Reaction Details |
| Report a problem with these data |
Target | Mitogen-activated protein kinase kinase kinase 12 |
---|
Ligand | BDBM50128333 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1523510 (CHEMBL3631014) |
---|
IC50 | 721±n/a nM |
---|
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 |
---|
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
|
|
|
BDBM50128333 |
---|
n/a |
---|
Name | BDBM50128333 |
Synonyms: | CHEMBL3629014 |
Type | Small organic molecule |
Emp. Form. | C22H26F2N6O |
Mol. Mass. | 428.4782 |
SMILES | FC1(F)CCC(C1)n1nc(Nc2cc(ccn2)C#N)cc1C1CCN(CC1)C1COC1 |
Structure |
|