Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetProto-oncogene tyrosine-protein kinase receptor Ret
LigandBDBM50153899
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1560166 (CHEMBL3778237)
IC50 44±n/a nM
Citation Newton, RBowler, KABurns, EMChapman, PJFairweather, EEFritzl, SJGoldberg, KMHamilton, NMHolt, SVHopkins, GVJones, SDJordan, AMLyons, AJNikki March, HMcDonald, NQMaguire, LAMould, DPPurkiss, AGSmall, HFStowell, AIThomson, GJWaddell, IDWaszkowycz, BWatson, AJOgilvie, DJ The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. Eur J Med Chem112:20-32 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Proto-oncogene tyrosine-protein kinase receptor Ret
Name:Proto-oncogene tyrosine-protein kinase receptor Ret
Synonyms:CDHF12 | CDHR16 | Cadherin family member 12 | PTC | Proto-oncogene c-Ret | RET | RET51 | RET_HUMAN | Tyrosine-protein kinase Ret (RET)
Type:Protein
Mol. Mass.:124318.29
Organism:Homo sapiens (Human)
Description:P07949
Residue:1114
Sequence:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50153899
n/a
NameBDBM50153899
Synonyms:CHEMBL3775940
TypeSmall organic molecule
Emp. Form.C17H16FN3O3
Mol. Mass.329.3256
SMILESCOc1cc2ncnc(Nc3c(C)c(O)ccc3F)c2cc1OC
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: