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TargetRAF proto-oncogene serine/threonine-protein kinase
LigandBDBM50428286
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1495745
IC50 150±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
More Info.:Get all data from this article,  Assay Method
 
RAF proto-oncogene serine/threonine-protein kinase
Name:RAF proto-oncogene serine/threonine-protein kinase
Synonyms:C-Raf Protein Kinase | Proto-oncogene c-RAF (RAF1) | RAF proto-oncogene serine/threonine-protein kinase (C-Raf) | RAF1 | Raf-1 | Serine/threonine-protein kinase RAF | Serine/threonine-protein kinase C-Raf | cRaf
Type:Serine/threonine-protein kinase
Mol. Mass.:73082.52
Organism:Homo sapiens (Human)
Description:P04049
Residue:648
Sequence:
MEHIQGAWKTISNGFGFKDAVFDGSSCISPTIVQQFGYQRRASDDGKLTDPSKTSNTIRV
FLPNKQRTVVNVRNGMSLHDCLMKALKVRGLQPECCAVFRLLHEHKGKKARLDWNTDAAS
LIGEELQVDFLDHVPLTTHNFARKTFLKLAFCDICQKFLLNGFRCQTCGYKFHEHCSTKV
PTMCVDWSNIRQLLLFPNSTIGDSGVPALPSLTMRRMRESVSRMPVSSQHRYSTPHAFTF
NTSSPSSEGSLSQRQRSTSTPNVHMVSTTLPVDSRMIEDAIRSHSESASPSALSSSPNNL
SPTGWSQPKTPVPAQRERAPVSGTQEKNKIRPRGQRDSSYYWEIEASEVMLSTRIGSGSF
GTVYKGKWHGDVAVKILKVVDPTPEQFQAFRNEVAVLRKTRHVNILLFMGYMTKDNLAIV
TQWCEGSSLYKHLHVQETKFQMFQLIDIARQTAQGMDYLHAKNIIHRDMKSNNIFLHEGL
TVKIGDFGLATVKSRWSGSQQVEQPTGSVLWMAPEVIRMQDNNPFSFQSDVYSYGIVLYE
LMTGELPYSHINNRDQIIFMVGRGYASPDLSKLYKNCPKAMKRLVADCVKKVKEERPLFP
QILSSIELLQHSLPKINRSASEPSLHRAAHTEDINACTLTTSPRLPVF
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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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