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Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM473695
Substrate
n/a
Meas. Tech.
Time-Resolved Fluorescence Transfer (FRET) Assay
IC50
1.30±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:
BDBM473695
Synonyms:
1-(cis-4-Aminocyclohexyl)-3-(3-chloro-1H- pyrrolo[2,3-b]pyridin-2-yl)-1H- pyrazolo[3,4-d]pyrimidin-4-amine dihydrochloride | US10844067, Example 38 | US11661423, Example 38
Type:
Small organic molecule
Emp. Form.:
C18H19ClN8
Mol. Mass.:
382.85
SMILES:
N[C@H]1CCC(CC1)n1nc(-c2[nH]c3ncccc3c2Cl)c2c(N)ncnc12 |r,wU:1.0,(1.48,-7.48,;1.08,-5.99,;-.41,-5.59,;-.81,-4.11,;.28,-3.02,;1.77,-3.42,;2.17,-4.9,;-.12,-1.53,;.79,-.28,;-.12,.96,;.28,2.45,;-.62,3.7,;.28,4.94,;-.04,6.45,;1.11,7.48,;2.57,7,;2.89,5.5,;1.75,4.47,;1.75,2.93,;3.08,2.16,;-1.58,.49,;-2.92,1.26,;-2.92,2.8,;-4.25,.49,;-4.25,-1.05,;-2.92,-1.82,;-1.58,-1.05,)|
Structure:
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