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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]
Ligand
BDBM435018
Substrate
n/a
Meas. Tech.
RET V804L Gatekeeper Mutant Assay
IC50
<10±n/a nM
Citation
 Brubaker, JD; Kim, JL; Wilson, KJ; Wilson, D; DiPietro, LV Inhibitors of RET US Patent  US11279688 Publication Date 3/22/2022 
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:
BDBM435018
Synonyms:
US10584114, Compound 144 | US11279688, Compound 144
Type:
Small organic molecule
Emp. Form.:
C26H28FN9O
Mol. Mass.:
501.5586
SMILES:
C[C@H](NC(=O)C1CCC(=CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1 |r,c:8|
Structure:
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