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TargetRAF proto-oncogene serine/threonine-protein kinase
LigandBDBM202798
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1663046 (CHEMBL4012727)
EC50 80±n/a nM
Citation Nishiguchi, GARico, ATanner, HAversa, RJTaft, BRSubramanian, SSetti, LBurger, MTWan, LTamez, VSmith, ALou, YBarsanti, PAAppleton, BAMamo, MTandeske, LDix, ITellew, JEHuang, SMathews Griner, LACooke, VGVan Abbema, AMerritt, HMa, SGampa, KFeng, FYuan, JWang, YHaling, JRVaziri, SHekmat-Nejad, MJansen, JMPolyakov, VZang, RSethuraman, VAmiri, PSingh, MLees, EShao, WStuart, DDDillon, MPRamurthy, S Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers. J Med Chem60:4869-4881 (2017) [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 | RAF proto-oncogene serine/threonine-protein kinase (C-Raf) | RAF1 | RAF1_HUMAN | 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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM202798
n/a
NameBDBM202798
Synonyms:US10245267, Example 145 | US10709712, Example 145 | US9242969, 145 | US9694016, 145
TypeSmall organic molecule
Emp. Form.C25H25F3N4O4
Mol. Mass.502.4856
SMILESCc1ncc(NC(=O)c2cccc(c2)C(F)(F)F)cc1-c1cnc(OCCO)c(c1)N1CCOCC1
Structure
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