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TargetMitogen-activated protein kinase kinase kinase 12
LigandBDBM50059199
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1460554
IC50 193±n/a nM
Citation Patel, SCohen, FDean, BJDe La Torre, KDeshmukh, GEstrada, AAGhosh, ASGibbons, PGustafson, AHuestis, MPLe Pichon, CELin, HLiu, WLiu, XLiu, YLy, CQLyssikatos, JPMa, CScearce-Levie, KShin, YGSolanoy, HStark, KLWang, JWang, BZhao, XLewcock, JWSiu, M Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models. J Med Chem58:401-18 (2015) [PubMed]  Article
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 | MAPK-upstream kinase | MUK | 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:
BDBM50059199
NameBDBM50059199
Synonyms:CHEMBL3393331
TypeSmall organic molecule
Emp. Form.C19H18F2N6
Mol. Mass.368.3832
SMILESCC(C)(C#N)c1cc(Nc2cc(ccn2)C#N)nc(c1)N1CCC(F)(F)C1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a