Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetC-RAF
LigandBDBM88106
Substrate/CompetitorMEK1 (K97R)
Meas. Tech.Raf Activity Assay
pH7.5±n/a
Temperature298.15±n/a K
IC50 0.54±n/a nM
Commentsextracted
Citation Aversa, RJBarsanti, PABurger, MDillon, MPDipesa, AHu, CLou, YNishiguchi, GPan, YPolyakov, VRamurthy, SRico, ASetti, LSmith, ASubramanian, STaft, BTanner, HWan, LYusuff, N Biaryl amide compounds as kinase inhibitors US Patent US9694016 Publication Date 7/4/2017
More Info.:Get all data from this article,  Assay Method
 
C-RAF
Name:C-RAF
Synonyms:Proto-oncogene C-Raf (C-Raf FL) | RAF proto-oncogene serine/threonine-protein kinase
Type:n/a
Mol. Mass.:73012.38
Organism:Homo sapiens (Human)
Description:n/a
Residue:648
Sequence:
MEHIQGAWKTISNGFGFKDAVFDGSSCISPTIVQQFGYQRRASDDGKLTDPSKTSNTIRV
FLPNKQRTVVNVRNGMSLHDCLMKALKVRGLQPECCAVFRLLHEHKGKKARLDWNTDAAS
LIGEELQVDFLDHVPLTTHNFARKTFLKLAFCDICQKFLLNGFRCQTCGYKFHEHCSTKV
PTMCVDWSNIRQLLLFPNSTIGDSGVPALPSLTMRRMRESVSRMPVSSQHRYSTPHAFTF
NTSSPSSEGSLSQRQRSTSTPNVHMVSTTLPVDSRMIEDAIRSHSESASPSALSSSPNNL
SPTGWSQPKTPVPAQRERAPVSGTQEKNKIRPRGQRDSSEEWEIEASEVMLSTRIGSGSF
GTVYKGKWHGDVAVKILKVVDPTPEQFQAFRNEVAVLRKTRHVNILLFMGYMTKDNLAIV
TQWCEGSSLYKHLHVQETKFQMFQLIDIARQTAQGMDYLHAKNIIHRDMKSNNIFLHEGL
TVKIGDFGLATVKSRWSGSQQVEQPTGSVLWMAPEVIRMQDNNPFSFQSDVYSYGIVLYE
LMTGELPYSHINNRDQIIFMVGRGYASPDLSKLYKNCPKAMKRLVADCVKKVKEERPLFP
QILSSIELLQHSLPKINRSASEPSLHRAAHTEDINACTLTTSPRLPVF
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM88106
NameBDBM88106
Synonyms:US10245267, Example 1143 | US10709712, Example 1143 | US9694016, 1143
TypeSmall organic molecule
Emp. Form.C25H27F2N5O3
Mol. Mass.483.5104
SMILESCCOc1cc(cc(n1)N1CCOCC1)-c1cc(NC(=O)c2ccnc(c2)C(C)(F)F)cnc1C
Structure
MEK1 (K97R)
Name:MEK1 (K97R)
Synonyms:Dual specificity mitogen-activated protein kinase kinase 1 (MEK1)(K97R)
Type:n/a
Mol. Mass.:43467.04
Organism:Homo sapiens (Human)
Description:Biotinylated full length MEK1 with an inactivating K97R ATP binding site mutation.
Residue:393
Sequence:
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARRLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff: