Reaction Details |
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Target | Proto-oncogene tyrosine-protein kinase receptor Ret [V804L] |
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Ligand | BDBM435018 |
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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 | <500±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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BDBM435018 |
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n/a |
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Name | BDBM435018 |
Synonyms: | US10584114, Compound 144 | US11279688, Compound 144 |
Type | Small organic molecule |
Emp. Form. | C26H28FN9O |
Mol. Mass. | 501.5586 |
SMILES | C[C@H](NC(=O)C1CCC(=CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1 |r,c:8| |
Structure |
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