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Target
Mitogen-activated protein kinase kinase kinase 12
Ligand
BDBM289483
Substrate
n/a
Meas. Tech.
DLK Kd Determinations
Kd
0.300±n/a nM
Citation
 Soth, MJ; Le, K; Jones, P; Cross, J Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease US Patent  US11560366 Publication Date 1/24/2023 
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:
BDBM289483
Synonyms:
1-(4-(6-amino-5- (trifluoromethyl)- pyridin-3-yl)-1-(bi- cyclo[1.1.1]pentan-1- yl)-1H-imidazol-2-yl)- 2-methylpropan-1-ol | US10093664, Example 59 | US11560366, Example 14
Type:
Small organic molecule
Emp. Form.:
C18H21F3N4O
Mol. Mass.:
366.3807
SMILES:
CC(C)C(O)c1nc(cn1C12CC(C1)C2)-c1cnc(N)c(c1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: