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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [M918T]
Ligand
BDBM597663
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
IC50
0.700±n/a nM
Citation
 Blake, JF; Dai, D; Haas, J; Jiang, Y; Kolakowski, GR; McFaddin, EA; McKenney, ML; Metcalf, AT; Moreno, DA; Prigaro, B; Ramann, GA; Ren, 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 [M918T]
Synonyms:
CDHF12 | CDHR16 | PTC | RET | RET51 | RET_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
124288.20
Organism:
Homo sapiens (Human)
Description:
P07949[M918T]
Residue:
1114
Sequence:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWTAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM597663
Synonyms:
7-cyclobutyl-5-(5- cyclopropylisoxazol-3-yl)- 7H-pyrrolo[2,3-d] pyrimidin-4-amine | US11603374, Example 18
Type:
Small organic molecule
Emp. Form.:
C16H17N5O
Mol. Mass.:
295.3391
SMILES:
Nc1ncnc2n(cc(-c3cc(on3)C3CC3)c12)C1CCC1
Structure:
Search PDB for entries with ligand similarity: