Reaction Details |
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Target | Proto-oncogene tyrosine-protein kinase receptor Ret [V804L] |
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Ligand | BDBM21 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Measurement of Biochemical Activity of Compounds |
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IC50 | 3597±n/a nM |
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Citation | Brubaker, JD; Kim, JL; Wilson, KJ; Wilson, D; DiPietro, LV Inhibitors of RET US Patent US10584114 Publication Date 3/10/2020 |
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More Info.: | Get all data from this article, Assay Method |
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Proto-oncogene tyrosine-protein kinase receptor Ret [V804L] |
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Name: | Proto-oncogene tyrosine-protein kinase receptor Ret [V804L] |
Synonyms: | CDHF12 | CDHR16 | PTC | RET | RET kinase (V804L) | RET kinase mutant (V804L) | RET51 | RET_HUMAN |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 124332.32 |
Organism: | Homo sapiens (Human) |
Description: | P07949[V804L] |
Residue: | 1114 |
Sequence: | MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLILEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
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BDBM21 |
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n/a |
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Name | BDBM21 |
Synonyms: | CHEMBL24828 | N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine | VANDETANIB | ZD-6474 | ZD6474 | cid_3081361 |
Type | n/a |
Emp. Form. | C22H24BrFN4O2 |
Mol. Mass. | 475.354 |
SMILES | COc1cc2c(Nc3ccc(Br)cc3F)ncnc2cc1OCC1CCN(C)CC1 |
Structure |
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