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Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM500596
Substrate
n/a
Meas. Tech.
Biochemical Enzyme Assay
IC50
<100±n/a nM
Citation
 Kaila, N; Linney, I; Ward, S; Wishart, G; Whittaker, B; Cote, A; Greenwood, JR; Leffler, A; Albanese, SK; Severance, 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:
BDBM500596
Synonyms:
7-((5-(4- methylpiperazin- 1-yl)pyridin- 2-yl)amino)-4- (4,5,6,7- tetrahydropyra- zolo[1,5- a]pyridin-3- yl)-2,3- dihydro-1H- pyrrolo[3,4- c]pyridin-1-one | US11021481, Compound I-255 | US11078201, Compound I-255 | US11548890, Compound I-255
Type:
Small organic molecule
Emp. Form.:
C24H28N8O
Mol. Mass.:
444.5321
SMILES:
CN1CCN(CC1)c1ccc(Nc2cnc(c3CNC(=O)c23)-c2cnn3CCCCc23)nc1
Structure:
Search PDB for entries with ligand similarity: