Target
Mitogen-activated protein kinase kinase kinase 12
Ligand
BDBM289474
Substrate
n/a
Meas. Tech.
Biological Activity Assay
Kd
9.50±n/a nM
Citation
 Soth, MJLiu, GLe, KCross, JJones, P Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease US Patent  US10093664 Publication Date 10/9/2018 
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:
BDBM289474
Synonyms:
5-(2-(sec-butyl)-1-(3- morpholinobicyclo- [1.1.1]pentan-1-yl)-1H- imidazol-4-yl)-3-(tri- fluoromethyl)pyridin-2- amine | US10093664, Example 50
Type:
Small organic molecule
Emp. Form.:
C22H28F3N5O
Mol. Mass.:
435.4858
SMILES:
CCC(C)c1nc(cn1C12CC(C1)(C2)N1CCOCC1)-c1cnc(N)c(c1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: