Target
Mitogen-activated protein kinase kinase kinase 12
Ligand
BDBM365305
Substrate
n/a
Meas. Tech.
TR-FRET assay
Ki
0.500±n/a nM
Citation
 Cohen, FPatel, S C-linked heterocycloaklyl substituted pyrimidines and their uses US Patent  US9868720 Publication Date 1/16/2018 
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:
BDBM365305
Synonyms:
US9868720, No. 426 | {3-[2-(3,3-Difluoro- pyrrolidin-1-yl)-6-(4-methyl- pyridin-2-ylamino)-pyrimidin- 4-yl]-piperidin- 1-yl}-(2-methoxy-4- methyl-phenyl)-methanone
Type:
Small organic molecule
Emp. Form.:
C28H32F2N6O2
Mol. Mass.:
522.5895
SMILES:
COc1cc(C)ccc1C(=O)N1CCCC(C1)c1cc(Nc2cc(C)ccn2)nc(n1)N1CCC(F)(F)C1
Structure:
Search PDB for entries with ligand similarity: