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TargetSerine/threonine-protein kinase A-Raf
LigandBDBM50428286
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1495743
IC50 26±n/a nM
Citation Henry JRKaufman MDPeng SBAhn YMCaldwell TMVogeti LTelikepalli HLu WPHood MMRutkoski TJSmith BDVogeti SMiller DWise SCChun LZhang XZhang YKays LHipskind PAWrobleski ADLobb KLClay JMCohen JDWalgren JLMcCann DPatel PClawson DKGuo SManglicmot DGroshong CLogan CStarling JJFlynn DL Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. J Med Chem 58:4165-79 (2015) [PubMed]  Article
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Serine/threonine-protein kinase A-Raf
Name:RAF serine/threonine protein kinase
Synonyms:ARAF | ARAF1 | PKS | PKS2 | Proto-oncogene A-Raf | Proto-oncogene A-Raf-1 | Proto-oncogene Pks
Type:Enzyme
Mol. Mass.:67610.81
Organism:Homo sapiens (Human)
Description:P10398
Residue:606
Sequence:
MEPPRGPPANGAEPSRAVGTVKVYLPNKQRTVVTVRDGMSVYDSLDKALKVRGLNQDCCV
VYRLIKGRKTVTAWDTAIAPLDGEELIVEVLEDVPLTMHNFVRKTFFSLAFCDFCLKFLF
HGFRCQTCGYKFHQHCSSKVPTVCVDMSTNRQQFYHSVQDLSGGSRQHEAPSNRPLNELL
TPQGPSPRTQHCDPEHFPFPAPANAPLQRIRSTSTPNVHMVSTTAPMDSNLIQLTGQSFS
TDAAGSRGGSDGTPRGSPSPASVSSGRKSPHSKSPAEQRERKSLADDKKKVKNLGYRDSG
YYWEVPPSEVQLLKRIGTGSFGTVFRGRWHGDVAVKVLKVSQPTAEQAQAFKNEMQVLRK
TRHVNILLFMGFMTRPGFAIITQWCEGSSLYHHLHVADTRFDMVQLIDVARQTAQGMDYL
HAKNIIHRDLKSNNIFLHEGLTVKIGDFGLATVKTRWSGAQPLEQPSGSVLWMAAEVIRM
QDPNPYSFQSDVYAYGVVLYELMTGSLPYSHIGCRDQIIFMVGRGYLSPDLSKISSNCPK
AMRRLLSDCLKFQREERPLFPQILATIELLQRSLPKIERSASEPSLHRTQADELPACLLS
AARLVP
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BDBM50428286
n/a
NameBDBM50428286
Synonyms:DABRAFENIB | GSK2118436A
TypeSmall organic molecule
Emp. Form.C23H20F3N5O2S2
Mol. Mass.519.562
SMILESCC(C)(C)c1nc(c(s1)-c1ccnc(N)n1)-c1cccc(NS(=O)(=O)c2c(F)cccc2F)c1F
Structure
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