Target
Proto-oncogene tyrosine-protein kinase receptor Ret [G810R]
Ligand
BDBM597673
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
IC50
3.70±n/a nM
Citation
 Blake, JFDai, DHaas, JJiang, YKolakowski, GRMcFaddin, EAMcKenney, MLMetcalf, ATMoreno, DAPrigaro, BRamann, GARen, L Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors US Patent  US11603374 Publication Date 3/14/2023 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [G810R]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (G810R) | RET | RET Kinase (G810R) | RET kinase mutant (G810R) | RET51 | RET_HUMAN | ret enzyme (g810r)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
124418.43
Organism:
Homo sapiens (Human)
Description:
P07949[G810R]
Residue:
1114
Sequence:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYRSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM597673
Synonyms:
US11603374, Example 28
Type:
Small organic molecule
Emp. Form.:
C17H19N5O2
Mol. Mass.:
325.3651
SMILES:
Nc1ncnc2n(cc(-c3cc(on3)C3CC3)c12)[C@@H]1C[C@H](CO)C1 |r,wU:18.21,20.24,(-2.78,4.69,;-3.17,3.2,;-4.68,2.88,;-5.16,1.42,;-4.13,.27,;-2.62,.59,;-1.37,-.31,;-.13,.59,;-.6,2.06,;.17,3.39,;1.71,3.39,;2.18,4.85,;.94,5.76,;-.31,4.85,;3.67,5.25,;5.16,4.85,;4.76,6.34,;-2.14,2.06,;-1.37,-1.85,;-2.46,-2.94,;-1.37,-4.03,;-1.37,-5.57,;-.04,-6.34,;-.29,-2.94,)|
Structure:
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