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Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM473725
Substrate
n/a
Meas. Tech.
RET and KDR Enzyme Assay
IC50
2.00±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  US11661423 Publication Date 5/30/2023 
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:
BDBM473725
Synonyms:
N-[trans-4-[4-Amino-3-(3-chloro-1H- pyrrolo[2,3-b]pyridin-2-yl)pyrazolo[3,4- d]pyrimidin-1- yl]cyclohexyl]cyclopropanecarboxamide | US10844067, Example 68 | US11661423, Example 68
Type:
Small organic molecule
Emp. Form.:
C22H23ClN8O
Mol. Mass.:
450.924
SMILES:
Nc1ncnc2n(nc(-c3[nH]c4ncccc4c3Cl)c12)C1CC[C@@H](CC1)NC(=O)C1CC1 |r,wU:23.30,(-3.56,3.74,;-3.56,2.2,;-4.9,1.43,;-4.9,-.11,;-3.56,-.88,;-2.23,-.11,;-.76,-.59,;.14,.66,;-.76,1.91,;-.36,3.39,;-1.27,4.64,;-.36,5.89,;-.68,7.39,;.46,8.42,;1.92,7.95,;2.24,6.44,;1.1,5.41,;1.1,3.87,;2.43,3.1,;-2.23,1.43,;-.36,-2.07,;-1.45,-3.16,;-1.06,-4.65,;.43,-5.05,;1.52,-3.96,;1.12,-2.47,;.83,-6.54,;2.32,-6.93,;2.72,-8.42,;3.41,-5.85,;4.9,-5.45,;3.81,-4.36,)|
Structure:
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