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Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM296724
Substrate
n/a
Meas. Tech.
Enzyme Assay
IC50
10.6±n/a nM
Citation
 Andrews, SW; Aronow, S; Blake, JF; Brandhuber, BJ; Cook, A; Haas, J; Jiang, Y; Kolakowski, GR; McFaddin, EA; McKenney, ML; McNulty, OT; Metcalf, AT; Moreno, DA; Tang, TP; Ren, L Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors US Patent  US10953005 Publication Date 3/23/2021 
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:
BDBM296724
Synonyms:
US10112942, Example 459 | US10137124, Example 459 | US10555944, Example 459 | US10953005, Example 459
Type:
Small organic molecule
Emp. Form.:
C29H29N7O3
Mol. Mass.:
523.5857
SMILES:
COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC3C[C@H](O)C3)cn3ncc(C#N)c23)cn1 |r,wU:26.29,(12.54,-2.37,;11.21,-1.6,;9.87,-2.37,;8.54,-1.6,;7.21,-2.37,;7.21,-3.91,;5.87,-4.68,;4.54,-3.91,;3.21,-4.68,;3.21,-3.14,;4.54,-2.37,;3.21,-1.6,;1.87,-2.37,;1.87,-3.91,;.54,-1.6,;-.8,-2.37,;-2.13,-1.6,;-2.13,-.06,;-.8,.71,;.54,-.06,;-3.46,.71,;-4.8,-.06,;-6.13,.71,;-7.46,-.06,;-8.95,.33,;-9.72,1.67,;-11.05,.9,;-12.54,1.3,;-10.28,-.44,;-6.13,2.25,;-4.8,3.02,;-4.48,4.52,;-2.94,4.68,;-2.32,3.28,;-.83,2.88,;.66,2.48,;-3.46,2.25,;8.54,-4.68,;9.87,-3.91,)|
Structure:
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