Reaction Details |
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Target | Proto-oncogene tyrosine-protein kinase receptor Ret [V804L] |
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Ligand | BDBM345847 |
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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] |
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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BDBM345847 |
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n/a |
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Name | BDBM345847 |
Synonyms: | US10202365, Compound 24 | US10774070, Compound 24 |
Type | Small organic molecule |
Emp. Form. | C26H26N10O |
Mol. Mass. | 494.551 |
SMILES | Cc1cc(C)n(n1)-c1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cn1 |
Structure |
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