Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804L]
LigandBDBM311641
Substrate/Competitorn/a
Meas. Tech.Inhibitory Activity Against Resistance Mutation of RET (In Vitro)
IC50 0.900±n/a nM
Citation Miyazaki, IShimamura, TKato, MFujita, HIguchi, S Fused pyrimidine compound or salt thereof US Patent US10155768 Publication Date 12/18/2018
More Info.:Get all data from this article,  Assay Method
 
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]
Name:Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]
Synonyms:CDHF12 | CDHR16 | PTC | RET | RET kinase (V804L) | RET kinase mutant (V804L) | RET51 | RET_HUMAN
Type:Enzyme Catalytic Domain
Mol. Mass.:124332.32
Organism:Homo sapiens (Human)
Description:P07949[V804L]
Residue:1114
Sequence:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLILEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM311641
n/a
NameBDBM311641
Synonyms:Ex. Cpd. 93 | US10807986, Example 93 | US11046696, Compound 93
TypeSmall organic molecule
Emp. Form.C25H25N7O2
Mol. Mass.455.5117
SMILESCOCc1ccc(NC(=O)c2c(C#Cc3cncn3C)n(c3ncnc(N)c23)C2(C)CC2)cc1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: