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TargetMitogen-activated protein kinase kinase kinase 12
LigandBDBM301518
Substrate/Competitorn/a
Meas. Tech.DLK TR-FRET Inhibition Assay
Ki 4.92±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:
BDBM301518
n/a
NameBDBM301518
Synonyms:US10131675, Example 3
TypeSmall organic molecule
Emp. Form.C23H25N7O
Mol. Mass.415.4909
SMILESCc1c[nH]c2ncc(cc12)-c1nc(N2CC3CC2C3)c2nc3n(CCOC3(C)C)c2n1 |(-6.24,-.74,;-5.47,-2.07,;-6.37,-3.32,;-5.47,-4.56,;-4,-4.09,;-2.67,-4.86,;-1.33,-4.09,;-1.33,-2.55,;-2.67,-1.78,;-4,-2.55,;,-1.78,;1.33,-2.55,;2.67,-1.78,;4,-2.55,;5.47,-2.07,;6.37,-3.32,;5.47,-4.56,;4,-4.09,;4.83,-3.32,;2.67,-.24,;3.81,.8,;3.19,2.2,;1.65,2.04,;.75,3.29,;1.37,4.69,;2.91,4.86,;3.81,3.61,;4.9,4.7,;5.3,3.21,;1.33,.53,;,-.24,)|
Structure
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