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Target
Mitogen-activated protein kinase kinase kinase 12
Ligand
BDBM50059253
Substrate
n/a
Meas. Tech.
ChEMBL_1460553 (CHEMBL3395585)
Ki
691±n/a nM
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 Chem 58:401-18 (2015) [PubMed]  Article 
Target
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:
MACLHETRTPSPSFGGFVSTLSEASMRKLDPDTSDCTPEKDLTPTHVLQLHEQDAGGPGGAAGSPESRASRVRADEVRLQCQSGSGFLEGLFGCLRPVWTMIGKAYSTEHKQQQEDLWEVPFEEILDLQWVGSGAQGAVFLGRFHGEEVAVKKVRDLKETDIKHLRKLKHPNIITFKGVCTQAPCYCILMEFCAQGQLYEVLRAGRPVTPSLLVDWSMGIAGGMNYLHLHKIIHRDLKSPNMLITYDDVVKISDFGTSKELSDKSTKMSFAGTVAWMAPEVIRNEPVSEKVDIWSFGVVLWELLTGEIPYKDVDSSAIIWGVGSNSLHLPVPSSCPDGFKILLRQCWNSKPRNRPSFRQILLHLDIASADVLSTPQETYFKSQAEWREEVKLHFEKIKSEGTCLHRLEEELVMRRREELRHALDIREHYERKLERANNLYMELNALMLQLELKERELLRREQALERRCPGLLKPHPSRGLLHGNTMEKLIKKRNVPQKLSPHSKRPDILKTESLLPKLDAALSGVGLPGCPKGPPSPGRSRRGKTRHRKASAKGSCGDLPGLRTAVPPHEPGGPGSPGGLGGGPSAWEACPPALRGLHHDLLLRKMSSSSPDLLSAALGSRGRGATGGAGDPGSPPPARGDTPPSEGSAPGSTSPDSPGGAKGEPPPPVGPGEGVGLLGTGREGTSGRGGSRAGSQHLTPAALLYRAAVTRSQKRGISSEEEEGEVDSEVELTSSQRWPQSLNMRQSLSTFSSENPSDGEEGTASEPSPSGTPEVGSTNTDERPDERSDDMCSQGSEIPLDPPPSEVIPGPEPSSLPIPHQELLRERGPPNSEDSDCDSTELDNSNSVDALRPPASLPP
  
Inhibitor
Name:
BDBM50059253
Synonyms:
CHEMBL3393311 | US9868720, No. 3
Type:
Small organic molecule
Emp. Form.:
C23H22F3N5O
Mol. Mass.:
441.4489
SMILES:
Cc1nc(Nc2ccc(cn2)C(F)(F)F)cc(n1)C1CCCN(C1)C(=O)c1ccccc1
Structure:
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