Reaction Details |
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Target | Mitogen-activated protein kinase kinase kinase 12 |
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Ligand | BDBM50271219 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1709819 (CHEMBL4119868) |
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IC50 | 274±n/a nM |
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Citation | Patel, S; Meilandt, WJ; Erickson, RI; Chen, J; Deshmukh, G; Estrada, AA; Fuji, RN; Gibbons, P; Gustafson, A; Harris, SF; Imperio, J; Liu, W; Liu, X; Liu, Y; Lyssikatos, JP; Ma, C; Yin, J; Lewcock, JW; Siu, M Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease. J Med Chem60:8083-8102 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Mitogen-activated protein kinase kinase kinase 12 |
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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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BDBM50271219 |
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n/a |
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Name | BDBM50271219 |
Synonyms: | CHEMBL4125824 |
Type | Small organic molecule |
Emp. Form. | C21H26F3N5O |
Mol. Mass. | 421.4592 |
SMILES | [H][C@@]12CN(CC3COC3)C[C@]1([H])[C@H]2c1cc(nn1C(C)C)-c1cnc(N)c(c1)C(F)(F)F |r| |
Structure |
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