Reaction Details |
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Target | Mitogen-activated protein kinase kinase kinase 12 |
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Ligand | BDBM50059211 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1460554 (CHEMBL3395586) |
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IC50 | 1300±n/a nM |
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Citation | Patel, S; Cohen, F; Dean, BJ; De La Torre, K; Deshmukh, G; Estrada, AA; Ghosh, AS; Gibbons, P; Gustafson, A; Huestis, MP; Le Pichon, CE; Lin, H; Liu, W; Liu, X; Liu, Y; Ly, CQ; Lyssikatos, JP; Ma, C; Scearce-Levie, K; Shin, YG; Solanoy, H; Stark, KL; Wang, J; Wang, B; Zhao, X; Lewcock, JW; Siu, M Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models. J Med Chem58:401-18 (2015) [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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BDBM50059211 |
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n/a |
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Name | BDBM50059211 |
Synonyms: | CHEMBL3393314 |
Type | Small organic molecule |
Emp. Form. | C25H29N5O |
Mol. Mass. | 415.5307 |
SMILES | CC(C)c1ccnc(Nc2cc(nc(C)n2)C2CCCN(C2)C(=O)c2ccccc2)c1 |
Structure |
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