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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [V804M]
Ligand
BDBM84747
Substrate
n/a
Meas. Tech.
Measurement of Inhibitory Activity Against RET (V804M)
IC50
4330±n/a nM
Citation
 Miyazaki, I; Shimamura, T; Kato, M; Fujita, H; Iguchi, S Fused pyrimidine compound or salt thereof US Patent  US10155768 Publication Date 12/18/2018 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [V804M]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (V804M) | RET | RET kinase mutant (V804M) | RET51 | RET_HUMAN | ret enzyme (v804m)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
124350.36
Organism:
Homo sapiens (Human)
Description:
P07949[V804M]
Residue:
1114
Sequence:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIMEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM84747
Synonyms:
(B) ZD6474 | US10155768, Vandetanib | US10183928, Vandetanib | US10202365, Compound Vandetanib | US10227329, Compound Vandetanib | US11046696, Vandetanib | US11279688, Compound Vandetanib | Vandetanib
Type:
n/a
Emp. Form.:
C22H24BrFN4O
Mol. Mass.:
459.355
SMILES:
CN1CCC(COc2cc3ncnc(Nc4ccc(Br)cc4F)c3cc2C)CC1
Structure:
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