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Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM473663
Substrate
n/a
Meas. Tech.
Time-Resolved Fluorescence Transfer (FRET) Assay
IC50
26.5±n/a nM
Citation
 Jordan, AM; Newton, R; Waszkowycz, B; Sutton, JM; Hynd, G; Paoletta, S; Fordyce, EA Heterocyclic compounds as RET kinase inhibitors US Patent  US10844067 Publication Date 11/24/2020 
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:
BDBM473663
Synonyms:
3-(1H-Indol-2-yl)-1-(trans-4- morpholinocyclohexyl)-1H-pyrazolo[3,4- d]pyrimidin-4-amine | US10844067, Example 6 | US11661423, Example 6
Type:
Small organic molecule
Emp. Form.:
C23H27N7O
Mol. Mass.:
417.5068
SMILES:
Nc1ncnc2n(nc(-c3cc4ccccc4[nH]3)c12)C1CC[C@@H](CC1)N1CCOCC1 |r,wU:22.29,(-2.47,4.28,;-2.47,2.74,;-3.81,1.97,;-3.81,.43,;-2.47,-.34,;-1.14,.43,;.33,-.04,;1.23,1.2,;.33,2.45,;.72,3.94,;2.19,4.41,;2.19,5.95,;3.33,6.98,;3.01,8.49,;1.55,8.97,;.4,7.94,;.72,6.43,;-.18,5.18,;-1.14,1.97,;.72,-1.53,;-.36,-2.62,;.03,-4.11,;1.52,-4.5,;2.61,-3.42,;2.21,-1.93,;1.92,-5.99,;.83,-7.08,;1.23,-8.57,;2.72,-8.97,;3.81,-7.88,;3.41,-6.39,)|
Structure:
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