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TargetMitogen-activated protein kinase kinase kinase 12
LigandBDBM301657
Substrate/Competitorn/a
Meas. Tech.DLK TR-FRET Inhibition Assay
Ki 2.23±n/a nM
Citation Estrada, APatel, SKellar, THuestis, MShore, DSiu, M Tricyclic DLK inhibitors and uses thereof US Patent US10131675 Publication Date 11/20/2018
More Info.:Get all data from this article,  Assay Method
 
Mitogen-activated protein kinase kinase kinase 12
Name:Mitogen-activated protein kinase kinase kinase 12
Synonyms:DLK | Dual leucine zipper bearing kinase | Leucine-zipper protein kinase | M3K12_HUMAN | MAP3K12 | MAPK-upstream kinase | MUK | Mitogen-activated protein kinase kinase kinase 12 | Mixed lineage kinase | ZPK
Type:PROTEIN
Mol. Mass.:93216.56
Organism:Homo sapiens (Human)
Description:ChEMBL_1460553
Residue:859
Sequence:
MACLHETRTPSPSFGGFVSTLSEASMRKLDPDTSDCTPEKDLTPTHVLQLHEQDAGGPGG
AAGSPESRASRVRADEVRLQCQSGSGFLEGLFGCLRPVWTMIGKAYSTEHKQQQEDLWEV
PFEEILDLQWVGSGAQGAVFLGRFHGEEVAVKKVRDLKETDIKHLRKLKHPNIITFKGVC
TQAPCYCILMEFCAQGQLYEVLRAGRPVTPSLLVDWSMGIAGGMNYLHLHKIIHRDLKSP
NMLITYDDVVKISDFGTSKELSDKSTKMSFAGTVAWMAPEVIRNEPVSEKVDIWSFGVVL
WELLTGEIPYKDVDSSAIIWGVGSNSLHLPVPSSCPDGFKILLRQCWNSKPRNRPSFRQI
LLHLDIASADVLSTPQETYFKSQAEWREEVKLHFEKIKSEGTCLHRLEEELVMRRREELR
HALDIREHYERKLERANNLYMELNALMLQLELKERELLRREQALERRCPGLLKPHPSRGL
LHGNTMEKLIKKRNVPQKLSPHSKRPDILKTESLLPKLDAALSGVGLPGCPKGPPSPGRS
RRGKTRHRKASAKGSCGDLPGLRTAVPPHEPGGPGSPGGLGGGPSAWEACPPALRGLHHD
LLLRKMSSSSPDLLSAALGSRGRGATGGAGDPGSPPPARGDTPPSEGSAPGSTSPDSPGG
AKGEPPPPVGPGEGVGLLGTGREGTSGRGGSRAGSQHLTPAALLYRAAVTRSQKRGISSE
EEEGEVDSEVELTSSQRWPQSLNMRQSLSTFSSENPSDGEEGTASEPSPSGTPEVGSTNT
DERPDERSDDMCSQGSEIPLDPPPSEVIPGPEPSSLPIPHQELLRERGPPNSEDSDCDST
ELDNSNSVDALRPPASLPP
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  Blast E-value cutoff:
BDBM301657
n/a
NameBDBM301657
Synonyms:US10131675, Example 144
TypeSmall organic molecule
Emp. Form.C22H23N7O
Mol. Mass.401.4643
SMILESCC1(C)OCCn2c1nc1c(nc(cc21)-c1cnc(N)c(c1)C#N)N1CC2CC1C2 |(-6.27,.53,;-5.87,-.96,;-7.36,-.56,;-6.5,-2.37,;-5.6,-3.61,;-4.06,-3.45,;-3.44,-2.05,;-4.34,-.8,;-3.44,.45,;-1.97,-.03,;-.64,.74,;.69,-.03,;.69,-1.57,;-.64,-2.34,;-1.97,-1.57,;2.03,-2.34,;2.03,-3.88,;3.36,-4.65,;4.7,-3.88,;6.03,-4.65,;4.7,-2.34,;3.36,-1.57,;6.03,-1.57,;7.36,-.8,;-.64,2.28,;-1.89,3.19,;-1.41,4.65,;.13,4.65,;.61,3.19,;-.64,3.32,)|
Structure
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