Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM501131
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  US11034694 Publication Date 6/15/2021 
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:
BDBM501131
Synonyms:
(R)-7-((6- ((dimethylamino)- methyl)-5-(3- hydroxytetra- hydrofuran-3- yl)pyridin-2- yl)amino)-4- (7-fluoroimidazo [1,2-a]pyridin- 3-yl)isoindolin- 1-one | US11021481, Compound I-803 | US11078201, Compound I-803 | US11548890, Compound I-803
Type:
Small organic molecule
Emp. Form.:
C27H27FN6O3
Mol. Mass.:
502.5401
SMILES:
CN(C)Cc1nc(Nc2ccc(c3CNC(=O)c23)-c2cnc3cc(F)ccn23)ccc1[C@@]1(O)CCOC1 |r|
Structure:
Search PDB for entries with ligand similarity: