Target
Mitogen-activated protein kinase kinase kinase 12
Ligand
BDBM301659
Substrate
n/a
Meas. Tech.
DLK TR-FRET Inhibition Assay
Ki
32.2±n/a nM
Citation
 Estrada, APatel, SKellar, THuestis, MShore, DSiu, M Tricyclic DLK inhibitors and uses thereof US Patent  US10131675 Publication Date 11/20/2018 
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:
BDBM301659
Synonyms:
US10131675, Example 146
Type:
Small organic molecule
Emp. Form.:
C21H22N8O
Mol. Mass.:
402.4524
SMILES:
CC1(C)OCCn2c1nc1c(nc(nc21)-c1cnc2[nH]cnc2c1)N1CC2CC1C2 |(6.17,1.48,;5.4,2.82,;6.88,3.22,;5.24,4.35,;3.83,4.98,;2.58,4.07,;2.74,2.54,;4.15,1.91,;3.99,.38,;2.48,.06,;1.71,-1.27,;.17,-1.27,;-.6,.06,;.17,1.39,;1.71,1.39,;-2.14,.06,;-2.91,1.39,;-4.45,1.39,;-5.22,.06,;-6.72,-.26,;-6.88,-1.79,;-5.48,-2.42,;-4.45,-1.27,;-2.91,-1.27,;2.48,-2.61,;4.02,-2.61,;4.5,-4.07,;3.25,-4.98,;2.01,-4.07,;3.1,-2.98,)|
Structure:
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