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Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM50563907
Substrate
n/a
Meas. Tech.
ChEMBL_2085409 (CHEMBL4766672)
IC50
188±n/a nM
Citation
 Yang, J; Chen, K; Zhang, G; Yang, QY; Li, YS; Huang, SZ; Wang, YL; Yang, W; Jiang, XJ; Yan, HX; Zhu, JQ; Xiang, R; Luo, YF; Li, WM; Wei, YQ; Li, LL; Yang, SY Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants. Eur J Med Chem 143:1148-1164 (2018) [PubMed]  Article 
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:
BDBM50563907
Synonyms:
CHEMBL4797171
Type:
Small organic molecule
Emp. Form.:
C20H16ClF3N6O2
Mol. Mass.:
464.828
SMILES:
FC(F)(F)c1cc(NC(=O)Nc2ccc(Nc3ncnc4NCCOc34)cc2)ccc1Cl
Structure:
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