Reaction Details |
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Target | Proto-oncogene tyrosine-protein kinase receptor Ret |
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Ligand | BDBM50021574 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1547165 (CHEMBL3756068) |
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IC50 | 358±n/a nM |
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Citation | Yoon, H; Kwak, Y; Choi, S; Cho, H; Kim, ND; Sim, T A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants. J Med Chem59:358-73 (2016) [PubMed] Article |
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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 |
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Name: | Proto-oncogene tyrosine-protein kinase receptor Ret |
Synonyms: | CDHF12 | CDHR16 | Cadherin family member 12 | PTC | Proto-oncogene c-Ret | RET | RET51 | RET_HUMAN | Tyrosine-protein kinase Ret (RET) |
Type: | Protein |
Mol. Mass.: | 124318.29 |
Organism: | Homo sapiens (Human) |
Description: | P07949 |
Residue: | 1114 |
Sequence: | MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
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BDBM50021574 |
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n/a |
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Name | BDBM50021574 |
Synonyms: | BMS-907351 | CABOZANTINIB | CHEBI:72317 | Cabometyx | Cometriq | US10183928, Cabozantinib | US10202365, Compound Cabozantinib | US10227329, Compound Cabozantinib | US10273211, Compound Cabozantinib | US10464902, Cabozantinib | US10774070, Compound Cabozantinib | US11279688, Compound Cabozantinib | XL-184 | cabozantinib s-malate |
Type | Small organic molecule |
Emp. Form. | C28H24FN3O5 |
Mol. Mass. | 501.5057 |
SMILES | COc1cc2nccc(Oc3ccc(NC(=O)C4(CC4)C(=O)Nc4ccc(F)cc4)cc3)c2cc1OC |
Structure |
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