT; Jeyaseelan, R; Kamath, A; Kukral, DW; Marathe, P; Mortillo, S; Qian, L; Tokarski, JS; Wautlet, BS; Zheng, X; Lombardo, LJ Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2. J Med Chem49:3766-9 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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RAC-alpha/RAC-beta/RAC-gamma serine/threonine-protein kinase |
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Name: | RAC-alpha/RAC-beta/RAC-gamma serine/threonine-protein kinase |
Synonyms: | Serine/threonine-protein kinase AKT |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 30507 |
Components: | This complex has 3 components. |
Component 1 |
Name: | RAC-beta serine/threonine-protein kinase |
Synonyms: | AKT2 | AKT2_HUMAN | PKB beta | Protein kinase Akt-2 | Protein kinase B (Akt 2) | Protein kinase B beta (AKT2) | Protein kinase B, beta | RAC-PK-beta | RAC-alpha serine/threonine-protein kinase (AKT2) | RAC-beta serine/threonine-protein kinase | RAC-beta serine/threonine-protein kinase (AKT2) | Serine/threonine-protein kinase AKT | Serine/threonine-protein kinase AKT2 | Serine/threonine-protein kinase Rac alpha/beta |
Type: | Enzyme |
Mol. Mass.: | 55766.64 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 481 |
Sequence: | MNEVSVIKEGWLHKRGEYIKTWRPRYFLLKSDGSFIGYKERPEAPDQTLPPLNNFSVAEC
QLMKTERPRPNTFVIRCLQWTTVIERTFHVDSPDEREEWMRAIQMVANSLKQRAPGEDPM
DYKCGSPSDSSTTEEMEVAVSKARAKVTMNDFDYLKLLGKGTFGKVILVREKATGRYYAM
KILRKEVIIAKDEVAHTVTESRVLQNTRHPFLTALKYAFQTHDRLCFVMEYANGGELFFH
LSRERVFTEERARFYGAEIVSALEYLHSRDVVYRDIKLENLMLDKDGHIKITDFGLCKEG
ISDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHERLFE
LILMEEIRFPRTLSPEAKSLLAGLLKKDPKQRLGGGPSDAKEVMEHRFFLSINWQDVVQK
KLLPPFKPQVTSEVDTRYFDDEFTAQSITITPPDRYDSLGLLELDQRTHFPQFSYSASIR
E
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Component 2 |
Name: | RAC-gamma serine/threonine-protein kinase |
Synonyms: | AKT3 | AKT3_HUMAN | PKB gamma | PKBG | Protein kinase Akt-3 | Protein kinase B (Akt 3) | Protein kinase B, gamma | RAC-PK-gamma | RAC-gamma serine/threonine-protein kinase | STK-2 | Serine/threonine-protein kinase AKT | Serine/threonine-protein kinase AKT3 |
Type: | Enzyme |
Mol. Mass.: | 55769.36 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 479 |
Sequence: | MSDVTIVKEGWVQKRGEYIKNWRPRYFLLKTDGSFIGYKEKPQDVDLPYPLNNFSVAKCQ
LMKTERPKPNTFIIRCLQWTTVIERTFHVDTPEEREEWTEAIQAVADRLQRQEEERMNCS
PTSQIDNIGEEEMDASTTHHKRKTMNDFDYLKLLGKGTFGKVILVREKASGKYYAMKILK
KEVIIAKDEVAHTLTESRVLKNTRHPFLTSLKYSFQTKDRLCFVMEYVNGGELFFHLSRE
RVFSEDRTRFYGAEIVSALDYLHSGKIVYRDLKLENLMLDKDGHIKITDFGLCKEGITDA
ATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILM
EDIKFPRTLSSDAKSLLSGLLIKDPNKRLGGGPDDAKEIMRHSFFSGVNWQDVYDKKLVP
PFKPQVTSETDTRYFDEEFTAQTITITPPEKYDEDGMDCMDNERRPHFPQFSYSASGRE
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Component 3 |
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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BDBM50189603 |
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n/a |
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Name | BDBM50189603 |
Synonyms: | CHEMBL377734 | N-cyclopropyl-2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5-yl)methylamino)benzamide |
Type | Small organic molecule |
Emp. Form. | C19H17F2N5OS |
Mol. Mass. | 401.433 |
SMILES | Fc1cc(F)c(cc1NCc1cnc(Nc2ccccn2)s1)C(=O)NC1CC1 |
Structure |
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