Reaction Details |
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Target | Proto-oncogene tyrosine-protein kinase receptor Ret |
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Ligand | BDBM50458627 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1764327 (CHEMBL4199574) |
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IC50 | 6.7±n/a nM |
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Citation | Schenck Eidam, H; Russell, J; Raha, K; DeMartino, M; Qin, D; Guan, HA; Zhang, Z; Zhen, G; Yu, H; Wu, C; Pan, Y; Joberty, G; Zinn, N; Laquerre, S; Robinson, S; White, A; Giddings, A; Mohammadi, E; Greenwood-Van Meerveld, B; Oliff, A; Kumar, S; Cheung, M Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS. ACS Med Chem Lett9:623-628 (2018) [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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BDBM50458627 |
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n/a |
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Name | BDBM50458627 |
Synonyms: | CHEMBL4218127 |
Type | Small organic molecule |
Emp. Form. | C26H26F4N2O4 |
Mol. Mass. | 506.4893 |
SMILES | CCOc1cc(=O)[nH]cc1-c1ccc(CC(=O)Nc2ccc(CC(C)(C)O)c(c2)C(F)(F)F)c(F)c1 |
Structure |
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