Target
Mitogen-activated protein kinase kinase kinase 12
Ligand
BDBM301562
Substrate
n/a
Meas. Tech.
DLK TR-FRET Inhibition Assay
Ki
992±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:
Human
Description:
ChEMBL_1460553
Residue:
859
Sequence:
MACLHETRTPSPSFGGFVSTLSEASMRKLDPDTSDCTPEKDLTPTHVLQLHEQDAGGPGGAAGSPESRASRVRADEVRLQCQSGSGFLEGLFGCLRPVWTMIGKAYSTEHKQQQEDLWEVPFEEILDLQWVGSGAQGAVFLGRFHGEEVAVKKVRDLKETDIKHLRKLKHPNIITFKGVCTQAPCYCILMEFCAQGQLYEVLRAGRPVTPSLLVDWSMGIAGGMNYLHLHKIIHRDLKSPNMLITYDDVVKISDFGTSKELSDKSTKMSFAGTVAWMAPEVIRNEPVSEKVDIWSFGVVLWELLTGEIPYKDVDSSAIIWGVGSNSLHLPVPSSCPDGFKILLRQCWNSKPRNRPSFRQILLHLDIASADVLSTPQETYFKSQAEWREEVKLHFEKIKSEGTCLHRLEEELVMRRREELRHALDIREHYERKLERANNLYMELNALMLQLELKERELLRREQALERRCPGLLKPHPSRGLLHGNTMEKLIKKRNVPQKLSPHSKRPDILKTESLLPKLDAALSGVGLPGCPKGPPSPGRSRRGKTRHRKASAKGSCGDLPGLRTAVPPHEPGGPGSPGGLGGGPSAWEACPPALRGLHHDLLLRKMSSSSPDLLSAALGSRGRGATGGAGDPGSPPPARGDTPPSEGSAPGSTSPDSPGGAKGEPPPPVGPGEGVGLLGTGREGTSGRGGSRAGSQHLTPAALLYRAAVTRSQKRGISSEEEEGEVDSEVELTSSQRWPQSLNMRQSLSTFSSENPSDGEEGTASEPSPSGTPEVGSTNTDERPDERSDDMCSQGSEIPLDPPPSEVIPGPEPSSLPIPHQELLRERGPPNSEDSDCDSTELDNSNSVDALRPPASLPP
  
Inhibitor
Name:
BDBM301562
Synonyms:
US10131675, Example 48
Type:
Small organic molecule
Emp. Form.:
C21H25N7O
Mol. Mass.:
391.4695
SMILES:
Cc1cc(cnc1N)-c1nc(N2CC3CC2C3)c2nc3n(CCOC3(C)C)c2n1 |(2.61,5.31,;1.27,4.54,;1.27,3,;-.06,2.23,;-1.39,3,;-1.39,4.54,;-.06,5.31,;-.06,6.85,;-.06,.69,;1.27,-.08,;1.27,-1.62,;2.61,-2.39,;2.61,-3.93,;4.07,-4.41,;4.98,-3.16,;4.07,-1.92,;3.36,-3.15,;-.06,-2.39,;-.38,-3.9,;-1.91,-4.06,;-2.54,-2.65,;-4.07,-2.49,;-4.98,-3.74,;-4.35,-5.15,;-2.82,-5.31,;-2.82,-6.85,;-1.73,-6.4,;-1.39,-1.62,;-1.39,-.08,)|
Structure:
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