| Reaction Details |
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 | Report a problem with these data |
| Target | Proto-oncogene tyrosine-protein kinase receptor Ret [G810R] |
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| Ligand | BDBM305680 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | RET G810R Mutant Assay |
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| IC50 | 114±n/a nM |
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| Citation |  Andrews, SW; Aronow, S; Blake, JF; Brandhuber, BJ; Collier, J; Cook, A; Haas, J; Jiang, Y; Kolakowski, GR; Mcfaddin, EA; Mckenney, ML; McNulty, OT; Metcalf, AT; Moreno, DA; Ramann, GA; Tang, TP; Ren, L; Walls, SM Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors US Patent US11648243 Publication Date 5/16/2023 |
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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 [G810R] |
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| Name: | Proto-oncogene tyrosine-protein kinase receptor Ret [G810R] |
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| Synonyms: | CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (G810R) | RET | RET Kinase (G810R) | RET kinase mutant (G810R) | RET51 | RET_HUMAN | ret enzyme (g810r) |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 124418.43 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P07949[G810R] |
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| Residue: | 1114 |
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| Sequence: | MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLIVEYAKYRSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
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| BDBM305680 |
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| n/a |
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| Name | BDBM305680 |
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| Synonyms: | US10144734, Example 698 | US10172845, Example 698 | US10441581, Example 698 | US10881652, Example 698 | US11648243, Example 698 |
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| Type | Small organic molecule |
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| Emp. Form. | C32H36ClN9O2 |
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| Mol. Mass. | 614.14 |
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| SMILES | Cc1cccc(Cl)c1C(=O)NC1(C)CCN(CC1)c1cnc(cn1)-c1cc(OCCN2CCNCC2)cn2ncc(C#N)c12 |
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| Structure | 
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