Reaction Details |
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Target | Proto-oncogene tyrosine-protein kinase receptor Ret |
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Ligand | BDBM347342 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1764328 (CHEMBL4199575) |
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Kd | 20.0±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: | 2.7.10.1 | Extracellular cell-membrane anchored RET cadherin 120 kDa fragment | Proto-oncogene tyrosine-protein kinase receptor Ret | RET_RAT | Ret | Soluble RET kinase fragment |
Type: | PROTEIN |
Mol. Mass.: | 124235.77 |
Organism: | Rattus norvegicus |
Description: | ChEMBL_117886 |
Residue: | 1115 |
Sequence: | MAKARSGAAGLGLKLFLLLPLLGEAPLGLYFSRDAYWERLYVDQPAGTPLLYVHALRDAP
GEVPSFRLGQYLYGVYRTRLHENDWIHIDSGTGLLYLNQSLDHSSWEQLSIRNGGFPLLT
VFLQVFLGSTAQREGECHWPGCARVYFSFINDTFPNCSSFKARDLCTPETGVSFRIRENR
PPGTFYQFRMLPVQFLCPNISVKYKLLEGDGLPFRCDPDCLEVSTRWALDRELQEKYVLE
AECAVAGPGANKEKVAVSFPVTVYDEDDSPPTFSGGVGTASAVVEFKRKEGTVVATLQVF
DADVVPASGELVRRYTSTLLSGDSWAQQTFRVEHTPNETLVQSNNNSVRATMHNYKLVLN
RSLSISESRVLQLVVLVNDSDFQGPGSGVLFLHFNVSVLPVTLNLPMAYSFPVNRRARRY
AQIGKVCVENCQEFSGVSIQYKLQPSSTNCSALGVVTSTEDTSGTLYVNDTEALRRPECT
ELQYTVVATDRQTRRQTQASLVVTVEGTYIAEEVGCPKSCAVNKRRPECEECGGLGSPTG
RCEWRQGDGKGITRNFSTCSPSTRTCPDGHCDALESRDINICPQDCLRGPIVGGHERGER
QGIKAGYGICNCFPDEKKCFCEPEDSQGPLCDELCRTVITAAVLFSFIISVLLSTFCIHR
YHKHAHKPPIASAEMTFCRPAQGFPISYSSSGTRRPSLDSMENQVSVDSFKIPEDPKWEF
PRKNLVLGKTLGEGEFGKVVKATAFRLKGRAGYTTVAVKMLKENASQSELRDLLSEFNLL
KQVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRDSRKIGPAYVSSGGSRNSSSLD
HPDERVLTMGDLISFAWQISRGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDV
YEEDSYVKKSKGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPER
LFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKSRDYLDLA
ASTPSDSLLYDDGLSEEETPLVDCNSAPLPRSLPSTWIENKLYGMSDPNWPGESPVPLTR
ADGTSTGFPRYANDSVYANWMVSPSAAKLMDTFDS
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BDBM347342 |
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n/a |
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Name | BDBM347342 |
Synonyms: | 2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide | US9789100, Example 30 |
Type | Small organic molecule |
Emp. Form. | C22H21F4N3O4 |
Mol. Mass. | 467.4135 |
SMILES | CCOc1cc(=O)[nH]cc1-c1ccc(CC(=O)Nc2cc(on2)C(C)(C)C(F)(F)F)c(F)c1 |
Structure |
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