Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM501162
Substrate
n/a
Meas. Tech.
Biochemical Enzyme Assay
IC50
<100±n/a nM
Citation
 Kaila, NLinney, IWard, SWishart, GWhittaker, BCote, AGreenwood, JRLeffler, AAlbanese, SKSeverance, DL Substituted isoindolin-1-ones and 2,3-dihydro-1h-pyrrolo[3,4-c]pyridin-1-ones as HPK1 antagonists US Patent  US11021481 Publication Date 6/1/2021 
Target
Name:
Mitogen-activated protein kinase kinase kinase kinase 1
Synonyms:
HPK1 | M4K1_HUMAN | MAP4K1
Type:
PROTEIN
Mol. Mass.:
91316.07
Organism:
Homo sapiens (Human)
Description:
ChEMBL_586597
Residue:
833
Sequence:
MDVVDPDIFNRDPRDHYDLLQRLGGGTYGEVFKARDKVSGDLVALKMVKMEPDDDVSTLQKEILILKTCRHANIVAYHGSYLWLQKLWICMEFCGAGSLQDIYQVTGSLSELQISYVCREVLQGLAYLHSQKKIHRDIKGANILINDAGEVRLADFGISAQIGATLARRLSFIGTPYWMAPEVAAVALKGGYNELCDIWSLGITAIELAELQPPLFDVHPLRVLFLMTKSGYQPPRLKEKGKWSAAFHNFIKVTLTKSPKKRPSATKMLSHQLVSQPGLNRGLILDLLDKLKNPGKGPSIGDIEDEEPELPPAIPRRIRSTHRSSSLGIPDADCCRRHMEFRKLRGMETRPPANTARLQPPRDLRSSSPRKQLSESSDDDYDDVDIPTPAEDTPPPLPPKPKFRSPSDEGPGSMGDDGQLSPGVLVRCASGPPPNSPRPGPPPSTSSPHLTAHSEPSLWNPPSRELDKPPLLPPKKEKMKRKGCALLVKLFNGCPLRIHSTAAWTHPSTKDQHLLLGAEEGIFILNRNDQEATLEMLFPSRTTWVYSINNVLMSLSGKTPHLYSHSILGLLERKETRAGNPIAHISPHRLLARKNMVSTKIQDTKGCRACCVAEGASSGGPFLCGALETSVVLLQWYQPMNKFLLVRQVLFPLPTPLSVFALLTGPGSELPAVCIGVSPGRPGKSVLFHTVRFGALSCWLGEMSTEHRGPVQVTQVEEDMVMVLMDGSVKLVTPEGSPVRGLRTPEIPMTEAVEAVAMVGGQLQAFWKHGVQVWALGSDQLLQELRDPTLTFRLLGSPRLECSGTISPHCNLLLPGSSNSPASASRVAGITGL
  
Inhibitor
Name:
BDBM501162
Synonyms:
7-((6- ((dimethylamino)- methyl)-5-(4- fluorotetrahy- dro-2H-pyran-4- yl)pyridin-2- yl)amino)-4-(7- fluoroimidazo [1,2-a]pyridin- 3-yl)isoindolin- 1-on e | US11021481, Compound I-834 | US11078201, Compound I-834 | US11548890, Compound I-834
Type:
Small organic molecule
Emp. Form.:
C28H28F2N6O2
Mol. Mass.:
518.5577
SMILES:
CN(C)Cc1nc(Nc2ccc(c3CNC(=O)c23)-c2cnc3cc(F)ccn23)ccc1C1(F)CCOCC1
Structure:
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