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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [V804M]
Ligand
BDBM488466
Substrate
n/a
Meas. Tech.
Enzyme Assay
IC50
3000±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  US10954241 Publication Date 3/23/2021 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [V804M]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (V804M) | RET | RET kinase mutant (V804M) | RET51 | RET_HUMAN | ret enzyme (v804m)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
124350.36
Organism:
Homo sapiens (Human)
Description:
P07949[V804M]
Residue:
1114
Sequence:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIMEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM488466
Synonyms:
1-Isopropyl-3-[6-(1,3,4-thiadiazol-2-yl)-1H-indol- 2-yl]pyrazolo[3,4-d]pyrimidin-4-amine | US10954241, Example 106 | US11548896, Example 106
Type:
Small organic molecule
Emp. Form.:
C18H16N8S
Mol. Mass.:
376.438
SMILES:
CC(C)n1nc(-c2cc3ccc(cc3[nH]2)-c2nncs2)c2c(N)ncnc12
Structure:
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