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Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM435017
Substrate
n/a
Meas. Tech.
Biochemical Activity 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
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:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM435017
Synonyms:
US10584114, Compound 142 | US11279688, Compound 142
Type:
Small organic molecule
Emp. Form.:
C28H32F2N8O2
Mol. Mass.:
550.6029
SMILES:
CO[C@]1(CC[C@](F)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1 |r,wU:2.25,26.29,5.5,wD:2.1,(1.11,-1.56,;1.11,-.02,;-.22,.75,;-.99,2.08,;-2.53,2.08,;-3.3,.75,;-4.07,-.59,;-2.53,-.59,;-.99,-.59,;-4.84,.75,;-5.61,2.08,;-7.15,2.08,;-7.92,3.41,;-7.92,.75,;-7.15,-.59,;-7.92,-1.92,;-9.46,-1.92,;-10.37,-.67,;-11.83,-1.15,;-13.08,-.24,;-11.83,-2.69,;-10.37,-3.17,;-5.61,-.59,;1.11,1.52,;1.11,3.06,;2.44,.75,;3.78,1.52,;3.78,3.06,;5.11,.75,;6.44,1.52,;7.78,.75,;7.78,-.79,;6.44,-1.56,;5.11,-.79,;9.11,-1.56,;10.52,-.94,;11.55,-2.08,;13.08,-1.92,;10.78,-3.41,;9.27,-3.09,)|
Structure:
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