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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [M918T]
Ligand
BDBM577022
Substrate
n/a
IC50
0.800±n/a nM
Citation
 Walls, SM; Ren, L; Ramann, GA; Moreno, DA; Metcalf, AT; McFaddin, EA; Kolakowski, GR; Blake, JF; Dai, D; Haas, J; Jiang, Y; Kahn, D Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors US Patent  US11472802 Publication Date 10/18/2022 
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:
BDBM577022
Synonyms:
3-(5-cyclopropyl-4-(1-methyl- 1H-imidazol-4-yl)isoxazol-3- yl)-1-isopropyl-1H- pyrazolo[4,3-c]pyridin-4- amine | US11472802, Example 31
Type:
Small organic molecule
Emp. Form.:
C19H21N7O
Mol. Mass.:
363.4163
SMILES:
CC(C)n1nc(-c2noc(C3CC3)c2-c2cn(C)cn2)c2c(N)nccc12
Structure:
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