| Reaction Details |
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 | Report a problem with these data |
| Target | Proto-oncogene tyrosine-protein kinase receptor Ret [V804L] |
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| Ligand | BDBM345853 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | RET V804L Gatekeeper Mutant Assay at KM |
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| IC50 | <10±n/a nM |
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| Citation |  Brooijmans, N; DiPietro, LV; Fleming, PE; Kim, JL; Wenglowsky, SM; Zhang, Y 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors US Patent US10774070 Publication Date 9/15/2020 |
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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] |
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| Synonyms: | CDHF12 | CDHR16 | PTC | RET | RET kinase (V804L) | RET kinase mutant (V804L) | RET51 | RET_HUMAN |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 124332.32 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P07949[V804L] |
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| Residue: | 1114 |
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| Sequence: | MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLILEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
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| BDBM345853 |
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| n/a |
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| Name | BDBM345853 |
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| Synonyms: | US10202365, Compound 30 | US10774070, Compound 30 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H22F2N10O |
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| Mol. Mass. | 516.5054 |
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| SMILES | C[C@H](NC(=O)c1ncc(cc1F)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1 |r| |
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| Structure | 
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