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TargetProto-oncogene tyrosine-protein kinase receptor Ret
LigandBDBM347342
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1764328 (CHEMBL4199575)
Kd 20.0±n/a nM
Citation Schenck Eidam, HRussell, JRaha, KDeMartino, MQin, DGuan, HAZhang, ZZhen, GYu, HWu, CPan, YJoberty, GZinn, NLaquerre, SRobinson, SWhite, AGiddings, AMohammadi, EGreenwood-Van Meerveld, BOliff, AKumar, SCheung, 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
More Info.:Get all data from this article,  Assay Method
 
Proto-oncogene tyrosine-protein kinase receptor Ret
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM347342
n/a
NameBDBM347342
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
TypeSmall organic molecule
Emp. Form.C22H21F4N3O4
Mol. Mass.467.4135
SMILESCCOc1cc(=O)[nH]cc1-c1ccc(CC(=O)Nc2cc(on2)C(C)(C)C(F)(F)F)c(F)c1
Structure
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