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Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM591144
Substrate
n/a
Meas. Tech.
HPK1-FL HTRF Enzymatic Assay
Ki
0.013±n/a nM
Citation
 Chan, B; Drobnick, J; Gazzard, L; Heffron, T; Liang, J; Malhotra, S; Mendonca, R; Rajapaksa, N; Stivala, C; Tellis, J; Wang, W; Wei, B; Zhou, A; Cartwright, MW; Lainchbury, M; Gancia, E; Seward, E; Madin, A; Favor, D; Fong, KC; Hu, Y; Good, A Isoquinolines as inhibitors of HPK1 US Patent  US11566003 Publication Date 1/31/2023 
Target
Name:
Mitogen-activated protein kinase kinase kinase kinase 1
Synonyms:
HPK1 | M4K1_HUMAN | MAP4K1
Type:
PROTEIN
Mol. Mass.:
91316.07
Organism:
Human
Description:
ChEMBL_586597
Residue:
833
Sequence:
MDVVDPDIFNRDPRDHYDLLQRLGGGTYGEVFKARDKVSGDLVALKMVKMEPDDDVSTLQKEILILKTCRHANIVAYHGSYLWLQKLWICMEFCGAGSLQDIYQVTGSLSELQISYVCREVLQGLAYLHSQKKIHRDIKGANILINDAGEVRLADFGISAQIGATLARRLSFIGTPYWMAPEVAAVALKGGYNELCDIWSLGITAIELAELQPPLFDVHPLRVLFLMTKSGYQPPRLKEKGKWSAAFHNFIKVTLTKSPKKRPSATKMLSHQLVSQPGLNRGLILDLLDKLKNPGKGPSIGDIEDEEPELPPAIPRRIRSTHRSSSLGIPDADCCRRHMEFRKLRGMETRPPANTARLQPPRDLRSSSPRKQLSESSDDDYDDVDIPTPAEDTPPPLPPKPKFRSPSDEGPGSMGDDGQLSPGVLVRCASGPPPNSPRPGPPPSTSSPHLTAHSEPSLWNPPSRELDKPPLLPPKKEKMKRKGCALLVKLFNGCPLRIHSTAAWTHPSTKDQHLLLGAEEGIFILNRNDQEATLEMLFPSRTTWVYSINNVLMSLSGKTPHLYSHSILGLLERKETRAGNPIAHISPHRLLARKNMVSTKIQDTKGCRACCVAEGASSGGPFLCGALETSVVLLQWYQPMNKFLLVRQVLFPLPTPLSVFALLTGPGSELPAVCIGVSPGRPGKSVLFHTVRFGALSCWLGEMSTEHRGPVQVTQVEEDMVMVLMDGSVKLVTPEGSPVRGLRTPEIPMTEAVEAVAMVGGQLQAFWKHGVQVWALGSDQLLQELRDPTLTFRLLGSPRLECSGTISPHCNLLLPGSSNSPASASRVAGITGL
  
Inhibitor
Name:
BDBM591144
Synonyms:
(1R,2S,3R)-N-(8-amino-7-fluoro-6-(8-methyl-2,3-dihydro-1H-pyrido[2,3-b][1,4]oxazin-7-yl)isoquinolin-3-yl)-2-methyl-3-(1-methyl-1H-pyrazol-4-yl)cyclopropane-1-carboxamide | US11566003, Compound 33
Type:
Small organic molecule
Emp. Form.:
C26H26FN7O2
Mol. Mass.:
487.5287
SMILES:
C[C@@H]1[C@@H]([C@H]1c1cnn(C)c1)C(=O)Nc1cc2cc(c(F)c(N)c2cn1)-c1cnc2OCCNc2c1C |r|
Structure:
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