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Target
Mitogen-activated protein kinase kinase kinase 12
Ligand
BDBM365298
Substrate
n/a
Meas. Tech.
TR-FRET assay
Ki
4.92±n/a nM
Citation
 Cohen, F; Patel, 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:
BDBM365298
Synonyms:
US9868720, No. 404 | {2-(3,3-Difluoro-pyrrolidin- 1-yl)-6-[1-(1H-pyrazol- 4-ylmethyl)-pyrrolidin- 3-yl]-pyrimidin-4- yl}-(4-trifluoromethyl- pyridin-2-yl)-amine
Type:
Small organic molecule
Emp. Form.:
C22H23F5N8
Mol. Mass.:
494.4636
SMILES:
FC(F)(F)c1ccnc(Nc2cc(nc(n2)N2CCC(F)(F)C2)C2CCN(Cc3cn[nH]c3)C2)c1
Structure:
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