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Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM473686
Substrate
n/a
Meas. Tech.
Time-Resolved Fluorescence Transfer (FRET) Assay
IC50
10.3±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:
BDBM473686
Synonyms:
US10844067, Example 29 | US10844067, Example 30 | US11661423, Example 30 | tert-Butyl N-[cis-4-(4-amino-3-{3-chloro- 1H-pyrrolo[2,3-b]pyridin-2-yl}-1H- pyrazolo[3,4-d]pyrimidin-1- yl)cyclohexyl]carbamate
Type:
Small organic molecule
Emp. Form.:
C23H27ClN8O2
Mol. Mass.:
482.966
SMILES:
CC(C)(C)OC(=O)N[C@H]1CCC(CC1)n1nc(-c2[nH]c3ncccc3c2Cl)c2c(N)ncnc12 |r,wU:8.7,(5.31,-8.33,;3.82,-7.93,;3.42,-9.42,;4.22,-6.44,;2.33,-7.53,;1.93,-6.04,;3.02,-4.96,;.45,-5.65,;.05,-4.16,;-1.45,-3.71,;-1.85,-2.22,;-.76,-1.13,;.72,-1.53,;1.12,-3.02,;-1.16,.36,;-.26,1.6,;-1.16,2.85,;-.76,4.34,;-1.67,5.58,;-.76,6.83,;-1.08,8.33,;.06,9.37,;1.53,8.89,;1.85,7.38,;.7,6.35,;.7,4.81,;2.04,4.04,;-2.63,2.37,;-3.96,3.14,;-3.96,4.68,;-5.29,2.37,;-5.29,.83,;-3.96,.06,;-2.63,.83,)|
Structure:
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