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TargetMitogen-activated protein kinase kinase kinase 12
LigandBDBM50128340
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1523510 (CHEMBL3631014)
IC50 8600±n/a nM
Citation Patel, SHarris, SFGibbons, PDeshmukh, GGustafson, AKellar, TLin, HLiu, XLiu, YLiu, YMa, CScearce-Levie, KGhosh, ASShin, YGSolanoy, HWang, JWang, BYin, JSiu, MLewcock, JW Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12). J Med Chem58:8182-99 (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 | 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:
BDBM50128340
n/a
NameBDBM50128340
Synonyms:CHEMBL3629173
TypeSmall organic molecule
Emp. Form.C20H23N5OS
Mol. Mass.381.495
SMILESN#Cc1ccnc(Nc2nc(C3CC3)c(s2)C2CCN(CC2)C2COC2)c1
Structure
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