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Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM500543
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  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:
BDBM500543
Synonyms:
4-(7-fluoroimidazo [1,2-a]pyridin- 3-yl)-7-[[5- 1(3R)-3-(1- hydroxy-1- methyl-ethyl)- 1-piperidyl]-2- pyridyl]amino] isoindolin-1-one | US11021481, Compound I-202 | US11078201, Compound I-202 | US11548890, Compound I-202
Type:
Small organic molecule
Emp. Form.:
C28H29FN6O2
Mol. Mass.:
500.5673
SMILES:
CC(C)(O)[C@@H]1CCCN(C1)c1ccc(Nc2ccc(c3CNC(=O)c23)-c2cnc3cc(F)ccn23)nc1 |r|
Structure:
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