Reaction Details |
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Target | Proto-oncogene tyrosine-protein kinase receptor Ret [V804M] |
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Ligand | BDBM50389730 |
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Substrate/Competitor | n/a |
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Meas. Tech. | RET and KDR Enzyme Assay |
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IC50 | 1870±n/a nM |
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Citation | Jordan, AM; Newton, R; Waszkowycz, B; Sutton, JM; Hynd, G; Paoletta, S; Fordyce, EA Heterocyclic compounds as RET kinase inhibitors US Patent US11661423 Publication Date 5/30/2023 |
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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 [V804M] |
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Name: | Proto-oncogene tyrosine-protein kinase receptor Ret [V804M] |
Synonyms: | CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (V804M) | RET | RET kinase mutant (V804M) | RET51 | RET_HUMAN | ret enzyme (v804m) |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 124350.36 |
Organism: | Homo sapiens (Human) |
Description: | P07949[V804M] |
Residue: | 1114 |
Sequence: | MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLIMEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
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BDBM50389730 |
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n/a |
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Name | BDBM50389730 |
Synonyms: | CHEMBL2069946 | US10172858, Table 2.7 | US10544104, Compound 24 | US10844067, Example 44 | US11247972, Compound 24 | US11661423, Example 44 | US9765037, Compound 24 | US9828378, # 7 |
Type | Small organic molecule |
Emp. Form. | C16H16N6 |
Mol. Mass. | 292.3384 |
SMILES | CC(C)n1nc(-c2cc3ccccc3[nH]2)c2c(N)ncnc12 |
Structure |
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