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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]
Ligand
BDBM50363397
Substrate
n/a
Meas. Tech.
In Vitro Assays
IC50
29.8±n/a nM
Citation
 Kim, JL; Wilson, KJ; Brubaker, JD Inhibitors of RET US Patent  US10183928 Publication Date 1/22/2019 
Target
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:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLILEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM50363397
Synonyms:
CHEMBL1946170 | REGORAFENIB | US10183928, Regorafenib | US10202365, Compound Regorafenib | US10227329, Compound Regorafenib | US10464902, Regorafenib | US10584114, Compound Regorafenib | US10774070, Compound Regorafenib | US11279688, Compound Regorafenib
Type:
Small organic molecule
Emp. Form.:
C21H15ClF4N4O3
Mol. Mass.:
482.815
SMILES:
CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)c(F)c2)ccn1
Structure:
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