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Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM591143
Substrate
n/a
Meas. Tech.
HPK1-FL HTRF Enzymatic Assay
Ki
0.014±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:
BDBM591143
Synonyms:
1-(8-amino-7-fluoro-6-(8-methyl- 2,3-dihydro-1H-pyrido[2,3- b][1,4]oxazin-7-yl)isoquinolin-3-yl)- 3-(cyclopropylmethyl)urea | US11566003, Compound 29
Type:
Small organic molecule
Emp. Form.:
C22H23FN6O2
Mol. Mass.:
422.4554
SMILES:
Cc1c2NCCOc2ncc1-c1cc2cc(NC(=O)NCC3CC3)ncc2c(N)c1F
Structure:
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