Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetRAF proto-oncogene serine/threonine-protein kinase
LigandBDBM50396483
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1495599
IC50 410±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 Chem58:4165-79 (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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50396483
NameBDBM50396483
Synonyms:PLX-4032 | RG 7204 | Ro 5185426 | US9388165, Reference, Vemurafenib (PLX-4032) | USRE47451, PLX-4032, Roche | VEMURAFENIB
TypeSmall organic molecule
Emp. Form.C23H18ClF2N3O3S
Mol. Mass.489.922
SMILESCCCS(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(cc23)-c2ccc(Cl)cc2)c1F
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a