Reaction Details |
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Target | Mitogen-activated protein kinase kinase kinase 12 |
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Ligand | BDBM50128340 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1523510 (CHEMBL3631014) |
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IC50 | 8600±n/a nM |
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Citation | Patel, S; Harris, SF; Gibbons, P; Deshmukh, G; Gustafson, A; Kellar, T; Lin, H; Liu, X; Liu, Y; Liu, Y; Ma, C; Scearce-Levie, K; Ghosh, AS; Shin, YG; Solanoy, H; Wang, J; Wang, B; Yin, J; Siu, M; Lewcock, 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 |
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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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BDBM50128340 |
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n/a |
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Name | BDBM50128340 |
Synonyms: | CHEMBL3629173 |
Type | Small organic molecule |
Emp. Form. | C20H23N5OS |
Mol. Mass. | 381.495 |
SMILES | N#Cc1ccnc(Nc2nc(C3CC3)c(s2)C2CCN(CC2)C2COC2)c1 |
Structure |
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